Gene Detail

Gene Symbol PIK3CA
Synonyms CLAPO | CLOVE | CWS5 | MCAP | MCM | MCMTC | p110-alpha | PI3K | PI3K-alpha
Gene Description PIK3CA, phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform, activates AKT/mTOR signaling to promote cell proliferation (PMID: 23411347). PIK3CA activating mutations have been identified in a number of tumor types such as breast cancer, colon cancer, endometrial cancer, glioblastoma, skin cancer, and ovarian cancer (PMID: 20535651).
Entrez Id 5290
Chromosome 3
Map Location 3q26.32
Canonical Transcript NM_006218

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Variant Impact Protein Effect Variant Description Associated with drug Resistance
G106V missense gain of function PIK3CA G106V does not lie within any known functional domains of the Pik3ca proten (UniProt.org). G106V results in activation of Pik3ca as indicated by increased Akt phosphorylation in cell culture (PMID: 21266528), increased cell invasion and migration in the context of an EGFR activating mutation in vitro (PMID: 29106415), and increased transformation ability in two different cell lines (PMID: 29533785).
R108H missense gain of function PIK3CA R108H lies within the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein (UniProt.org). R108H results in increased phosphorylation of Akt, activation of downstream signaling in cell culture (PMID: 18829572), and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
N1068Kfs*5 frameshift gain of function - predicted PIK3CA N1068Kfs*5 indicates a shift in the reading frame starting at the Pik3ca stop codon that results in the addition of 5 amino acids to the 1068 aa Pik3ca protein (UniProt.org). N1068Kfs*5 has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
E78K missense unknown PIK3CA E78K lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). E78K has been identified in the scientific literature (PMID: 27126994), but has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
F550S missense unknown PIK3CA F550S lies within the PIK helical domain of the Pik3ca protein (UniProt.org). F550S has been identified in sequencing studies (PMID: 17317825, PMID: 19487299), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
R777M missense unknown PIK3CA R777M does not lie within any known functional domains of the Pik3ca protein (UniProt.org). R777M has been identified in sequencing studies (PMID: 22810696), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
E110K missense unknown PIK3CA E110K does not lie within any known functional domains of the Pik3ca protein (UniProt.org). E110K has been identified in the scientific literature (PMID: 23619167), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
Q546_E547insQTS insertion unknown PIK3CA Q546_E547insQTS results in the insertion of three amino acids in the PIK helical domain of the Pik3ca protein between amino acids 546 and 547 (UniProt.org). Q546_E547insQTS has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
G512* nonsense loss of function - predicted PIK3CA G512* results in a premature truncation of the Pik3ca protein at amino acid 512 of 1068 (UniProt.org). Due to the loss of the PI3K/PI4K kinase domain (UniProt.org), G512* is predicted to lead to a loss of Pik3ca function.
E453Q missense gain of function PIK3CA E453Q lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E453Q confers a gain of function to Pik3ca as indicated by increased lipid kinase activity in cell culture (PMID: 15930273) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
H1048R missense unknown PIK3CA H1048R lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1048R has been identified in sequencing studies (PMID: 28638113), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
R93Q missense no effect - predicted PIK3CA R93Q lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R93Q results in Akt phosphorylation to levels similar to wild-type Pik3ca in cell culture (PMID: 21266528) and therefore, is predicted to have no effect on Pik3ca protein function.
positive unknown unknown PIK3CA positive indicates the presence of the PIK3CA gene, mRNA and/or protein.
G1049A missense unknown PIK3CA G1049A lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). G1049A has been identified in sequencing studies (PMID: 24062397), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Apr 2018).
V344G missense gain of function - predicted PIK3CA V344G lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). V344G has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
C420G missense unknown PIK3CA C420G lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). C420G results in increased Akt phosphorylation and cell proliferation, and is transforming in cell culture (PMID: 18074223), however in another study, C420G induced similar cell proliferation and cell viability as wild-type Pik3ca, in two different cell lines (PMID: 29533785).
P421L missense unknown PIK3CA P421L lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P421L has been identified in sequencing studies (PMID: 20049837), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
Q643H missense unknown PIK3CA Q643H lies within the PIK helical domain of the Pik3ca protein (UniProt.org). Q643H has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
G914R missense unknown PIK3CA G914R lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). G914R has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
F909L missense unknown PIK3CA F909L lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). F909L has been identified in the scientific literature (PMID: 24440717), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E218K missense no effect - predicted PIK3CA E218K lies within the PI3K-RBD domain of the Pik3ca protein (UniProt.org). E218K has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
R93W missense gain of function PIK3CA R93W lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R93W confers a gain of function on the Pik3ca protein as indicated by in increased phosphorylation of Akt in cell culture (PMID: 21266528) and increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
G1049S missense unknown PIK3CA G1049S lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). G1049S has been identified in the scientific literature (PMID: 17052259, PMID: 27177864), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E469delinsDK indel gain of function - predicted PIK3CA E469delinsDK results in the deletion of one amino acid within the C2 PI3K-type domain of the Pik3ca protein, combined with the insertion of an aspartic acid (D) and lysine (K) at the same site (UniProt.org). E469delinsDK has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
K111E missense gain of function PIK3CA K111E lies within the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein (UniProt.org). K111E confers a gain of function on the Pik3ca protein as indicated by increased lipid kinase activity and phosphorylation of Akt in cell culture (PMID: 22949682, PMID: 17376864) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
Q546K missense gain of function PIK3CA Q546K lies within the PIK helical domain of the Pik3ca protein (UniProt.org, PMID: 17376864). Q546K confers a gain of function to Pik3ca as indicated by constitutive phosphorylation of downstream targets Akt and S6, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
R115* nonsense loss of function - predicted PIK3CA R115* results in a premature truncation of the Pik3ca protein at amino acid 115 of 1068 (UniProt.org). Due to the loss of multiple functional domains, including the protein kinase domain (UniProt.org), R115* is predicted to lead to a loss of function.
H1047Y missense gain of function PIK3CA H1047Y is a hotspot mutation that lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1047Y confers a gain of function on the Pik3ca protein as indicated by increased phosphorylation of Akt, activation of downstream signaling, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
K179T missense unknown PIK3CA K179T does not lie within any known functional domains of the Pik3ca protein (UniProt.org). K179T has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E365K missense gain of function - predicted PIK3CA E365K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E365K is predicted to confer a gain of function to Pik3ca, as indicated by increased phosphorylation of downstream targets Akt, GSK3-beta, FoxO1, FoxO3a, and S6 in cell culture (PMID: 18829572, PMID: 21266528), and in one of two cell lines, increased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
A1046V missense unknown PIK3CA A1046V lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). A1046V has been identified in the scientific literature (PMID: 23107319, PMID: 26796526), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
E109del deletion unknown PIK3CA E109del results in the deletion of an amino acid in the Pik3ca protein at amino acid 109 (UniProt.org). E109del has been identified in sequencing studies (PMID: 25850943, PMID: 24121792), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
Q60K missense no effect PIK3CA Q60K lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). Q60K demonstrates kinase activity and transformation potential similar to wild-type Pik3ca protein (PMID: 18074223, PMID: 29533785).
V955I missense gain of function - predicted PIK3CA V955I lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). V955I results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2), and confers resistance to Erbitux (cetuximab) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function. Y
amp none no effect PIK3CA amplification indicates an increased number of copies of the PIK3CA gene. However, the mechanism causing the increase is unspecified.
E545K missense gain of function PIK3CA E545K is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E545K results in increased phosphorylation of Akt and Mek1/2, growth factor-independent cell survival, and is transforming in culture (PMID: 26627007, PMID: 29533785).
R108P missense unknown PIK3CA R108P lies within the p85 domain of the Pik3ca protein (PMID: 15016963). R108P has been identified in sequencing studies (PMID: 15016963), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
E453del deletion unknown PIK3CA E453del results in the deletion of one amino acid in the C2 PI3K-type domain of the Pik3ca protein at amino acid 453 (UniProt.org). E453del has been identified in sequencing studies (PMID: 20049837), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
C901F missense gain of function - predicted PIK3CA C901F lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). C901F has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
N1000D missense unknown PIK3CA N1000D lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). N1000D has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
R992P missense unknown PIK3CA R992P lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). R992P has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
D350N missense gain of function - predicted PIK3CA D350N lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). D350N has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
P447_L455del deletion gain of function PIK3CA P447_L455del results in the deletion of nine amino acids in the C2 PI3K-type domain of the Pik3ca protein from amino acids 447 to 455 (UniProt.org). P447_L455del confers a gain of function to the Pik3ca protein as demonstrated by transformation in culture and activation of the PI3K/Akt/Mtor pathway via increased phosphorylation of Akt, Erk, P70S6K, and P90RSK (PMID: 21266528, PMID: 29284706).
G451V missense unknown PIK3CA G451V lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). G451V has not been biochemically characterized, but in one of two cell lines, G451V induced increased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
V356I missense no effect - predicted PIK3CA V356I lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). V356I has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
G363A missense unknown PIK3CA G363A lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). G363A demonstrates increased PI3K pathway signaling and moderate growth in culture (PMID: 23619167), however in another study, G363A resulted in similar cell proliferation and viability levels as wild-type Pik3ca, in two different cell lines (PMID: 29533785).
R38S missense unknown PIK3CA R38S lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R38S has not been characterized, but is predicted to affect the enzymatic activity of Pik3ca by structural modeling (PMID: 19305151).
K111R missense unknown PIK3CA K111R does not lie within any known functional domains of the Pik3ca protein (UniProt.org). K111R has been identified in the sequencing studies (PMID: 23917401), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Oct 2018).
H1047T missense unknown PIK3CA H1047T lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1047T has been identified in the scientific literature (PMID: 29636477), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
V344M missense gain of function - predicted PIK3CA V344M lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). V344M has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
E726K missense gain of function - predicted PIK3CA E726K does not lie within any known functional domains of the Pik3ca protein (UniProt.org). E726K has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation in cell culture (PMID: 29533785).
R617W missense unknown PIK3CA R617W lies within the PIK helical domain of the Pik3ca protein (UniProt.org). R617W has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
V146I missense unknown PIK3CA V146I does not lie within any known functional domains of the Pik3ca protein (UniProt.org). V146I has been identified in the scientific literature (PMID: 26080840), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
E542Q missense unknown PIK3CA E542Q lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E542Q has not been biochemically characterized, but in one of two cell lines, E542Q induced similar cell proliferation and cell viability as wild-type Pik3ca (PMID: 29533785).
G106_R108del deletion gain of function PIK3CA G106_R108del results in the deletion of three amino acids in the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein from amino acids 106 to 108 (UniProt.org). G106_R108del results in increased phosphorylation of Akt and is transforming in cell culture (PMID: 19394761, PMID: 29533785).
Q546P missense gain of function PIK3CA Q546P lies within the PIK helical domain of the Pik3ca protein (UniProt.org). Q546P results in increased phosphorylation of Akt, activation of downstream signaling, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
E80K missense unknown PIK3CA E80K lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). E80K has been identified in sequencing studies (PMID: 22722201), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
P377R missense unknown PIK3CA P377R lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P377R has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
S773F missense unknown PIK3CA S773F does not lie within any known functional domains of the Pik3ca protein (UniProt.org). S773F has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
E547K missense loss of function - predicted PIK3CA E547K is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (PMID: 27177864, UniProt.org). E547K has not been biochemically characterized, but is predicted to confer a loss of function on the Pik3ca protein as demonstrated by decreased transformation ability as compared to wild-type Pik3ca (PMID: 29533785).
E545Q missense gain of function - predicted PIK3CA E545Q is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E545Q has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by growth factor-independent cell survival and transformation in culture (PMID: 26627007, PMID: 29533785).
T544I missense unknown PIK3CA T544I lies within the PIK helical domain of the Pik3ca protein (UniProt.org). T544I has been identified in the scientific literature (PMID: 25073438, PMID: 26276776), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
C378Y missense unknown PIK3CA C378Y lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). C378Y has not been biochemically characterized, but demonstrates increased transformation ability in one of two different cell lines (PMID: 29533785).
D549Y missense unknown PIK3CA D549Y lies within the PIK helical domain of the Pik3ca protein (UniProt.org). D549Y has been identified in the scientific literature (PMID: 28808038), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
S553N missense unknown PIK3CA S553N lies within the PIK helical domain of the Pik3ca protein (UniProt.org). S553N has been identified in the scientific literature (PMID: 23066039, PMID: 24983367), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
Y272* nonsense loss of function - predicted PIK3CA Y272* results in a premature truncation of the Pik3ca protein at amino acid 272 of 1068 (UniProt.org). Due to the loss of multiple functional domains in the Pik3ca protein (UniProt.org), Y272* is predicted to lead to a loss of function.
G451R missense gain of function - predicted PIK3CA G451R lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). G451R has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
P124L missense gain of function - predicted PIK3CA P124L does not lie within any known functional domains of the Pik3ca protein (UniProt.org). P124L results in activation of Pik3ca signaling as indicated by increased Akt phosphorylation in culture (PMID: 22430209) and therefore, is predicted to result in a gain of Pik3ca protein function.
R93P missense gain of function - predicted PIK3CA R93P lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R93P has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
K111N missense gain of function PIK3CA K111N lies within the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein (UniProt.org). K111N results in increased phosphorylation of Akt, activation of downstream signaling, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
dec exp none no effect PIK3CA dec exp indicates decreased expression of the Pik3ca protein and/or mRNA. However, the mechanism causing the decreased expression is unspecified.
E545A missense gain of function PIK3CA E545A is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E545A confers a gain of function on the Pik3ca protein as demonstrated by increased phosphorylation of Akt and transformation in cell culture (PMID: 17376864, PMID: 29533785).
E545X missense gain of function PIK3CA E545X indicates any Pik3ca missense mutation which results in the glutamic acid (E) at amino acid 545 being replaced by a different amino acid. PIK3CA E545X mutations are "hotspot" mutations resulting in increased Pik3ca kinase activity (PMID: 15930273).
K51N missense no effect - predicted PIK3CA K51N lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). K51N did not result in increased cell proliferation in culture compared to wild-type Pik3ca and therefore, is predicted to have no effect on Pik3ca protein function (PMID: 29636477).
G364R missense gain of function PIK3CA G364R lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). G364R results in increased phosphorylation of Akt in cell culture (PMID: 21266528) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
N345T missense gain of function - predicted PIK3CA N345T lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345T has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
E453K missense gain of function PIK3CA E453K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E453K results in increased phosphorylation of Akt and Mek1/2, enhanced cell survival, and is transforming in culture (PMID: 26627007, PMID: 29533785).
L339I missense unknown PIK3CA L339I lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). L339I has been identified in the scientific literature (PMID: 25078343), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
N345I missense gain of function - predicted PIK3CA N345I lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345I is predicted to confer a gain of function to the Pik3ca protein as indicated by increased cell survival, however, it is not transforming in culture (PMID: 26627007), but in two other studies, N345I demonstrated increased transformation ability in multiple different cell lines, as compared to wild-type Pik3ca (PMID: 29533785, PMID: 29636477).
A1020V missense no effect PIK3CA A1020V lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). A1020V demonstrates transformation potential and supports cell survival to similar level of wild-type Pik3ca protein in cell culture (PMID: 26627007, PMID: 29533785).
K966E missense gain of function - predicted PIK3CA K966E lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). K966E results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2), and confers resistance to Erbitux (cetuximab) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function. Y
P449_L455del deletion gain of function PIK3CA P449_L455del results in the deletion of seven amino acids in the C2 PI3K-type domain of the Pik3ca protein from amino acids 449 to 455 (UniProt.org). P449_L455del results in increased Akt phosphorylation in cell culture relative to wild-type Pik3ca in culture (PMID: 21266528) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
N1068fs frameshift gain of function PIK3CA N1068fs results in a change in the amino acid sequence of the Pik3ca protein beginning at the stop codon, aa 1068 (UniProt.org). N1068fs (reported as N1068fs*4) confers a gain of function to the Pik3ca protein, as demonstrated by activation of Akt/mTor signaling and tumorigenesis in transgenic animal models (PMID: 21703185).
R38C missense gain of function PIK3CA R38C lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R38C confers a gain of function to Pik3ca, as indicated by increased phosphorylation of downstream targets Akt, GSK3-beta, FoxO1, FoxO3a, and S6 in cell culture (PMID: 18829572) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
R398H missense no effect - predicted PIK3CA R398H lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). R398H has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
Y1021N missense unknown PIK3CA Y1021N lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). Y1021N has been identified in the scientific literature (PMID: 22949056, PMID: 15289301), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
act mut unknown gain of function PIK3CA act mut indicates that this variant results in a gain of function in the Pik3ca protein. However, the specific amino acid change has not been identified.
M1043T missense unknown PIK3CA M1043T lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1043T has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E109_I112delinsD indel gain of function - predicted PIK3CA E109_I112delinsD results in a deletion of four amino acids from amino acid 109 to 112 of the Pik3ca protein, combined with the insertion of an aspartic acid (D) at the same site (UniProt.org). E109_I112delinsD has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
I910V missense unknown PIK3CA I910V lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). I910V has not been biochemically characterized, but in one of two cell lines, I910V induced increased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
G1007R missense gain of function - predicted PIK3CA G1007R lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). G1007R has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
R93L missense unknown PIK3CA R93L lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R93L has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
T1025I missense unknown PIK3CA T1025I lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). T1025I has been identified in sequencing studies (PMID: 25680416, PMID: 22949056), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
R357Q missense unknown PIK3CA R357Q lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). R357Q has been identified in sequencing studies (PMID: 25233892, PMID: 23528559, PMID: 28446505), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
P466S missense unknown PIK3CA P466S lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P466S has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E103_G106delinsD indel gain of function - predicted PIK3CA E103_G106delinsD results in a deletion of 4 amino acids from amino acid 103 to 106 within the PI3K-ABD of the Pik3ca protein, combined with the insertion of an aspartic acid (D) at the same site (UniProt.org). E103_G106delinsD has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
M1040V missense no effect - predicted PIK3CA M1040V lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1040V has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
S405Y missense unknown PIK3CA S405Y lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). S405Y has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
E116K missense no effect PIK3CA E116K does not lie within any known functional domains of the Pik3ca protein (UniProt.org). E116K phosphorylates Akt to similar level of wild-type Pik3ca and is not transforming in culture (PMID: 17376864).
M1043V missense gain of function PIK3CA M1043V lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1043V confers a gain of function on the Pik3ca protein as indicated by increased phosphorylation of Akt, activation of downstream signaling, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
Q75K missense unknown PIK3CA Q75K lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). Q75K has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
P298S missense unknown PIK3CA P298S does not lie within any known functional domains of the Pik3ca protein (UniProt.org). P298S has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
Q546H missense unknown PIK3CA Q546H lies within the PIK helical domain of the Pik3ca protein (UniProt.org). Q546H has been identified in the scientific literature (PMID: 23370426, PMID: 19148475, PMID: 28860563), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
D520V missense unknown PIK3CA D520V lies within the PIK helical domain of the Pik3ca protein (UniProt.org). D520V has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R108C missense unknown PIK3CA R108C does not lie within any known functional domains of the Pik3ca protein (UniProt.org). R108C has not been biochemically characterized, but demonstrates increased transformation ability in one of two different cell lines (PMID: 29533785).
P539R missense gain of function PIK3CA P539R lies within the PIK helical domain of the Pik3ca protein (UniProt.org). P539R increases the stability of the Pik3ca protein, confers a gain of function, as indicated by constitutive phosphorylation of downstream targets Akt and S6, and is transforming in cell culture (PMID: 18951408, PMID: 17376864, PMID: 29533785).
N1044K missense gain of function PIK3CA N1044K lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). N1044K confers a gain of function to Pik3ca protein as indicated by increased cell survival and transforming ability in cell culture (PMID: 26627007, PMID: 29533785).
S332_L334del deletion loss of function - predicted PIK3CA S332_L334del results in the deletion of three amino acids in the Pik3ca protein from amino acids 332 to 334 (UniProt.org). S332_L334del has not been biochemically characterized, but is predicted to confer a loss of function on the Pik3ca protein as demonstrated by decreased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
F1039L missense unknown PIK3CA F1039L lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). F1039L has been identified in sequencing studies (PMID: 22949056, PMID: 19487299), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
H1065L missense unknown PIK3CA H1065L lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1065L has been identified in the scientific literature (PMID: 18084252), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E453A missense gain of function PIK3CA E453A lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E453A confers a gain of function to Pik3ca, as indicated by increased Akt phosphorylation in cell culture (PMID: 21266528) and increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
I112N missense unknown PIK3CA I112N does not lie within any known functional domains of the Pik3ca protein (UniProt.org). I112N has not been biochemically characterized, but demonstrates increased transformation ability in one of two different cell lines (PMID: 29533785).
R108L missense no effect - predicted PIK3CA R108L does not lie within any known functional domains of the Pik3ca protein (UniProt.org). R108L has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
T324I missense unknown PIK3CA T324I does not lie within any known functional domains of the Pik3ca protein (UniProt.org). T324I has been identified in the scientific literature (PMID: 16778113, PMID: 18343945), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
Q546E missense gain of function - predicted PIK3CA Q546E lies within the PIK helical domain of the Pik3ca protein (UniProt.org). Q546E has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased cell survival and transforming ability in cell culture (PMID: 26627007, PMID: 29533785).
H47R missense unknown PIK3CA H47R lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). H47R has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
P449T missense gain of function - predicted PIK3CA P449T lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P449T results in increased Pik3ca kinase activity in culture (PMID: 20530683) and therefore, is predicted to result in a gain of Pik3ca protein function.
R115L missense gain of function PIK3CA R115L does not lie within any known functional domains of the Pik3ca protein (UniProt.org). R115L confers a gain of function to the Pik3ca protein as demonstrated by increased cell growth, activation of the PI3K pathway (PMID: 23619167), and increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
R88Q missense gain of function PIK3CA R88Q lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R88Q confers a gain of function to the Pik3ca protein as indicated by increased phosphorylation of downstream targets Akt and S6 (PMID: 18829572) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
Y1021H missense unknown PIK3CA Y1021H lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). Y1021H has been identified in the scientific literature (PMID: 18084252, PMID: 27302833, PMID: 22610119), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
E545V missense unknown PIK3CA E545V is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E545V has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Sep 2018).
D1029H missense unknown PIK3CA D1029H lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). D1029H has been identified in the scientific literature (PMID: 22330809, PMID: 22949056, PMID: 23718828), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
F614I missense no effect - predicted PIK3CA F614I lies within the PIK helical domain of the Pik3ca protein (UniProt.org). F614I has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
Y1021F missense unknown PIK3CA Y1021F lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). Y1021F has been identified in the scientific literature (PMID: 22949056, PMID: 24440717), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R38G missense unknown PIK3CA R38G lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R38G has been identified in the scientific literature (PMID: 27425854), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
F930S missense gain of function - predicted PIK3CA F930S lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). F930S results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2), and confers resistance to Erbitux (cetuximab) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function. Y
I406V missense unknown PIK3CA I406V lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). I406V has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E542A missense gain of function - predicted PIK3CA E542A lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E542A has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
E978K missense unknown PIK3CA E978K lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). E978K has been identified in the scientific literature (PMID: 28119489), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
D1056G missense unknown PIK3CA D1056G lies within the PI3K/PI4K kinase domain of the Pik3ca protein (UniProt.org). D1056G has been identified in the scientific literature (PMID: 17317825), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
V955G missense gain of function - predicted PIK3CA V955G lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). V955G results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2), and confers resistance to Erbitux (cetuximab) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function. Y
D1045V missense unknown PIK3CA D1045V lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). D1045V has been identified in the scientific literature (PMID: 28936923), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
D926N missense unknown PIK3CA D926N lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). D926N has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
P487Q missense unknown PIK3CA P487Q lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P487Q has not been biochemically characterized, but in one of two cell lines, P487Q had decreased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
D1029Y missense gain of function PIK3CA D1029Y lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). D1029Y results in increased phosphorylation of Akt and is transforming in cell culture (PMID: 19394761).
E149G missense no effect - predicted PIK3CA E149G does not lie within any known functional domains of the Pik3ca protein (UniProt.org). E149G has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
V105_R108del deletion gain of function - predicted PIK3CA V105_R108del results in the deletion of four amino acids in the Pik3ca protein from amino acids 105 to 108 (UniProt.org). V105_R108del has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
H450_P458del deletion gain of function PIK3CA H450_P458del results in the deletion of nine amino acids in the C2 PI3K-type domain of the Pik3ca protein from amino acids 450 to 458 (UniProt.org). H450_P458del confers a gain of function to the Pik3ca protein as demonstrated by transformation in culture and activation of the PI3K/Akt/Mtor pathway via increased phosphorylation of Akt, Erk, P70S6K, and P90RSK (PMID: 29284706).
E522A missense unknown PIK3CA E522A lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E522A has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
mutant unknown unknown PIK3CA mutant indicates an unspecified mutation within the PIK3CA gene.
E545D missense gain of function - predicted PIK3CA E545D lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E545D has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
G12D missense unknown PIK3CA G12D does not lie within any known functional domains of the Pik3ca protein (UniProt.org). G12D has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
Y1021C missense unknown PIK3CA Y1021C lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). Y1021C has not been biochemically characterized, but demonstrates increased transformation ability in one of two different cell lines (PMID: 29533785).
V344A missense unknown PIK3CA V344A lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). V344A demonstrates AKT phosphorylation similar to wild-type Pik3ca protein in cell culture (PMID: 21266528), however in another study, V344A demonstrated increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
E81K missense unknown PIK3CA E81K lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). E81K results in increased Akt phosphorylation, activation of Mtor signaling, and growth advantage in patient-derived dermal fibroblasts in culture (PMID: 25915946), however in another study, E81K decreased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
N457K missense unknown PIK3CA N457K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N457K has been identified in the scientific literature (PMID: 19844788), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
C407F missense unknown PIK3CA C407F lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). C407F has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R818C missense no effect - predicted PIK3CA R818C lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). R818C has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
P449_N457del deletion gain of function - predicted PIK3CA P449_N457del results in the deletion of nine amino acids in the Pik3ca protein from amino acids 449 to 457 (UniProt.org). P449_N457del has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
A1035V missense unknown PIK3CA A1035V lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). A1035V has been identified in the scientific literature (PMID: 18193083, PMID: 22498935, PMID: 23665199), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
C407W missense unknown PIK3CA C407W lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). C407W has been identified in the scientific literature (PMID: 20826764, PMID: 25850943), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
H701P missense no effect PIK3CA H701P does not lie within any known functional domains of the Pik3ca protein (UniProt.org). H701P demonstrates transformation potential and ability to promote growth factor-independent cell survival at similar levels to wild-type Pik3ca protein in cell culture (PMID: 26627007, PMID: 29533785).
V952A missense gain of function - predicted PIK3CA V952A lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). V952A results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2), and confers resistance to Erbitux (cetuximab) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function. Y
T1025K missense unknown PIK3CA T1025K lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). T1025K has been identified in the scientific literature (PMID: 27672108), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
D300Y missense unknown PIK3CA D300Y does not lie within any known functional domains of the Pik3ca protein (UniProt.org). D300Y has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R88L missense unknown PIK3CA R88L lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R88L has been identified in the scientific literature (PMID: 27672108, PMID: 25233892), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
A1046E missense unknown PIK3CA A1046E lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). A1046E has been identified in the scientific literature (PMID: 18022911, PMID: 22357840, PMID: 22753589), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
S900I missense unknown PIK3CA S900I lies within the PI3K/PI4K kinase domain of the Pik3ca protein (UniProt.org). S900I has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
Y56H missense unknown PIK3CA Y56H lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). Y56H has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
H1047P missense unknown PIK3CA H1047P is a hotspot mutation that lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1047P has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Sep 2018).
E1037K missense gain of function - predicted PIK3CA E1037K lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). E1037K has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
E418K missense unknown PIK3CA E418K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E418K has been identified in sequencing studies (PMID: 25148578, PMID: 25344691, PMID: 25056374), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
H1047K missense unknown PIK3CA H1047K is a hotspot mutation that lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1047K has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Sep 2018).
C24Y missense no effect - predicted PIK3CA C24Y lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). C24Y has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
D350G missense gain of function PIK3CA D350G lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). D350G results in increased phosphorylation of Akt in cell culture (PMID: 24265155) and demonstrates increased transformation ability in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
A1046T missense unknown PIK3CA A1046T lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). A1046T has been identified in the scientific literature (PMID: 25150293, PMID: 22357840, PMID: 21239505), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R401Q missense unknown PIK3CA R401Q lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). R401Q has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
L866F missense unknown PIK3CA L866F lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). L866F has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
N345K missense gain of function PIK3CA N345K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345K results in increased phosphorylation of Akt, activation of downstream signaling, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
S629C missense gain of function - predicted PIK3CA S629C lies within the PIK helical domain of the Pik3ca protein (UniProt.org). S629C has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
M1043L missense gain of function - predicted PIK3CA M1043L lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1043L has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
I31M missense no effect PIK3CA I31M lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). I31M demonstrates transformation potential and ability to promote growth factor-independent cell survival at similar levels to wild-type Pik3ca protein in cell culture (PMID: 26627007, PMID: 29533785 ).
Q546R missense gain of function - predicted PIK3CA Q546R lies within the helical domain of the Pik3ca protein (PMID: 24559118). Q546R has not been biochemically characterized, but is predicted to confer a gain of function to the Pik3ca protein as demonstrated by increased cell survival and transforming ability in cell culture (PMID: 26627007, PMID: 29533785).
E103_P104del deletion gain of function - predicted PIK3CA E103_P104del results in the deletion of two amino acids in the Pik3ca protein from amino acids 103 to 104 (UniProt.org). E103_P104del has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
R770Q missense unknown PIK3CA R770Q does not lie within any known functional domains of the Pik3ca protein (UniProt.org). R770Q has been identified in the scientific literature (PMID: 24755471, PMID: 26681737), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R916C missense unknown PIK3CA R916C lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). R916C has been identified in sequencing studies (PMID: 24356096), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
D549H missense unknown PIK3CA D549H lies within the helical domain of the Pik3ca protein (PMID: 21829508). D549H has been identified in the scientific literature (PMID: 21667306, PMID: 22271473, PMID: 25426553), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
E453G missense unknown PIK3CA E453G lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E453G has been identified in sequencing studies (PMID: 26832993), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R108del deletion unknown PIK3CA R108del results in the deletion of one amino acid in the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein at amino acid 113 (UniProt.org). R108del has been identified in the scientific literature (PMID: 27161972), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
I910M missense unknown PIK3CA I910M lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). I910M has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
L456Afs*13 frameshift unknown PIK3CA L456Afs*13 indicates a shift in the reading frame starting at amino acid 456 and terminating 13 residues downstream causing a premature truncation of the 1068 amino acid Pik3ca protein (UniProt.org). L456Afs*13 has not been biochemically characterized, but demonstrates decreased transformation ability in one of two different cell lines (PMID: 29533785).
Y165H missense unknown PIK3CA Y165H does not lie within any known functional domains of the Pik3ca protein (UniProt.org). PIK3CA Y165H has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
D1045N missense unknown PIK3CA D1045N lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). D1045N has been identified in the scientific literature (PMID: 25624430, PMID: 26850916), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
M1040I missense unknown PIK3CA M1040I lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1040I has been identified in the scientific literature (PMID: 28240010, PMID: 25119929), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
G1049R missense gain of function PIK3CA G1049R lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). G1049R confers a gain of function on the Pik3ca protein as demonstrated by increased phosphorylation of Akt and Mek1/2, growth factor-independent cell survival, and transforming in cell culture (PMID: 26627007, PMID: 29533785).
R975S missense no effect - predicted PIK3CA R975S lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). R975S has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
E542G missense gain of function - predicted PIK3CA E542G lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E542G has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
R1023Q missense unknown PIK3CA R1023Q lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). R1023Q has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
P471L missense gain of function - predicted PIK3CA P471L lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P471L has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
P449L missense unknown PIK3CA P449L lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P449L has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
A1046_H1047insTSA insertion unknown PIK3CA A1046_H1047insTSA results in the insertion of three amino acids in the PI3K/PI4K domain of the Pik3ca protein between amino acids 1046 and 1047 (UniProt.org). A1046_H1047insTSA has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
C971R missense gain of function - predicted PIK3CA C971R lies within the PI3K/PI4K kinase domain of the Pik3ca protein (UniProt.org). C971R results in increased PI3K pathway signaling, moderate growth in culture (PMID: 23619167), but in one of two cell lines, C971R increased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to result in a gain of Pik3ca protein function.
C604R missense gain of function - predicted PIK3CA C604R lies within the PIK helical domain of the Pik3ca protein (UniProt.org). C604R has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
D538Y missense no effect - predicted PIK3CA D538Y lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). D538Y did not result in increased cell proliferation in culture compared to wild-type Pik3ca and therefore, is predicted to have no effect on Pik3ca protein function (PMID: 29636477).
G118D missense gain of function PIK3CA G118D lies within the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein (UniProt.org). G118D confers a gain of function on the Pik3ca protein as indicated by enhanced lipid kinase activity in cell culture, increased phosphorylation of Akt in cells derived from Cowden syndrome patients harboring germline mutations (PMID: 22949682, PMID: 23246288), and increased transformation ability in two different cell lines (PMID: 29533785).
C901Y missense unknown PIK3CA C901Y lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). C901Y has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
D454Y missense unknown PIK3CA D454Y lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). D454Y has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
I20M missense unknown PIK3CA I20M lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). I20M has been identified in the scientific literature (PMID: 28119489), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
W552G missense unknown PIK3CA W552G lies within the PIK helical domain of the Pik3ca protein (UniProt.org). W552G has been identified in the scientific literature (PMID: 16778113), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
H1047R missense gain of function PIK3CA H1047R is a hotspot mutation that lies within the kinase domain of the Pik3ca protein (UniProt.org). H1047R confers a gain of function on the Pik3ca protein as indicated by increased phosphorylation of Akt and Mek1/2, growth factor-independent cell survival, and transformation in cell culture (PMID: 26627007, PMID: 29533785).
H665Q missense unknown PIK3CA H665Q lies within the PIK helical domain of the Pik3ca protein (UniProt.org). H665Q has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
N1044S missense unknown PIK3CA N1044S lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). N1044S has been identified in sequencing studies (PMID: 17050665), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
N345Y missense unknown PIK3CA N345Y lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345Y has not been characterized and therefore its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E710G missense no effect - predicted PIK3CA E710G lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). E710G did not result in increased cell proliferation in culture compared to wild-type Pik3ca and therefore, is predicted to have no effect on Pik3ca protein function (PMID: 29636477).
D939G missense gain of function - predicted PIK3CA D939G lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). D939G has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
H1048L missense unknown PIK3CA H1048L lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). H1048L has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
R1023L missense unknown PIK3CA R1023L lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). R1023L has been identified in the scientific literature (PMID: 19844788, PMID: 28984400), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
T1025A missense gain of function - predicted PIK3CA T1025A lies within the PI3K/PI4K kinase domain of the Pik3ca protein (UniProt.org). T1025A has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
over exp none no effect PIK3CA over exp indicates an over expression of the Pik3ca protein and/or mRNA. However, the mechanism causing the over expression is unspecified.
E545G missense gain of function PIK3CA E545G is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E545G confers a gain of function on the Pik3ca protein as demonstrated by increased phosphorylation of Akt and transformation in cell culture (PMID: 17376864, PMID: 29533785).
C420R missense gain of function PIK3CA C420R lies within the C2 PI3K-type domain of the Pik3ca protein (PMID: 17376864). C420R confers a gain of function on Pik3ca, as indicated by constitutive phosphorylation of downstream targets Akt and S6, and is transforming in cell culture (PMID: 17376864, PMID: 29533785).
K111del deletion gain of function - predicted PIK3CA K111del results in the deletion of one amino acid in the Pik3ca protein at amino acid 111 (UniProt.org). K111del has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
T1025N missense gain of function - predicted PIK3CA T1025N lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). T1025N has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
C407Y missense unknown PIK3CA C407Y lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). C407Y has been identified in sequencing studies (PMID: 27302833), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
I391M missense unknown PIK3CA I391M lies within the C2 domain of the Pik3ca protein (UniProt.org). I391M demonstrated similar function to wild-type Pik3ca protein in cultured cells (PMID: 20530683), however in another study, I391M increased cell proliferation and cell viability as compared to wild-type Pik3ca, in one of two different cell lines (PMID: 29533785).
N1044D missense unknown PIK3CA N1044D lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). N1044D has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
Q546L missense gain of function - predicted PIK3CA Q546L lies within the PIK helical domain of the Pik3ca protein (UniProt.org). Q546L has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
H1047Q missense unknown PIK3CA H1047Q is a hotspot mutation that lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1047Q has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Sep 2018).
I889M missense unknown PIK3CA I889M lies within the PI3K/PI4K kinase domain of the Pik3ca protein (UniProt.org). I889M has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
Q75E missense unknown PIK3CA Q75E lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). Q75E has not been identified in sequencing studies (PMID: 28781987), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
D549N missense gain of function - predicted PIK3CA D549N lies within the PIK helical domain of the Pik3ca protein (UniProt.org). D549N has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
M1043I missense gain of function PIK3CA M1043I lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1043I confers a gain of function on the Pik3ca protein as indicated by in increased phosphorylation of Akt, activation of downstream signaling, and transformation in cell culture (PMID: 17376864, PMID: 29533785).
P366R missense gain of function - predicted PIK3CA P366R lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). P366R has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
N347K missense unknown PIK3CA N347K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N347K has been identified in sequencing studies (PMID: 25078343), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Aug 2018).
P539S missense unknown PIK3CA P539S lies within the PIK helical domain of the Pik3ca protein (UniProt.org). P539S has been identified in the scientific literature (PMID: 22292935), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
G106R missense gain of function - predicted PIK3CA G106R does not lie within any known functional domains of the Pik3ca proten (UniProt.org). G106R is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased Akt phosphorylation in cell culture (PMID: 21266528) and in one of two cell lines, increased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
R38H missense gain of function - predicted PIK3CA R38H lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). R38H results in moderate increase of Pik3ca kinase activity and Akt phosphorylation, but is not transforming in cell culture (PMID: 15930273), however in another study, R38H increased transformation in two different cell lines, as compared to wild-type Pik3ca (PMID: 29533785).
E542V missense gain of function PIK3CA E542V is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E542V confers a gain of function on Pik3ca, as indicated by increased phosphorylation of Akt and Mek1/2, growth-factor independent cell survival, and is transforming in culture (PMID: 26627007, PMID: 29533785).
H1047L missense gain of function PIK3CA H1047L is a hotspot mutation that lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). H1047L confers a gain of function on the Pik3ca protein as indicated by increased phosphorylation of Akt and Mek1/2, growth factor-independent cell survival, and transformation in cell culture (PMID: 26627007, PMID: 29533785).
N1044Y missense unknown PIK3CA N1044Y lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). N1044Y has not been identified in sequencing studies (PMID: 27191687), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
N345S missense unknown PIK3CA N345S lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345S has been identified in sequencing studies (PMID: 28222664), but has not been biochemically characterized and therefore its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
H1047X missense gain of function PIK3CA H1047X indicates any Pik3ca missense mutation which results in the histidine (H) at amino acid 1047 being replaced by a different amino acid. PIK3CA H1047X mutations are "hotspot" mutations resulting in increased Pik3ca kinase activity and transformation activity in culture (PMID: 15930273).
E110del deletion gain of function - predicted PIK3CA E110del results in the deletion of an amino acid in an unknown region of the Pik3ca protein (UniProt.org). E110del has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
K944N missense gain of function - predicted PIK3CA K944N lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). K944N results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2), and confers resistance to Erbitux (cetuximab) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function. Y
P104L missense gain of function - predicted PIK3CA P104L lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). P104L has not been biochemically characterized, but is predicted to confer a gain of function on the Pik3ca protein as demonstrated by increased transformation ability in two different cell lines (PMID: 29533785).
R425L missense unknown PIK3CA R425L lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). R425L has been identified in the scientific literature (PMID: 28167203), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
E39K missense gain of function - predicted PIK3CA E39K lies within the PI3K-ABD domain of the Pik3ca protein (UniProt.org). E39K is predicted to confer a gain of function to the Pik3ca protein as demonstrated by increased transformation ability in different cell lines (PMID: 29533785, PMID: 29636477).
K567R missense unknown PIK3CA K567R lies within the PIK helical domain of the Pik3ca protein (UniProt.org). K567R has been identified in the scientific literature (PMID: 17314276), but has not been biochemically characterized and therefore, its effect on PIK3CA protein function is unknown (PubMed, Feb 2018).
wild-type none no effect Wild-type PIK3CA indicates that no mutation has been detected within the PIK3CA gene.
N345H missense unknown PIK3CA N345H lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345H has been identified in the scientific literature (PMID: 25846456), but has not been biochemically characterized and therefore its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
R524M missense unknown PIK3CA R524M lies within the PIK helical domain of the Pik3ca protein (UniProt.org). R524M has been identified in sequencing studies (PMID: 21225506, PMID: 16822308), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Mar 2018).
H701R missense unknown PIK3CA H701R does not lie within any known functional domains of the Pik3ca protein (UniProt.org). H701R has not been characterized in the scientific literature and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
L766F missense no effect - predicted PIK3CA L766F does not lie within any known functional domains of the Pik3ca protein (UniProt.org). L766F has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
M1004I missense unknown PIK3CA M1004I lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). M1004I has not been biochemically characterized, but in one of two cell lines, M1004I induced increased cell proliferation and cell viability as compared to wild-type Pik3ca (PMID: 29533785).
N170S missense unknown PIK3CA N170S does not lie within any known functional domains of the Pik3ca protein (UniProt.org). N170S has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
S405F missense unknown PIK3CA S405F lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). S405F has been identified in sequencing studies (PMID: 24695838, PMID: 27738081), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jun 2018).
I273V missense unknown PIK3CA I273V lies within the PI3K-RBD domain of the Pik3ca protein (UniProt.org). I273V has been identified in the scientific literature (PMID: 27126994), but has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
W11L missense no effect - predicted PIK3CA W11L does not lie within any known functional domains of the Pik3ca protein (UniProt.org). W11L has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
E365V missense unknown PIK3CA E365V lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). E365V has not been biochemically characterized, but demonstrates increased transformation ability in one of two different cell lines (PMID: 29533785).
T1025S missense gain of function PIK3CA T1025S lies within the PI3K/PI4K domain in the Pik3ca protein (UniProt.org). T1025S confers a gain of function to the Pik3ca protein as indicated by constitutive activation of downstream signaling and transformation in cultured cells (PMID: 17376864).
G1049C missense unknown PIK3CA G1049C lies within the PI3K/PI4K domain of the Pik3ca protein (UniProt.org). G1049C has been identified in sequencing studies (PMID: 23266353), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
L938* nonsense gain of function - predicted PIK3CA L938* results in a premature truncation of the Pik3ca protein at amino acid 938 of 1068 (UniProt.org). L938* results in activation of Pik3ca signaling as indicated by increased phosphorylation of Akt and Mapk3/Mapk1 (Erk1/2) in culture (PMID: 28424201) and therefore, is predicted to result in a gain of Pik3ca protein function.
E542K missense gain of function PIK3CA E542K is a hotspot mutation that lies within the PIK helical domain of the Pik3ca protein (UniProt.org). E542K results in increased phosphorylation of Akt, growth factor-independent cell survival, and is transforming in cell culture (PMID: 16533766, PMID: 26627007, PMID: 29533785).
G1049D missense unknown PIK3CA G1049D lies within the PI3K/PI4K protein kinase domain of the Pik3ca protein (UniProt.org). G1049D has been identified in sequencing studies (PMID: 24062397, PMID: 26452060), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
E81* nonsense loss of function - predicted PIK3CA E81* results in a premature truncation of the Pik3ca protein at amino acid 81 of 1068 (UniProt.org). Due to the loss of PI3K/PI4K kinase domain (UniProt.org), E81* is predicted to lead to a loss of Pik3ca function.
L113del deletion unknown PIK3CA L113del results in the deletion of one amino acid in the Pik3ca protein at amino acid 113 (UniProt.org). L113del has not been characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
N345D missense unknown PIK3CA N345D lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). N345D has not been characterized and therefore its effect on Pik3ca protein function is unknown (PubMed, Feb 2018).
T544N missense unknown PIK3CA T544N lies within the PIK helical domain of the Pik3ca protein (UniProt.org). T544N has been identified in the scientific literature (PMID: 26276776), but has not been biochemically characterized and therefore, its effect on Pik3ca protein function is unknown (PubMed, Jul 2018).
R382K missense no effect - predicted PIK3CA R382K lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). R382K has not been biochemically characterized, but results in similar cell proliferation and viability levels as wild-type Pik3ca (PMID: 29533785) and therefore, is predicted to have no effect on Pik3ca protein function.
C378R missense gain of function PIK3CA C378R lies within the C2 PI3K-type domain of the Pik3ca protein (UniProt.org). C378R results in constitutive activation of Pi3k and Akt signaling, and decreased apoptosis in cell culture (PMID: 17363507).
Molecular Profile Protein Effect Treatment Approaches
PIK3CA G106V gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R108H gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R108H PTEN mut
PIK3CA N1068Kfs*5 gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E78K unknown
PIK3CA E78K PIK3CA D939G PIK3CA E726K
PIK3CA F550S unknown
PIK3CA R777M unknown
PIK3CA E110K unknown
PIK3CA Q546_E547insQTS unknown
PIK3CA G512* loss of function - predicted
PIK3CA E453Q gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H1048R unknown
PIK3CA R93Q no effect - predicted
PIK3CA positive unknown
PIK3CA G1049A unknown
PIK3CA V344G gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA C420G unknown
PIK3CA P421L unknown
PIK3CA Q643H unknown
PIK3CA G914R unknown
PIK3CA F909L unknown
PIK3CA E218K no effect - predicted
PIK3CA R93W gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA D350G PIK3CA R93W PTEN R130G
PIK3CA G1049S unknown
PIK3CA E469delinsDK gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA K111E gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
KRAS G12V PIK3CA Q546K TP53 R282W
PIK3CA Q546K gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R115* loss of function - predicted
KRAS G13C PIK3CA H1047Y PTEN G143fs PTEN K267fs
PIK3CA H1047Y gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA K179T unknown
PIK3CA E365K PTEN mut
PIK3CA E365K gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA A1046V unknown
PIK3CA E109del unknown
PIK3CA Q60K no effect
PIK3CA V955I gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA amp no effect
PIK3CA G1049R KRAS G12D PIK3CA amp
PIK3CA amp KRAS amp
PIK3CA E545K gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
KRAS G12V PIK3CA E545K TP53 R273*
KRAS G12V PIK3CA E545K TP53 R335fs
BRAF G596R PIK3CA E545K
KRAS Q61H PIK3CA E545K
KRAS G13D PIK3CA E545K
ERBB2 pos PIK3CA E545K
PIK3CA E545K PTEN loss
ERBB2 amp PIK3CA E545K
KRAS mutant PIK3CA E545K
KRAS G13D PIK3CA E545k TP53 S241F
KRAS G13D PIK3CA E545K PIK3CA D549N
KRAS G13D PIK3CA D549N PIK3CA E545K
KRAS G12V PIK3CA E545K TP53 wild-type
AKT1 over exp PIK3CA E545K
KRAS G12D PIK3CA E545K PIK3CA H1047L TP53 wild-type
ERBB2 amp PIK3CA E545K PIK3CA K567R
PIK3CA R108P unknown
PIK3CA E453del unknown
PIK3CA E453del PIK3CA T1025K PIK3CA R88L PTEN mut PTEN loss
PIK3CA C901F gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA N1000D unknown
PIK3CA R992P unknown
PIK3CA D350N gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P447_L455del gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA G451V unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA V356I no effect - predicted
PIK3CA G363A unknown
PIK3CA R38S unknown
PIK3CA K111R unknown
PIK3CA H1047R PIK3CA K111R PTEN wild-type
PIK3CA H1047T unknown
PIK3CA V344M gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E726K gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R617W unknown
PIK3CA V146I unknown
PIK3CA E542Q unknown
PIK3CA G106_R108del PTEN wild-type
PIK3CA G106_R108del gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA Q546P gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E80K unknown
PIK3CA P377R unknown
PIK3CA S773F unknown
PIK3CA E547K loss of function - predicted
PIK3CA E545Q gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA T544I unknown
PIK3CA C378Y unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA D549Y unknown
PIK3CA S553N unknown
PIK3CA Y272* loss of function - predicted
PIK3CA G451R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P124L PTEN del
PIK3CA P124L gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R93P gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
ERBB2 amp PIK3CA K111N
ERBB2 pos PIK3CA K111N
PIK3CA K111N gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA dec exp no effect
PIK3CA E545A gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E545X gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E545X KRAS G12X
PIK3CA K51N no effect - predicted
PIK3CA G364R gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
ERBB2 pos PIK3CA N345T
PIK3CA N345T gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
ERBB2 over exp PIK3CA N345T
PIK3CA E453K gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
KRAS G12D PIK3CA E453K
PIK3CA L339I unknown
PIK3CA N345I gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA A1020V no effect
PIK3CA K966E gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P449_L455del gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA N1068fs gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R38C PTEN loss
PIK3CA R38C PTEN mut
PIK3CA R38C gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R398H no effect - predicted
PIK3CA Y1021N unknown
ERBB2 pos PTEN loss PIK3CA act mut
PIK3CA act mut PTEN wild-type
PIK3CA act mut PTEN dec exp
PIK3CA act mut gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA act mut ERBB2 act mut
ERBB2 pos PIK3CA act mut
PIK3CA M1043T unknown
PIK3CA E109_I112delinsD gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA I910V unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA G1007R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R93L unknown
PIK3CA T1025I unknown
PIK3CA R357Q unknown
PIK3CA P466S unknown
PIK3CA E103_G106delinsD gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA M1040V no effect - predicted
PIK3CA S405Y unknown
PIK3CA E116K no effect
PIK3CA M1043V gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA Q75K unknown
PIK3CA P298S unknown
PIK3CA Q546H unknown
PIK3CA D520V unknown
PIK3CA R108C unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs
PIK3CA P539R gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P539R PIK3CA H1047R
PIK3CA N1044K gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA S332_L334del loss of function - predicted
PIK3CA F1039L unknown
PIK3CA H1065L unknown
PIK3CA E453A gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA I112N unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R108L no effect - predicted
PIK3CA T324I unknown
PIK3CA Q546E gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H47R unknown
PIK3CA P449T gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
BRAF V600E PIK3CA P449T
BRAF V600E PIK3CA P449T TP53 R273H
PIK3CA R115L gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R88Q PTEN mut
BRAF wild-type KRAS wild-type PIK3CA R88Q
PIK3CA R88Q gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R88Q PTEN mut KRAS G12V
PIK3CA Y1021H unknown
PIK3CA E545V unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA D1029H unknown
PIK3CA F614I no effect - predicted
PIK3CA Y1021F unknown
PIK3CA R38G unknown
PIK3CA F930S gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA I406V unknown
PIK3CA E542A gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E978K unknown
PIK3CA D1056G unknown
PIK3CA V955G gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA D1045V unknown
PIK3CA D926N unknown
PIK3CA P487Q unknown
PIK3CA D1029Y PTEN loss
PIK3CA D1029Y PTEN inact mut
PIK3CA D1029Y gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E149G no effect - predicted
PIK3CA V105_R108del gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H450_P458del gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E522A unknown
PIK3CA mut + KRAS mut + PTEN del
ERBB2 pos PIK3CA mut
PIK3CA mutant ERBB2 pos
PIK3CA mutant KRAS Q61X
BRAF wild-type KRAS wild-type PIK3CA mutant
BRAF V600E PIK3CA mut
ERBB2 amp PIK3CA mut
PIK3CA mut BRAF V600E
FGFR1 over exp PIK3CA mut
PIK3CA mutant CDKN2A mutant
KRAS mut PIK3CA mut
PIK3CA mutant PTEN loss
APC mut BRAF mut PIK3CA mut SMAD4 mut TP53 mut
PIK3CA mutant KRAS G12X KRAS G13X
PIK3CA mutant unknown
PIK3CA mut BRAF mut
ERBB2 over exp PIK3CA mut
FGFR1 amp PIK3CA mutant
PIK3CA E545D gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA G12D unknown
PIK3CA Y1021C unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA V344A unknown
PIK3CA E81K unknown
PIK3CA N457K unknown
PIK3CA C407F unknown
PIK3CA R818C no effect - predicted
PIK3CA P449_N457del gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA A1035V unknown
PIK3CA C407W unknown
PIK3CA H701P no effect
PIK3CA V952A gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA T1025K unknown
PIK3CA D300Y unknown
PIK3CA R88L unknown
PIK3CA A1046E unknown
PIK3CA S900I unknown
PIK3CA Y56H unknown
PIK3CA H1047P unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E1037K gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E418K unknown
BRAF V600E PIK3CA H1047K
PIK3CA H1047K unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA C24Y no effect - predicted
PIK3CA D350G gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA A1046T unknown
PIK3CA R401Q unknown
PIK3CA L866F unknown
ERBB2 amp PIK3CA N345K
PIK3CA N345K gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA S629C gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA M1043L gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA I31M no effect
KRAS G12D PIK3CA Q546R
KRAS Q61H PIK3CA Q546R
PIK3CA Q546R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E103_P104del gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R770Q unknown
PIK3CA R916C unknown
PIK3CA D549H unknown
PIK3CA E453G unknown
PIK3CA R108del unknown
PIK3CA I910M unknown
PIK3CA L456Afs*13 unknown
PIK3CA Y165H unknown
PIK3CA D1045N unknown
PIK3CA M1040I unknown
KRAS G12D PIK3CA G1049R
PIK3CA G1049R gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R975S no effect - predicted
PIK3CA E542G gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R1023Q unknown
PIK3CA P471L gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P449L unknown
PIK3CA A1046_H1047insTSA unknown
PIK3CA C971R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA C604R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA D538Y no effect - predicted
EGFR L858R EGFR T790M PIK3CA G118D
PIK3CA G118D gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA C901Y unknown
PIK3CA D454Y unknown
PIK3CA I20M unknown
PIK3CA W552G unknown
KRAS G13D PIK3CA H1047R TP53 wild-type
KRAS G12C PIK3CA H1047R TP53 R248W
KRAS G13D PIK3CA H1047R
PIK3CA H1047R PTEN E307K
KRAS mutant PIK3CA H1047R
BRAF V600X PIK3CA H1047R PTEN Y86fs
KRAS G12F PIK3CA H1047R
KRAS G12D PIK3CA H1047R TP53 wild-type
PIK3CA H1047R gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H1047R PTEN loss
KRAS G12D PIK3CA H1047R PTEN R130G
ERBB2 over exp PIK3CA H1047R SRC over exp
BRAF V600E PIK3CA H1047R
AKT1 over exp PIK3CA H1047R
ERBB2 pos PIK3CA H1047R
ERBB2 amp PIK3CA H1047R
KRAS G12D PIK3CA H1047R TP53 R248W
ERBB2 over exp PIK3CA H1047R
BRAF V600E PIK3CA H1047R TP53 wild-type
KRAS wild-type PIK3CA H1047R
PIK3CA H1047R TP53 S90fs
PIK3CA H665Q unknown
PIK3CA N1044S unknown
PIK3CA N345Y unknown
PIK3CA E710G no effect - predicted
PIK3CA D939G gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H1048L unknown
PIK3CA R1023L unknown
PIK3CA T1025A gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA over exp no effect
PIK3CA E545G gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
ERBB2 amp PIK3CA C420R
ERBB2 pos PIK3CA C420R
PIK3CA C420R gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA K111del gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA T1025N gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA C407Y unknown
ERBB2 pos PIK3CA I391M
PIK3CA I391M unknown
PIK3CA N1044D unknown
KRAS G12D PIK3CA Q546L
PIK3CA Q546L gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H1047Q unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA I889M unknown
PIK3CA Q75E unknown
PIK3CA D549N gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA M1043I gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P366R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA N347K unknown
PIK3CA P539S unknown
PIK3CA G106R gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R38H gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E542V gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
ERBB2 over exp PIK3CA H1047L
PIK3CA H1047L gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
ERBB2 pos PIK3CA H1047L
PIK3CA N1044Y unknown
PIK3CA N345S unknown
PIK3CA H1047X gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA H1047X BRAF V600X
PIK3CA H1047X KRAS G12X
PIK3CA E110del gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA K944N gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA P104L gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA R425L unknown
ERBB2 A775_G776insYVMA PIK3CA R425L
PIK3CA E39K gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
KRAS G12V PIK3CA wild-type
BRAF mut PIK3CA wild-type
BRAF V600E/K PIK3CA wild-type
PIK3CA wild-type no effect
NRAS mut PIK3CA wild-type
PIK3CA wild-type PTEN Y27fs
PIK3CA wild-type PTEN loss
KRAS mutant PIK3CA wild-type
ERBB2 pos PIK3CA wild-type
BRAF wild-type KRAS wild-type NRAS wild-type PIK3CA wild-type
ERBB2 amp PIK3CA wild-type
PIK3CA wild-type PTEN R55fs
PIK3CA wild-type PTEN inact mut
MP BRAF KRAS NRAS PIK3CA
PIK3CA N345H unknown
PIK3CA R524M unknown
PIK3CA H701R unknown
PIK3CA L766F no effect - predicted
PIK3CA M1004I unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA N170S unknown
PIK3CA S405F unknown
PIK3CA I273V unknown
PIK3CA W11L no effect - predicted
PIK3CA E365V unknown Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA T1025S gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA G1049C unknown
PIK3CA L938* gain of function - predicted Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
PIK3CA E542K gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
EGFR over exp PIK3CA E542K
PIK3CA E542K PTEN loss
KRAS Q61L PIK3CA E542K
KRAS Q61H PIK3CA E542K
KRAS Q61L PIK3CA E542K TP53 T118Qfs*5
PIK3CA G1049D unknown
PIK3CA E81* loss of function - predicted
PIK3CA L113del unknown
PIK3CA N345D unknown
PIK3CA T544N unknown
PIK3CA R382K no effect - predicted
PIK3CA C378R gain of function Akt Inhibitor (Pan) Akt1 Inhibitor Akt2 Inhibitor mTOR Inhibitor mTORC1 Inhibitor mTORC2 Inhibitor PI3K Inhibitor (Pan) PIK3CA inhibitor
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA R108H PTEN mut endometrial cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA R108H and PTEN mutations in culture (PMID: 22662154). 22662154
PIK3CA E78K PIK3CA D939G PIK3CA E726K estrogen-receptor positive breast cancer no benefit Letrozole + BYL719 Phase Ib/II Actionable In a Phase Ib trial, an estrogen-receptor positive breast cancer patient harboring PIK3CA mutations, E78K, D939G, and E726K, demonstrated progressive disease when treated with a combination of Femara (letrozole) and Alpelisib (BYL719) (PMID: 27126994). 27126994
PIK3CA V344G glioblastoma multiforme no benefit YM-024 Preclinical Actionable In a preclinical study, YM-024 did not inhibit proliferation of glioblastoma cell lines harboring PIK3CA V344G in culture (PMID: 24718026). 24718026
PIK3CA D350G PIK3CA R93W PTEN R130G endometrial cancer sensitive ARQ092 Preclinical - Pdx Actionable In a preclinical study, a patient-derived xenograft (PDX) model of endometrial cancer harboring PIK3CA D350G, PIK3CA R93W, and PTEN R130G was sensitive to ARQ092, demonstrating greater than 90% inhibition of tumor growth (PMID: 26469692). 26469692
KRAS G12V PIK3CA Q546K TP53 R282W colorectal cancer predicted - sensitive Selumetinib Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) inhibited tumor growth of patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA Q546K, and TP53 R282W (PMID: 26272063). 26272063
KRAS G12V PIK3CA Q546K TP53 R282W colorectal cancer decreased response BEZ235 Preclinical - Pdx Actionable In a preclinical study, BEZ235 delayed tumor growth of patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA Q546K, and TP53 R282W (PMID: 26272063). 26272063
KRAS G12V PIK3CA Q546K TP53 R282W colorectal cancer sensitive Selumetinib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) and BEZ235 combination treatment resulted in enhanced tumor growth stabilization compared to single agent in patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA Q546K and TP53 R282W (PMID: 26272063). 26272063
PIK3CA Q546K Advanced Solid Tumor sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
PIK3CA Q546K breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). 26627007
KRAS G13C PIK3CA H1047Y PTEN G143fs PTEN K267fs ovarian clear cell adenocarcinoma sensitive DS-7423 Preclinical - Cell line xenograft Actionable In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring KRAS G13C, PIK3CA H1047Y, PTEN G143fs, and PTEN K267fs was sensitive to treatment with DS-7423, demonstrating inhibition of cell proliferation in culture and tumor growth inhibition in xenograft models (PMID: 24504419). 24504419
PIK3CA H1047Y endometrial cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth in a human endometrial cancer cell line harboring a PIK3CA H1047Y mutation, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
PIK3CA H1047Y glioblastoma multiforme sensitive YM-024 Preclinical Actionable In a preclinical study, glioblastoma cell lines harboring PIK3CA H1047Y demonstrated increased sensitivity to YM-204 induced growth inhibition (PMID: 24718026). 24718026
PIK3CA E365K PTEN mut endometrial cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA E365K and PTEN mutations in culture (PMID: 22662154). 22662154
PIK3CA E365K PTEN mut endocervical carcinoma sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA E365K and PTEN mutations in culture (PMID: 22662154). 22662154
PIK3CA V955I colorectal cancer resistant Fluorouracil + Cetuximab Clinical Study Actionable In a clinical study, PIK3CA V955I was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in colorectal cancer patients, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA V955I (PMID: 28424201). 28424201
PIK3CA amp triple-receptor negative breast cancer sensitive NVP-AEW541 + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, NVP-AEW541 enhanced sensitivity of PIK3CA amplified triple-receptor negative breast cancer cells to Pictilisib (GDC-0941) in culture (PMID: 27196766). 27196766
PIK3CA amp urinary bladder cancer sensitive Gemcitabine + Pictilisib Preclinical - Pdx Actionable In a preclinical study, Pictilisib (GDC-0941) and Gemzar (gemcitabine) combination treatment resulted in inhibition of Akt phosphorylation and improved tumor growth inhibition and survival compared to single agent therapy in patient-derived xenograft (PDX) models of PIK3CA amplified bladder cancer (PMID: 28808038). 28808038
PIK3CA amp ovarian cancer sensitive Panulisib Preclinical Actionable In a preclinical study, Panulisib (P7170) downregulated mTOR pathway signaling in ovarian cancer cells with amplified PIK3CA (PMID: 25700704). 25700704
PIK3CA amp ovarian cancer sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited PI3K signaling and proliferation of a PIK3CA amplified human ovarian cancer cell line in culture, and inhibited tumor growth in xenograft models (PMID: 25637314). 25637314
PIK3CA amp nasopharynx carcinoma sensitive MK2206 Phase II Actionable In a Phase II study, MK2206 increased stable disease to 12 months in a nasopharyngeal carcinoma patient with Pik3ca amplification (PMID: 26084990). 26084990
PIK3CA amp head and neck squamous cell carcinoma predicted - sensitive AZD8055 Preclinical - Cell culture Actionable In a preclinical study, treatment with AZD8055 resulted in antiproliferative activity in head and neck squamous cell carcinoma cells harboring PIK3CA amplification in culture (PMID: 28446642). 28446642
PIK3CA amp head and neck squamous cell carcinoma sensitive Radiotherapy + Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, Taselisib (GDC-0032) enhanced the effects of radiation induced apoptosis in HNSCC cell lines and cell line xenograft models with PIK3CA amplification (PMID: 26589432). 26589432
PIK3CA amp triple-receptor negative breast cancer sensitive Linsitinib + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Linsitinib (OSI-906) enhanced sensitivity of PIK3CA amplified triple-receptor negative breast cancer cells to Pictilisib (GDC-0941) in culture (PMID: 27196766). 27196766
PIK3CA amp head and neck squamous cell carcinoma sensitive BEZ235 Preclinical - Cell culture Actionable In a preclinical study, BEZ235 resulted in antiproliferative activity in head and neck squamous cell carcinoma cells harboring PIK3CA amplification in culture (PMID: 28446642). 28446642
PIK3CA amp ovarian cancer sensitive SAR245409 Preclinical - Cell line xenograft Actionable In a preclinical study, an ovarian cancer cell line harboring PIK3CA E545K was sensitive to XL765 (SAR245409), demonstrating inhibition of cell proliferation in culture, and inhibition of tumor growth in cell line xenograft models (PMID: 24634413). 24634413
PIK3CA G1049R KRAS G12D PIK3CA amp endometrial cancer sensitive BEZ235 + PD98509 Preclinical Actionable In a preclinical study, the combination of BEZ235 and the MEK1 inhibitor PD98509 worked synergistically or additively to inhibit growth of endometrial cancer cells harboring PIK3CA G1049R, KRAS G12D, and amplification of PIK3CA in culture (PMID: 22662154). 22662154
PIK3CA amp KRAS amp endometrial cancer sensitive BEZ235 + PD98509 Preclinical Actionable In a preclinical study, the combination of BEZ235 and the MEK1 inhibitor PD98509 worked synergistically or additively to inhibit growth of endometrial cancer cells with amplification of PIK3CA and KRAS in culture (PMID: 22662154). 22662154
PIK3CA E545K colon cancer sensitive LY2780301 Phase I Actionable In a Phase I trial, a colon cancer patient harboring PIK3CA E545K was sensitive to LY2780301, demonstrating stable disease for approximately 125 days (PMID: 25902900). 25902900
PIK3CA E545K breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA E545K was sensitive to ARQ 751 in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
PIK3CA E545K Advanced Solid Tumor resistant A66 Preclinical Actionable In a preclinical study, cancer cell lines harboring PIK3CA E545K did not demonstrate sensitivity to A66 in culture, in contrast with cells harboring PIK3CA H1047R (PMID: 21668414). 21668414
PIK3CA E545K breast cancer sensitive PKI-402 Preclinical - Cell line xenograft Actionable In a preclinical study, treatment with PKI-402 resulted in decreased Akt phosphorylation and tumor regression in ERBB2 (HER2)-positive breast cancer cell line xenograft models harboring PIK3CA E545K (PMID: 20371716). 20371716
PIK3CA E545K esophagus squamous cell carcinoma sensitive LY294002 Preclinical Actionable In a preclinical study, LY294002 inhibited cell proliferation of esophagus squamous cell carcinoma cells expressing PIK3CA E545K (PMID: 18262558). 18262558
PIK3CA E545K breast cancer sensitive Everolimus Preclinical Actionable In a preclinical study, breast cancer cell lines harboring a PIK3CA E545K mutation had increased sensitivity to Afinitor (everolimus) in culture (PMID: 20664172). 20664172
PIK3CA E545K Advanced Solid Tumor sensitive rigosertib Preclinical - Cell culture Actionable In a preclinical study, Estybon (rigosertib) inhibited oncogenic transformation in fibroblast cells over-expressing PIK3CA E545K in culture (PMID: 27104980). 27104980
PIK3CA E545K breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells expressing PIK3CA E545K (PMID: 21558396). 21558396
PIK3CA E545K urinary bladder cancer sensitive Gemcitabine + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) and Gemzar (gemcitabine) synergistically inhibited Akt phosphorylation and growth of bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). 28808038
PIK3CA E545K estrogen-receptor positive breast cancer sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA E545K in culture and suppressed tumor growth in xenograft models (PMID: 26839307). 26839307
PIK3CA E545K colorectal cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 decreased cell proliferation in colorectal cancer cells harboring a PIK3CA E545K mutation in cell culture (PMID: 21966435). 21966435
PIK3CA E545K lung squamous cell carcinoma sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). 26013318
PIK3CA E545K breast cancer sensitive Gedatolisib Preclinical Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human breast cancer cells harboring PIK3CA E545K in culture (PMID: 21325073, PMID: 17314276). 17314276 21325073
PIK3CA E545K Advanced Solid Tumor sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K lung squamous cell carcinoma sensitive BEZ235 Preclinical - Cell culture Actionable In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). 26013318
PIK3CA E545K Advanced Solid Tumor sensitive Alpelisib Preclinical - Pdx Actionable In a preclinical study, Alpelisib (BYL719) inhibited PIK3CA E545K and showed anti-tumor activity in patient-derived xenograft models harboring a PIK3CA E545K mutation (PMID: 24608574). 24608574
PIK3CA E545K breast cancer sensitive WYE-125132 Preclinical Actionable In a preclinical study, WYE-125132 inhibited proliferation of breast cancer cells with a PIK3CA E545K mutation (PMID: 20068177). 20068177
PIK3CA E545K breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K non-small cell lung carcinoma sensitive Copanlisib + Paclitaxel Preclinical - Pdx Actionable In a preclinical study, Aliqopa (copanlisib), in combination with Taxol (paclitaxel), induced tumor regression in PIK3CA E545K-mutant patient-derived non-small cell lung cancer xenografts (PMID: 24170767). 24170767
PIK3CA E545K Advanced Solid Tumor sensitive GDC-0980 Phase I Actionable In a Phase I trial, Apitolisib (GDC-0980) resulted in a partial response in two patients, one with head and neck squamous cell carcinoma and another with ovarian cancer, both harboring PIK3CA E545K (PMID: 26787751). 26787751
PIK3CA E545K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K urinary bladder cancer sensitive Pictilisib + Sorafenib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) and Nexavar (sorafenib) synergistically decreased Erk and Akt phosphorylation, inhibited survival of bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). 28808038
PIK3CA E545K breast cancer sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K urinary bladder cancer sensitive Cisplatin + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) and Platinol (cisplatin) synergistically inhibited Akt phosphorylation and growth of bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). 28808038
PIK3CA E545K breast cancer sensitive ARQ092 Preclinical - Cell culture Actionable In a preclinical study, treatment with ARQ092 resulted in growth inhibition in hormone receptor positive breast cancer cells harboring PIK3CA E545K in culture (PMID: 26469692). 26469692
PIK3CA E545K breast cancer sensitive BAY1125976 Preclinical - Cell line xenograft Actionable In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K in culture, and inhibited AKT signaling and tumor growth in xenograft models (PMID: 27699769). 27699769
PIK3CA E545K gastrointestinal system cancer sensitive Capivasertib Preclinical Actionable In a preclinical study, gastric cancer cells harboring PI3KCA E545K mutations were sensitive to the AKT inhibitor AZD5363 (PMID: 24088382). 24088382
PIK3CA E545K hilar cholangiocellular carcinoma unknown Sirolimus Phase 0 Actionable In a pilot clinical trial, Rapamune (sirolumus) demonstrated modest clinical activity in patients with PIK3CA-mutant gastric cancer (n=3) or hilar cholangiocarcinoma (n=1; harboring PIK3CA E545K), with a 0% response rate, median progression-free survival of 1.9 months, and median overall survival of 3.6 months (PMID: 28685070). 28685070
PIK3CA E545K Advanced Solid Tumor sensitive Sirolimus Preclinical Actionable In a preclinical study, Rapamune (sirolimus) demonstrated efficacy in inhibiting transformation of cultured cells containing PIK3CA E545K mutations (PMID: 15647370). 15647370
PIK3CA E545K breast cancer sensitive SAR245409 Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA E545K was sensitive to XL765 (SAR245409), demonstrating inhibition of cell proliferation and colony formation in culture, and inhibition of tumor growth in cell line xenograft models (PMID: 24634413). 24634413
PIK3CA E545K colorectal cancer resistant Fluorouracil + Cetuximab Preclinical - Cell culture Actionable In a preclinical study, colorectal cancer cells over expressing PIK3CA E545K were resistant to Erbitux (cetuximab) and Fluorouracil combination treatment in culture (PMID: 28424201). 28424201
PIK3CA E545K breast carcinoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited PI3K signaling and proliferation of a human breast carcinoma cell line harboring PIK3CA E545K in culture and inhibited tumor growth in xenograft models (PMID: 25637314). 25637314
PIK3CA E545K breast cancer no benefit BEZ235 + Venetoclax Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize breast cancer cell lines harboring PIK3CA E545K to Venclexta (venetoclax) in culture (PMID: 27974663). 27974663
PIK3CA E545K head and neck squamous cell carcinoma sensitive rigosertib Preclinical - Pdx Actionable In a preclinical study, head and neck squamous cell carcinoma patient-derived xenograft models harboring a PIK3CA E545K mutation demonstrated increased sensitivity to Estybon (rigosertib) (PMID: 23873848). 23873848
PIK3CA E545K thyroid cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, expression of PIK3CA E545K in a thyroid cancer cell line resulted in increased sensitivity to MK2206 in culture (PMID: 21289267). 21289267
PIK3CA E545K breast cancer predicted - sensitive BEZ235 + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA E545K to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA E545K breast cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K breast cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). 26627007
PIK3CA E545K head and neck squamous cell carcinoma predicted - sensitive Carboplatin + Paclitaxel + Temsirolimus Phase II Actionable In a Phase II trial, a patient with head and neck squamous cell carcinoma harboring PIK3CA E545K demonstrated a partial response when treated with the combination of Torisel (temsirolimus), Paraplatin (carboplatin), and Taxol (paclitaxel) (PMID: 28961834). 28961834
PIK3CA E545K breast cancer sensitive DHM25 Preclinical - Cell culture Actionable In a preclinical study, DHM25 increased cell death in a breast cancer cell line harboring PIK3CA E545K in culture (PMID: 26237138). 26237138
PIK3CA E545K colorectal cancer sensitive Cetuximab + Irinotecan Clinical Study Actionable In a retrospective study, treatment with the combination of Erbitux (cetuximab) and Camptosar (irinotecan) resulted in stable disease in 50% (1/2) and 14 months without evidence of disease in 50% (1/2) of colorectal carcinoma patients harboring a PIK3CA E545K mutation (PMID: 25714871). 25714871
PIK3CA E545K cervical cancer sensitive PW12 Preclinical Actionable In a preclinical study, PW12 inhibited proliferation of cervical cancer cells with a PIK3CA E545K mutation (PMID: 22391131). 22391131
PIK3CA E545K leukemia sensitive LY3023414 Preclinical Actionable In a preclinical study, LY3023414 inhibited tumor growth in a transgenic animal model of leukemia driven by PIK3CA E545K (PMID: 27439478). 27439478
PIK3CA E545K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E545K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
PIK3CA E545K urinary bladder cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) inhibited Akt phosphorylation, resulted in growth inhibition in bladder cancer cells harboring PIK3CA E545K in culture (PMID: 28808038). 28808038
PIK3CA E545K lung squamous cell carcinoma sensitive Buparlisib Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). 26013318
PIK3CA E545K ovarian cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of ovarian cancer cells harboring PIK3CA E545K in culture (PMID: 21558396). 21558396
KRAS G12V PIK3CA E545K TP53 R273* colorectal cancer resistant BEZ235 Preclinical - Pdx Actionable In a preclinical study, patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA E545K, and TP53 R273* did not respond to BEZ235 treatment (PMID: 26272063). 26272063
KRAS G12V PIK3CA E545K TP53 R273* colorectal cancer no benefit Selumetinib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) and BEZ235 combination treatment did not improve tumor growth stabilization compared to single agent in patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA E545K and TP53 R273* (PMID: 26272063). 26272063
KRAS G12V PIK3CA E545K TP53 R273* colorectal cancer resistant Selumetinib Preclinical - Pdx Actionable In a preclinical study, patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA E545K, and TP53 R273* did not respond to Selumetinib (AZD6244) treatment (PMID: 26272063). 26272063
KRAS G12V PIK3CA E545K TP53 R335fs colorectal cancer no benefit MLN0128 + PD-0325901 Preclinical - Pdx Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 combination treatment did not result in tumor growth stabilization in patient-derived xenograft models of colorectal cancer harboring KRAS G12V, PIK3CA E545K, and TP53 R335fs (PMID: 26272063). 26272063
BRAF G596R PIK3CA E545K colorectal cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of colorectal cancer cells harboring both BRAF G596R and PIK3CA E545K in culture (PMID: 26243863). 26243863
KRAS Q61H PIK3CA E545K non-small cell lung carcinoma decreased response Pimasertib Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells harboring KRAS Q61H and PIK3CA E545K demonstrated decreased response to Pimasertib (MSC1936369B) in culture (PMID: 23629727). 23629727
KRAS Q61H PIK3CA E545K non-small cell lung carcinoma sensitive Pimasertib + Sorafenib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Nexavar (sorafenib) synergistically inhibited proliferation of non-small cell lung cancer cells harboring KRAS Q61H and PIK3CA E545K in culture (PMID: 23629727). 23629727
KRAS Q61H PIK3CA E545K non-small cell lung carcinoma sensitive Pimasertib + Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Stivarga (regorafenib) synergistically inhibited proliferation of non-small cell lung cancer cells harboring KRAS Q61H and PIK3CA E545K in culture (PMID: 23629727). 23629727
KRAS Q61H PIK3CA E545K non-small cell lung carcinoma sensitive Everolimus + Pimasertib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Afinitor (everolimus) synergistically inhibited proliferation of non-small cell lung cancer cells harboring KRAS Q61H and PIK3CA E545K in culture (PMID: 23629727). 23629727
KRAS G13D PIK3CA E545K colorectal adenocarcinoma sensitive Cobimetinib + Pictilisib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Pictilisib (GDC-0941) and Cobimetinib (GDC-0973) inhibited tumor growth in a colorectal adenocarcinoma xenograft model harboring KRAS G13D and PIK3CA E545K mutations, and demonstrated improved efficacy over either agent alone (PMID: 22084396). 22084396
KRAS G13D PIK3CA E545K endometrial cancer resistant Everolimus Preclinical - Cell line xenograft Actionable In a preclinical study, expression of KRAS G13D in an endometrial cancer cell line harboring PIK3CA E545K conferred resistance to Afinitor (everolimus) in xenograft models (PMID: 20664172). 20664172
ERBB2 pos PIK3CA E545K Her2-receptor positive breast cancer sensitive trastuzumab emtansine Preclinical - Cell line xenograft Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited survival of Herceptin (trastuzumab)-resistant ERBB2 (HER2) positive breast cancer cells harboring PIK3CA E545K in culture, and induced tumor regression in cell line xenograft models (PMID: 26920887). 26920887
PIK3CA E545K PTEN loss stomach cancer unknown Sirolimus Phase 0 Actionable In a pilot clinical trial, Rapamune (sirolumus) demonstrated modest clinical activity in patients with PIK3CA-mutant gastric cancer (n=3) or hilar cholangiocarcinoma (n=1), including 2 gastric cancer patients harboring PIK3CA E545K and PTEN loss, with a 0% response rate, median progression-free survival of 1.9 months, and median overall survival of 3.6 months (PMID: 28685070). 28685070
ERBB2 amp PIK3CA E545K breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model co-harboring ERBB2 (HER2) amplification and PIK3CA E545K demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
ERBB2 amp PIK3CA E545K breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA E545K and ERBB2 (HER2) amplification in culture (PMID: 21558396). 21558396
KRAS mutant PIK3CA E545K colon cancer no benefit Cetuximab Preclinical Actionable In a preclinical study, Erbitux (cetuximab) did not inhibit proliferation of colon cancer cell lines harboring mutant KRAS and PIK3CA E545K in culture (PMID: 26715098). 26715098
KRAS mutant PIK3CA E545K colon cancer sensitive BKM120 + Cetuximab Preclinical Actionable In a preclinical study, Buparlisib (BKM120) worked synergistically with Erbitux (cetuximab) to inhibit proliferation of colon cancer cell lines harboring mutant KRAS and PIK3CA E545K in culture (PMID: 26715098). 26715098
KRAS mutant PIK3CA E545K colon cancer decreased response Buparlisib Preclinical Actionable In a preclinical study, colon cancer cell lines harboring mutant KRAS and PIK3CA E545K demonstrated reduced sensitivity to Buparlisib (BKM120) induced growth inhibition in culture (PMID: 26715098). 26715098
KRAS G13D PIK3CA E545k TP53 S241F colorectal cancer sensitive MLN0128 + PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 synergistically inhibited Erk and PI3K signaling and proliferation, but did not induce apoptosis in colorectal cancer cells harboring KRAS G13D, PIK3CA E545K, and TP53 S241F in culture (PMID: 26272063). 26272063
KRAS G13D PIK3CA E545K PIK3CA D549N colon cancer decreased response Gedatolisib Preclinical Actionable In a preclinical study, human colon cancer cells harboring KRAS G13D, PIK3CA E545K, and PIK3CA D549N had a decreased response to Gedatolisib (PKI-587) in culture (PMID: 21325073, PMID: 24042735). 21325073 24042735
KRAS G13D PIK3CA E545K PIK3CA D549N colorectal cancer resistant Regorafenib Preclinical Actionable In a preclinical study, human colorectal cancer cell lines harboring KRAS G13D, PIK3CA E545K and PIK3CA D549N were resistant to Stivarga (regorafenib) in culture (PMID: 25838391). 25838391
KRAS G13D PIK3CA E545K PIK3CA D549N colorectal cancer sensitive Regorafenib + Cetuximab Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Erbitux (cetuximab) and Stivarga (regorafenib) inhibited growth, reduced Akt and Mapk phosphorylation, and induced apoptosis of human colorectal cancer cell lines harboring KRAS G13D, PIK3CA E545K, and PIK3CA D549N in culture and reduced tumor growth in cell line xenograft models (PMID: 25838391). 25838391
KRAS G13D PIK3CA D549N PIK3CA E545K colorectal cancer sensitive Pimasertib + Sorafenib Preclinical - Cell line xenograft Actionable In a preclinical study, Pimasertib (MSC1936369B) and Nexavar (sorafenib) synergistically inhibited Mapk and Akt signaling, resulted in growth inhibition of colorectal cancer cells harboring KRAS G13D, PIK3CA D549N, and PIK3CA E545K in culture and in cell line xenograft models (PMID: 23629727). 23629727
KRAS G13D PIK3CA D549N PIK3CA E545K colorectal cancer decreased response Pimasertib Preclinical - Cell culture Actionable In a preclinical study, colorectal cancer cells harboring KRAS G13D, PIK3CA D549N and PIK3CA E545K demonstrated decreased response to Pimasertib (MSC1936369B) in culture (PMID: 23629727). 23629727
KRAS G13D PIK3CA D549N PIK3CA E545K colorectal cancer sensitive Pimasertib + BEZ235 Preclinical - Cell line xenograft Actionable In a preclinical study, Pimasertib (MSC1936369B) and BEZ235 combination treatment inhibited tumor growth in colorectal cancer cell line xenograft models harboring KRAS G13D, PIK3CA D549N, and PIK3CA E545K (PMID: 23629727). 23629727
KRAS G13D PIK3CA D549N PIK3CA E545K colorectal cancer sensitive Pimasertib + Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Stivarga (regorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring KRAS G13D, PIK3CA D549N, and PIK3CA E545K in culture (PMID: 23629727). 23629727
KRAS G13D PIK3CA D549N PIK3CA E545K colorectal cancer sensitive Everolimus + Pimasertib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Afinitor (everolimus) synergistically inhibited proliferation of colorectal cancer cells harboring KRAS G13D, PIK3CA D549N, and PIK3CA E545K in culture (PMID: 23629727). 23629727
KRAS G12V PIK3CA E545K TP53 wild-type colorectal cancer decreased response BEZ235 Preclinical - Pdx Actionable In a preclinical study, BEZ235 delayed tumor growth in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12V and PIK3CA E545K (PMID: 26272063). 26272063
KRAS G12V PIK3CA E545K TP53 wild-type colorectal cancer sensitive Selumetinib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) and BEZ235 combination treatment resulted in enhanced tumor growth stabilization compared to single agent in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12V and PIK3CA E545K (PMID: 26272063). 26272063
KRAS G12V PIK3CA E545K TP53 wild-type colorectal cancer decreased response Selumetinib Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) delayed tumor growth in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12V and PIK3CA E545K (PMID: 26272063). 26272063
AKT1 over exp PIK3CA E545K breast cancer resistant Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Akt1 over expression in breast cancer cells harboring PIK3CA E545K resulted in resistance to Pictilisib (GDC-0941) in culture (PMID: 27604488). 27604488
KRAS G12D PIK3CA E545K PIK3CA H1047L TP53 wild-type colorectal cancer sensitive MLN0128 + PD-0325901 Preclinical - Pdx Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 combination treatment resulted in tumor growth stabilization in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12D, PIK3CA E545K and H1047L (PMID: 26272063). 26272063
ERBB2 amp PIK3CA E545K PIK3CA K567R Her2-receptor positive breast cancer sensitive Gedatolisib Preclinical - Cell line xenograft Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited PI3K signaling, cell growth and induced apoptosis in human breast cancer cells harboring ERBB2 (HER2) amplification, PIK3CA E545K, and PIK3CA K567R in culture and in cell line xenografts (PMID: 21325073, PMID: 17314276). 17314276 21325073
PIK3CA E453del PIK3CA T1025K PIK3CA R88L PTEN mut PTEN loss endometrial carcinoma sensitive Copanlisib Phase I Actionable In a Phase I clinical trial, an endometrial carcinoma patient harboring PIK3CA T1052K, R88L, and E453del, as well as a PTEN mutation and loss of PTEN protein expression demonstrated a complete response to treatment with Aliqopa (copanlisib) (PMID: 27672108). 27672108
PIK3CA P447_L455del estrogen-receptor positive breast cancer sensitive Letrozole + BYL719 Clinical Study Actionable In a clinical case study, a patient with estrogen-receptor positive breast cancer harboring PIK3CA P447_L455del demonstrated an 11 month sustained response to the combination therapy of Femara (letrozole) and Alpelisib (BYL719) (PMID: 29284706). 29284706
PIK3CA D549Y urinary bladder cancer decreased response Pictilisib Preclinical - Pdx Actionable In a preclinical study, Pictilisib (GDC-0941) demonstrated limited tumor growth inhibition and survival benefit in patient-derived xenograft (PDX) models of bladder cancer harboring PIK3CA D549Y (PMID: 28808038). 28808038
PIK3CA P124L PTEN del urinary bladder cancer decreased response Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) demonstrated limited inhibition of Akt phosphorylation and growth in bladder cancer cells harboring PIK3CA P124L and PTEN deletion in culture (PMID: 28808038). 28808038
ERBB2 amp PIK3CA K111N breast cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth and Akt phosphorylation, and promoted apoptosis in a human breast cancer cell line harboring PIK3CA K111N and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
ERBB2 pos PIK3CA K111N Her2-receptor positive breast cancer sensitive trastuzumab emtansine Preclinical - Cell line xenograft Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited survival of ERBB2 (HER2) positive breast cancer cells harboring PIK3CA K111N in culture, and induced tumor regression in cell line xenograft models (PMID: 26920887). 26920887
PIK3CA K111N breast cancer sensitive ARQ092 Preclinical - Cell culture Actionable In a preclinical study, hormone receptor positive breast cancer cells harboring PIK3CA K111N were sensitive to ARQ092 in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
PIK3CA K111N estrogen-receptor positive breast cancer sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA K111N in culture and induced tumor regression in xenograft models (PMID: 26839307). 26839307
PIK3CA K111N breast cancer sensitive DHM25 Preclinical - Cell culture Actionable In a preclinical study, DHM25 increased cell death in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 26237138). 26237138
PIK3CA K111N breast cancer sensitive BAY1125976 Preclinical - Cell culture Actionable In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 27699769). 27699769
PIK3CA K111N breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA K111N was sensitive to ARQ 751 in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
PIK3CA E545X KRAS G12X colorectal cancer sensitive Temsirolimus Clinical Study Actionable In a clinical study, two colorectal cancer patients harboring both a PIK3CA E545 and KRAS G12 mutation demonstrated stable disease when treated with Torisel (temsirolimus) (PMID: 21216929). 21216929
ERBB2 over exp PIK3CA N345T stomach cancer predicted - resistant Trastuzumab Clinical Study Actionable In a clinical study (AMNESIA-1), assessment of pre-treatment tumor samples from ERBB2 (HER2)-positive gastric or gastroesophageal cancer patients (defined as HER2 IHC 3+ or HER2 IHC 2+/ISH+) identified PIK3CA mutations in 15% (3/20) of patients demonstrating primary resistance to Herceptin (trastuzumab), including 1 patient harboring PIK3CA N345T (PMID: 29208673). 29208673
PIK3CA E453K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E453K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
KRAS G12D PIK3CA E453K stomach cancer sensitive Capivasertib Preclinical Actionable In a preclinical study, AZD5363 inhibited proliferation of the AGS gastric cancer cell line, which has been reported to harbor KRAS G12D and PIK3CA E453K mutations (PMID: 24088382, PMID: 19755509). 19755509 24088382
PIK3CA N345I breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA N345I demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
PIK3CA K966E colorectal cancer resistant Fluorouracil + Cetuximab Clinical Study Actionable In a clinical study, PIK3CA K966E was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in colorectal cancer patients, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA K966E (PMID: 28424201). 28424201
PIK3CA R38C PTEN loss endometrial cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of an endometrial cancer cell line harboring PIK3CA R38C and PTEN loss in culture (PMID: 21558396). 21558396
PIK3CA R38C PTEN mut endometrial cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 decreased growth of endometrial cancer cells harboring PIK3CA R38C and PTEN mutations in culture and in xenograft models (PMID: 22662154). 22662154
PIK3CA act mut PTEN wild-type breast cancer sensitive Torkinib Preclinical - Cell culture Actionable In a preclinical study, 9/9 breast cancer cell lines harboring a PIK3CA activating mutation and PTEN wild-type demonstrated sensitivity to treatment with Torkinib (PP242) in culture, resulting in decreased cell viability (PMID: 21358673). 21358673
PIK3CA act mut PTEN wild-type breast cancer sensitive Everolimus Preclinical - Cell culture Actionable In a preclinical study, 8/9 breast cancer cell lines harboring a PIK3CA activating mutation and PTEN wild-type demonstrated sensitivity to treatment with Afinitor (everolimus) in culture, resulting in decreased cell viability (PMID: 21358673). 21358673
PIK3CA act mut PTEN dec exp renal cell carcinoma no benefit GDC-0980 Phase II Actionable In a retrospective analysis from a Phase II clinical trial, patients with metastatic renal cell carcinoma treated with Apitolisib (GDC-0980) had no difference in progression free survival when stratified by the presence (n=21) or absence (n=15) of PIK3CA activating mutation or loss of Pten expression (PMID: 26951309). 26951309
PIK3CA act mut PTEN dec exp renal cell carcinoma no benefit Everolimus Phase II Actionable In a retrospective analysis from a Phase II clinical trial, patients with metastatic renal cell carcinoma treated with Afinitor (everolimus) had no difference in progression free survival when stratified by the presence (n=21) or absence (n=17) of PIK3CA activating mutations (PMID: 26951309). 26951309
PIK3CA act mut breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, breast cancer cell lines harboring activating mutations in PIK3CA had increased sensitivity to MK2206 in cell culture (PMID: 22932669). 22932669
PIK3CA act mut breast cancer predicted - sensitive Torin 1 + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, the ATP-competitive mTORC1/2 inhibitor Torin1 sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA act mut estrogen-receptor positive breast cancer predicted - sensitive AZD5363 + Tamoxifen Preclinical - Cell culture Actionable In a preclinical study, the combination of AZD5363 and 4-hydroxytamoxifen (4-OHT) worked synergistically or additively to inhibit growth of several estrogen receptor-positive breast cancer cell lines in culture, including cell lines with PIK3CA activating mutations, and overcame tamoxifen resistance in a resistant cell line (PMID: 26116361). 26116361
PIK3CA act mut lung small cell carcinoma predicted - sensitive Navitoclax + Pictilisib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Navitoclax (ABT-263) and GDC-0941 resulted in increased tumor growth delay and apoptosis in a small cell lung cancer cell line xenograft model harboring a PIK3CA activating mutation compared to either drug alone (PMID: 27197306). 27197306
PIK3CA act mut head and neck squamous cell carcinoma sensitive Gedatolisib Preclinical Actionable In a preclinical study, PF-05212384 decreased viability of head and neck squamous carcinoma cells harboring a PIK3CA activating mutation in cell culture (PMID: 24823695). 24823695
PIK3CA act mut Advanced Solid Tumor sensitive Afuresertib Preclinical Actionable In a preclinical study, various tumor cell lines harboring PI3KCA activating mutations demonstrated increased sensitivity to Afuresertib (GSK2110183) in cultured cells (PMID: 24978597). 24978597
PIK3CA act mut Advanced Solid Tumor sensitive BAY1125976 Preclinical Actionable In a preclinical study, BAY1125976 demonstrated anti-tumor efficacy in multiple xenograft tumor models of different cancers with PIK3CA mutations or PTEN deletions and displayed synergy with other anti-cancer therapies (Cancer Res 2013;73(8 Suppl):Abstract nr 2050). detail...
PIK3CA act mut breast cancer predicted - sensitive Ridaforolimus + MK2206 Phase I Actionable In a Phase I clinical trial, Ridaforolimus in combination with MK-2206 demonstrated clinical activity in breast cancer patients expressing a PI3K pathway dependent gene expression signature, with complete response in 14.3% (2/14), partial response in 12.5% (2/16), and 2 patients achieving stable disease (PMID: 26187616). 26187616
PIK3CA act mut Advanced Solid Tumor sensitive Metformin Preclinical Actionable In a preclinical study, Glucophage (metformin) demonstrated efficacy in treating dietary restriction-resistant human xenograft tumors harboring a PIK3CA-activating mutation (PMID: 23986086). 23986086
PIK3CA act mut breast cancer no benefit Alpelisib + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) did not sensitize breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA act mut non-small cell lung carcinoma sensitive Pictilisib Preclinical - Cell line xenograft Actionable In preclinical studies, the PI3K inhibitor GDC-0941 demonstrated efficacy against NSCLC tumor cell lines in culture and in xenograft models harboring alterations in the PI3K pathway (PMID: 23136191). 23136191
PIK3CA act mut breast cancer predicted - sensitive BEZ235 + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA act mut breast cancer predicted - sensitive Vistusertib + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, the ATP-competitive mTORC1/2 inhibitor Vistusertib (AZD2014) sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA act mut Advanced Solid Tumor sensitive Everolimus Preclinical - Cell line xenograft Actionable In a preclinical study, Afinitor (everolimus) demonstrated efficacy in multiple cancer cell lines in culture and xenograft models with PIK3CA activating mutations (PMID: 20664172). 20664172
PIK3CA act mut breast cancer predicted - sensitive MLN0128 + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, the ATP-competitive mTORC1/2 inhibitor Sapanisertib (MLN0128) sensitized breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA act mut triple-receptor negative breast cancer predicted - sensitive Bevacizumab + Doxorubicin + Everolimus Phase I Actionable In a Phase I trial, triple-receptor negative breast cancer patients, including those with PIK3CA activating mutations, demonstrated an overall response rate of 21% (11/52) and clinical benefit rate of 40% (21/52) when treated with a combination of Avastin (bevacizumab), Adriamycin (doxorubicin), and either Afinitor (everolimus) or Torisel (temsirolimus) (PMID: 27893038). 27893038
PIK3CA act mut breast cancer no benefit BKM120 + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) did not sensitize breast cancer cell lines harboring PIK3CA activating mutations to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA act mut ovarian clear cell adenocarcinoma sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 demonstrated efficacy in mouse xenograft models of ovarian clear cell adenocarcinoma with PIK3CA mutations (PMID: 24927217). 24927217
PIK3CA act mut Advanced Solid Tumor conflicting Taselisib Phase II Actionable In a Phase II (MATCH) trial, Taselisib (GDC-0032) treatment resulted in no objective response (0/65) but prolonged stable disease (estimated 6-month progression-free survival rate 27%) in patients with advanced solid tumors harboring PIK3CA activating mutations (J Clin Oncol 36, 2018 (suppl; abstr 101); NCT02465060). detail...
PIK3CA act mut Advanced Solid Tumor conflicting Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, Taselisib (GDC-0032) effectively suppressed growth of multiple tumor types in cell line xenograft models, with greater selectivity for PIK3CA activating mutants (PMID: 23662903). 23662903
PIK3CA act mut breast cancer no benefit BEZ235 + Venetoclax Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize breast cancer cell lines harboring PIK3CA activating mutations to Venclexta (venetoclax) in culture (PMID: 27974663). 27974663
PIK3CA act mut triple-receptor negative breast cancer predicted - sensitive Bevacizumab + Doxorubicin + Temsirolimus Phase I Actionable In a Phase I trial, triple-receptor negative breast cancer patients, including those with PIK3CA activating mutations, demonstrated an overall response rate of 21% (11/52) and clinical benefit rate of 40% (21/52) when treated with a combination of Avastin (bevacizumab), Adriamycin (doxorubicin), and either Afinitor (everolimus) or Torisel (temsirolimus) (PMID: 27893038). 27893038
PIK3CA act mut breast cancer sensitive Copanlisib Preclinical Actionable In a preclinical study, breast cancer cell lines with a PIK3CA activating mutation and/or ERBB2 (HER2) over expression demonstrated increased sensitivity to inhibition of proliferation by Aliqopa (copanlisib) in culture, compared to ERBB2 (HER2)-negative and wild-type PIK3CA cell lines (PMID: 24170767). 24170767
PIK3CA act mut breast cancer sensitive Copanlisib Phase I Actionable In a Phase I clinical trial, treatment with Aliqopa (copanlisib) resulted in partial response in one and stable disease in another patient with breast cancer harboring activating PIK3CA mutations (PMID: 27672108; NCT00962611). 27672108
PIK3CA act mut head and neck squamous cell carcinoma predicted - sensitive AZD8055 + Cetuximab Preclinical - Pdx Actionable In a preclinical study, two head and neck squamous cell carcinoma patient-derived xenograft (PDX) models harboring a PIK3CA activating mutation demonstrated greater delayed tumor growth when treated with a combination of AZD8055 and Erbitux (cetuximab) compared to either agent alone (PMID: 28446642). 28446642
PIK3CA act mut Advanced Solid Tumor sensitive GSK1059615 Preclinical Actionable In a preclinical study, solid tumor cell lines harboring PIK3CA activating mutations demonstrated increased sensitivity to GSK1059615 in culture (Clin Cancer Res October 1, 2008 14; B37). detail...
PIK3CA act mut Advanced Solid Tumor sensitive Ipatasertib + Paclitaxel Phase Ib/II Actionable In a Phase Ib trial, Ipatasertib (GDC-0068) in combination with Abraxane (paclitaxel) demonstrated safety and anti-tumor activity in patients with advanced solid tumors, including patients with PIK3CA activating mutations (Annals of Oncology (2014) 25 (suppl_4): iv146-iv164. 10.1093/annonc/mdu331). detail...
PIK3CA act mut ERBB2 act mut breast cancer sensitive VS-5584 Preclinical Actionable In a preclinical study, breast cancer cells with mutations in both ERBB2 (HER2) and PIK3CA were more sensitive to VS-5584 (PMID: 23270925). 23270925
ERBB2 pos PIK3CA act mut Her2-receptor positive breast cancer predicted - sensitive BKM120 + Trastuzumab Phase I Actionable In a Phase I trial, the combination of Buparlisib (BKM120) and Herceptin (trastuzumab) was well tolerated and resulted in some preliminary efficacy in patients with ERBB2 (HER2)-positive breast cancer harboring PIK3CA activating mutations and/or PTEN mutations that had progressed on trastuzumab-based therapy (PMID: 24470511). 24470511
ERBB2 pos PIK3CA act mut uterine cancer sensitive Taselisib Preclinical Actionable In a preclinical study, Taselisib (GDC-0032) inhibited growth of HER2 positive uterine cancer cell lines with PIK3CA mutations (PMID: 25172762). 25172762
ERBB2 pos PIK3CA act mut Her2-receptor positive breast cancer sensitive Palbociclib + Pictilisib Preclinical Actionable In a preclinical study, Ibrance (palbociclib) and Pictilisib (GDC-0941) worked synergistically to inhibit survival of ERBB2 (HER2)-positive breast cancer cell lines harboring PIK3CA mutations in culture (PMID: 27020857). 27020857
ERBB2 pos PIK3CA act mut Her2-receptor positive breast cancer decreased response Trastuzumab Clinical Study Actionable In a retrospective analysis, ERBB2 (HER2)-positive breast cancer patients with PI3K pathway activation due to PTEN loss and/or PIK3CA activating mutation demonstrated a decreased median progression-free survival of 4.5 months, compared to 9.0 months for patients without PI3K pathway activation following treatment with a Herceptin (trastuzumab) containing regimen (PMID: 21676217). 21676217
ERBB2 pos PIK3CA act mut Her2-receptor positive breast cancer decreased response Trastuzumab Clinical Study Actionable In a clinical study, ERBB2 (HER2)-positive breast cancer patients with PI3K pathway activation resulting from low PTEN expression and/or PIK3CA activating mutations demonstrated decreased progression-free survival following treatment with Herceptin (trastuzumab) compared to patients without PI3K pathway activation (PMID: 17936563). 17936563
PIK3CA M1043V Advanced Solid Tumor sensitive Sirolimus Preclinical Actionable In a preclinical study, Rapamune (sirolimus) inhibited proliferation in cultured cells expressing PIK3CA M1043V (PMID: 17376864). 17376864
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs endometrial cancer sensitive BGJ398 + BKM120 Preclinical - Cell culture Actionable In a preclinical study, the combination of BGJ398 and Buparlisib (BKM120) resulted in a synergistic effect, demonstrating inhibition of cell proliferation, decreased colony formation, and cell death in an endometrial cancer cell line harboring FGFR2 N550K, PIK3CA I20M and P539R, and PTEN R130Q and T321fs*23 in culture (PMID: 28119489). 28119489
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs endometrial cancer sensitive Alpelisib + BGJ398 Preclinical - Cell culture Actionable In a preclinical study, the combination of BGJ398 and Alpelisib (BYL719) resulted in a synergistic effect, demonstrating inhibition of cell proliferation and induced cell death in an endometrial cancer cell line harboring FGFR2 N550K, PIK3CA I20M and P539R, and PTEN R130Q and T321fs*23 in culture (PMID: 28119489). 28119489
FGFR2 N550K PIK3CA I20M PIK3CA P539R PTEN R130Q PTEN T321fs endometrial cancer sensitive BGJ398 + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, the combination of BGJ398 and Pictilisib (GDC-0941) resulted in a synergistic effect, demonstrating inhibition of cell proliferation, decreased colony formation, and cell death in an endometrial cancer cell line harboring FGFR2 N550K, PIK3CA I20M and P539R, and PTEN R130Q and T321fs*23 in culture (PMID: 28119489). 28119489
PIK3CA P539R breast cancer sensitive BAY1125976 Preclinical - Cell culture Actionable In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA P539R in culture (PMID: 27699769). 27699769
PIK3CA P539R PIK3CA H1047R breast cancer sensitive PF-04691502 Preclinical - Cell culture Actionable In a preclinical study, PF-04691502 inhibited Akt phosphorylation and proliferation of breast cancer cells harboring both PIK3CA P539R and H1047R in culture (PMID: 21750219). 21750219
PIK3CA P539R PIK3CA H1047R breast cancer sensitive ARQ092 Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells harboring PIK3CA P539R and H1047R were sensitive to ARQ092 in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
PIK3CA P539R PIK3CA H1047R breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA P539R and PH1047R was sensitive to ARQ 751 in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
BRAF V600E PIK3CA P449T colorectal cancer sensitive Pimasertib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). 23629727
BRAF V600E PIK3CA P449T colorectal cancer sensitive Pimasertib + Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Stivarga (regorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). 23629727
BRAF V600E PIK3CA P449T colorectal cancer resistant Cetuximab Preclinical Actionable In a preclinical study, human colorectal cancer cells harboring BRAF V600E and PIK3CA P449T were resistant to Erbitux (cetuximab) in culture (PMID: 25838391). 25838391
BRAF V600E PIK3CA P449T colorectal cancer sensitive Everolimus + Pimasertib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Afinitor (everolimus) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). 23629727
BRAF V600E PIK3CA P449T colorectal cancer sensitive Regorafenib + Cetuximab Preclinical Actionable In a preclinical study, the combination of Erbitux (cetuximab) and Stivarga (regorafenib) inhibited growth, reduced Akt and Mapk phosphorylation, and induced apoptosis of human colorectal cancer cell lines harboring BRAF V600E and PIK3CA P449T in culture (PMID: 25838391). 25838391
BRAF V600E PIK3CA P449T colorectal cancer sensitive Pimasertib + Sorafenib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Nexavar (sorafenib) synergistically inhibited proliferation of colorectal cancer cells harboring BRAF V600E and PIK3CA P449T in culture (PMID: 23629727). 23629727
BRAF V600E PIK3CA P449T colorectal cancer resistant Regorafenib Preclinical Actionable In a preclinical study, human colorectal cancer cells harboring BRAF V600E and PIK3CA P449T were resistant to Stivarga (regorafenib) in culture (PMID: 25838391). 25838391
BRAF V600E PIK3CA P449T TP53 R273H colorectal cancer sensitive MLN0128 + PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 synergistically inhibited Erk and PI3K signaling and growth of colorectal cancer cells harboring BRAF V600E, PIK3CA P449T, and TP53 R273H in culture and in cell line xenograft models, but did not have synergistic effect on apoptosis (PMID: 26272063). 26272063
PIK3CA R88Q PTEN mut endometrial cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA R88Q and PTEN mutations in culture (PMID: 22662154). 22662154
PIK3CA R88Q PTEN mut endometrial cancer sensitive Everolimus Preclinical Actionable In a preclinical study, Afinitor (everolimus) inhibited proliferation of endometrial cancer cells harboring PIK3CA R88Q and PTEN mutations in culture (PMID: 22662154). 22662154
PIK3CA R88Q colorectal cancer sensitive Cetuximab + Fluorouracil + Irinotecan + Floxuridine Clinical Study Actionable In a retrospective study, treatment with the combination of Erbitux (cetuximab), Adrucil (fluorouracil), Camptosar (irinotecan), and Floxuridine resulted in at least 24 months without evidence of disease in a colorectal carcinoma patient harboring a PIK3CA R88Q mutation (PMID: 25714871). 25714871
PIK3CA R88Q malignant pleural mesothelioma sensitive GDC-0980 Phase I Actionable In a Phase I trial, treatment with Apitolisib (GDC-0980) resulted in a partial response in a patient with malignant pleural mesothelioma harboring PIK3CA R88Q (PMID: 26787751). 26787751
PIK3CA R88Q PTEN mut KRAS G12V endometrial cancer decreased response Everolimus Preclinical Actionable In a preclinical study, endometrial cancer cells harboring PIK3CA R88Q. PTEN mutations, and KRAS G12V demonstrated decreased sensitivity to Afinitor (everolimus) compared with cells without KRAS mutations in culture (PMID: 22662154). 22662154
PIK3CA R88Q PTEN mut KRAS G12V endometrial cancer decreased response BEZ235 Preclinical Actionable In a preclinical study, endometrial cancer cells harboring PIK3CA R88Q. PTEN mutations, and KRAS G12V demonstrated decreased sensitivity to BEZ235 compared with cells without KRAS mutations in culture (PMID: 22662154). 22662154
PIK3CA E545V ovarian clear cell adenocarcinoma sensitive DS-7423 Preclinical - Cell culture Actionable In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring PIK3CA E545V was sensitive to DS-7423 in culture, demonstrating inhibition of cell proliferation (PMID: 24504419). 24504419
PIK3CA F930S colorectal cancer resistant Fluorouracil + Cetuximab Clinical Study Actionable In a clinical study, PIK3CA F930S was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in colorectal cancer patients, which is consistent with cell culture studies demonstrating moderate resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA F930S (PMID: 28424201). 28424201
PIK3CA V955G colorectal cancer resistant Fluorouracil + Cetuximab Clinical Study Actionable In a clinical study, PIK3CA V955G was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in colorectal cancer patients, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA V955G (PMID: 28424201). 28424201
PIK3CA H450_P458del breast cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, transformed breast epithelial cells expressing PIK3CA H450_P458del were sensitive to treatment with Alpelisib (BYL719) in culture, demonstrating growth inhibition and decreased invasiveness of acini (PMID: 29284706). 29284706
ERBB2 pos PIK3CA mut Her2-receptor positive breast cancer decreased response Trastuzumab Clinical Study Actionable In a clinical study, a retrospective analysis of Herceptin (trastuzumab) treatment in ERBB2 (HER2) positive breast cancer patients demonstrated patients harboring a PIK3CA mutation trended towards a decreased response when compared to patients with wild-type PIK3CA (PMID: 27687302). 27687302
ERBB2 pos PIK3CA mut Her2-receptor positive breast cancer decreased response Lapatinib + Capecitabine Phase III Actionable In a Phase III trial, Tykerb (lapatinib) and Xeloda (capecitabine) combination treatment resulted in decreased median progression free survival (4.3 vs. 6.4 months), median overall survival (17.3 vs. 27.8 months), and overall response rate(17.1% vs. 39.7%) in ERBB2 (HER2) positive breast cancer patients harboring PIK3CA mutations compared to PIK3CA wild type patients (PMID: 26920887). 26920887
ERBB2 pos PIK3CA mut Her2-receptor positive breast cancer decreased response Lapatinib Clinical Study Actionable In a clinical study, a retrospective analysis of Tykerb (lapatinib) treatment in ERBB2 (HER2) positive breast cancer patients demonstrated patients harboring a PIK3CA mutation trended towards a decreased response when compared to patients with wild-type PIK3CA (PMID: 27687302). 27687302
ERBB2 pos PIK3CA mut Her2-receptor positive breast cancer sensitive AT13148 Preclinical - Cell line xenograft Actionable In a preclinical study, AT13148 inhibited tumor growth in a ERBB2 (HER2)-positive human breast cancer cell line xenograft model harboring mutant PIK3CA (PMID: 22781553). 22781553
PIK3CA mutant ERBB2 pos Her2-receptor positive breast cancer decreased response Trastuzumab + Lapatinib Clinical Study Actionable In a clinical study, a retrospective analysis of the combined treatment, Herceptin (trastuzumab) and Tykerb (lapatinib), in ERBB2 (HER2) positive breast cancer patients demonstrated patients harboring a PIK3CA mutation trended towards a decreased response when compared to patients with wild-type PIK3CA (PMID: 27687302). 27687302
PIK3CA mutant ERBB2 pos Her2-receptor positive breast cancer decreased response Trastuzumab + Lapatinib Phase II Actionable In a Phase II trial, ERBB2-positive breast cancer patients harboring PIK3CA mutations demonstrated lower pathologic complete remission rate (12.5%) compared to those with wild-type PIK3CA (48.4%) after Herceptin (trastuzumab) and Tykerb (lapatinib) combination therapy (PMID: 26245675). 26245675
PIK3CA mutant KRAS Q61X ovarian carcinoma sensitive Bevacizumab + Temsirolimus + Doxil Clinical Study Actionable In a clinical study, the combination of Torisel (temsirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxorubicin) resulted in a partial response in a patient with ovarian carcinoma harboring both a PIK3CA mutation and a KRAS Q61 mutation (PMID: 21216929). 21216929
BRAF wild-type KRAS wild-type PIK3CA mutant colorectal cancer sensitive Cetuximab Clinical Study Actionable In a retrospective study, Erbitux (cetuximab) treatment, alone or in combination, resulted in disease regression or stable disease in 88% (7/8) KRAS/BRAF-wild type colorectal carcinoma patients harboring a PIK3CA mutation (PMID: 25714871). 25714871
BRAF V600E PIK3CA mut colorectal cancer sensitive ASN003 Preclinical - Cell line xenograft Actionable In a preclinical study, a colorectal cancer cell line xenograft model co-harboring BRAF V600E and a PIK3CA mutation demonstrated tumor growth inhibition when treated with ASN003 (Mol Cancer Ther 2015;14(12 Suppl 2):Abstract nr B100). detail...
ERBB2 amp PIK3CA mut uterine corpus serous adenocarcinoma sensitive Neratinib + Taselisib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Nerlynx (neratinib) and Taselisib (GDC-0032), compared to either agent alone, resulted in greater inhibition of cell cycle activity in a uterine serous carcinoma cell line harboring ERBB2 (HER2) amplification and a PIK3CA mutation in culture, and in xenograft models, showed increased tumor growth inhibition and tumor regression (PMID: 26333383). 26333383
ERBB2 amp PIK3CA mut Her2-receptor positive breast cancer sensitive Ipatasertib Preclinical - Cell line xenograft Actionable In a preclinical study, ERBB2 (HER2)-receptor positive breast cancer cell line xenograft models harboring amplification of ERBB2 (HER2) and a PIK3CA mutation demonstrated sensitivity to treatment with Ipatasertib (GDC-0068), resulting in inhibition of tumor growth (PMID: 24141624). 24141624
ERBB2 amp PIK3CA mut breast cancer sensitive CUDC-907 Preclinical Actionable In a preclinical study, CUDC-907 inhibited downstream signaling and growth of PIK3CA-mutant breast cancer cells with ERBB2 amplification in culture (PMID: 22693356). 22693356
ERBB2 amp PIK3CA mut Her2-receptor positive breast cancer sensitive Copanlisib Preclinical - Cell line xenograft Actionable In a preclinical study, Aliqopa (copanlisib) promoted tumor regression in xenograft models of a human ERBB2 (HER2)-amplified breast cancer cell line harboring a PIK3CA activating mutation (PMID: 24170767). 24170767
FGFR1 over exp PIK3CA mut estrogen-receptor positive breast cancer sensitive Alpelisib + Lucitanib Preclinical - Cell culture Actionable In a preclinical study, an estrogen-receptor positive breast cancer cell line over expressing FGFR1 and expressing a PIK3CA mutation demonstrated sensitivity to the combination of Alpelisib (BYL719) and Lucitanib (E-3810) in culture (PMID: 27126994). 27126994
PIK3CA mutant CDKN2A mutant breast cancer sensitive Sapanisertib Preclinical Actionable In a preclinical study, a breast cancer cell line harboring mutations in PIK3CA and CDKN2A demonstrated sensitivity to Sapanisertib (MLN0128) in culture (PMID: 25261369). 25261369
KRAS mut PIK3CA mut non-small cell lung carcinoma sensitive Buparlisib Phase II Actionable In a Phase II trial, one patient with Kras and Pikc3a mutant non-squamous NSCLC had a partial response to Buparlisib (BKM120) however, stage 2 of the study was not initiated due to failure of meeting overall stage 1 response endpoints (PMID: 26098748). 26098748
KRAS mut PIK3CA mut non-small cell lung carcinoma sensitive Selumetinib + BEZ235 Preclinical - Cell line xenograft Actionable In a preclinical study, Selumetinib (AZD6244) in combination with BEZ235, synergistically prevented proliferation of an Iressa (gefitinib)-resistant NSCLC cell line harboring KRAS and PIK3CA mutations in culture and in cell line xenograft models (PMID: 24939055). 24939055
KRAS mut PIK3CA mut colon cancer sensitive A-443654 Preclinical Actionable In a preclinical study, A-443654 inhibited proliferation of colon cancer cell lines that have been reported to harbor KRAS and PIK3CA mutations in culture (PMID: 24569089, PMID: 24978597). 24978597 24569089
KRAS mut PIK3CA mut colorectal cancer sensitive CGM097 + Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of CGM097 and Mekinist (trametinib) treatment compared to treatment with either agent alone in a colorectal cancer cell line resulted in a greater decrease in colony formation in culture, and improved stable disease in xenograft models (PMID: 27659046). 27659046
KRAS mut PIK3CA mut Advanced Solid Tumor resistant Everolimus Preclinical Actionable In a preclinical study, human cancer cells with PIK3CA mutations demonstrated sensitivity to Afinitor (everolimus), but a coincident KRAS mutation led to Afinitor (everolimus) resistance (PMID: 20664172). 20664174 20664172
KRAS mut PIK3CA mut colorectal cancer sensitive ABT-263 + CGM097 + Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, Navitoclax (ABT-263) improved the therapeutic effects of the combination of CGM097 and Mekinist (trametinib) in colorectal cancer cells, resulting in greater apoptotic activity and growth inhibition in culture, and tumor regression in xenograft models (PMID: 27659046). 27659046
KRAS mut PIK3CA mut non-small cell lung carcinoma sensitive PF-04691502 Preclinical - Cell line xenograft Actionable In a preclinical study, PF-04691502 inhibited tumor growth in non-small cell lung cancer cell line xenograft models harboring both PIK3CA and KRAS mutations (PMID: 21750219). 21750219
KRAS mut PIK3CA mut colon cancer sensitive GDC-0980 Preclinical - Cell line xenograft Actionable In a preclincal study, GDC-0980 delayed tumor growth in colon cancer cell line xenograft models harboring KRAS and PIKC3A mutations (PMID: 21998291). 21998291
KRAS mut PIK3CA mut colon cancer sensitive CUDC-907 Preclinical Actionable In a preclinical study, CUDC-907 inhibited growth and induced apoptosis in a human colon cancer cell line harboring PIK3CA and KRAS mutations (PMID: 22693356). 22693356
KRAS mut PIK3CA mut colorectal cancer sensitive SAR245409 Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line co-harboring a KRAS mutation and PIK3CA mutation was sensitive to XL765 (SAR245409), demonstrating inhibition of cell proliferation in culture (PMID: 24634413). 24634413
KRAS mut PIK3CA mut colon cancer sensitive Copanlisib Preclinical - Cell line xenograft Actionable In a preclinical study, treatment with Aliqopa (copanlisib) inhibited tumor growth in xenograft models of a human colon cancer cell line harboring PIK3CA and KRAS mutations (PMID: 24170767). 24170767
KRAS mut PIK3CA mut colorectal cancer no benefit Taselisib Phase I Actionable In a Phase I trial, a colorectal cancer patient co-harboring a PIK3CA mutation and KRAS mutation progressed on treatment with Taselisib (GDC-0032) (PMID: 28331003). 28331003
KRAS mut PIK3CA mut Advanced Solid Tumor sensitive CH5132799 Preclinical Actionable In a preclinical study, human solid tumor cell lines harboring coincident PIK3CA and KRAS mutations demonstrated sensitivity to CH5132799 in culture (PMID: 21558396). 21558396
KRAS mut PIK3CA mut Advanced Solid Tumor sensitive Alpelisib Preclinical Actionable In a preclinical study, Alpelisib (BYL719) inhibited growth in multiple tumor cell lines expressing PIK3CA mutations, and concurrent KRAS mutations was not associated with resistance (PMID: 24608574). 24608574
KRAS mut PIK3CA mut non-small cell lung carcinoma decreased response Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) mildly inhibited the growth of an Iressa (gefitinib)-resistant NSCLC cell line with KRAS and PIK3CA mutations (PMID: 24939055). 24939055
KRAS mut PIK3CA mut Advanced Solid Tumor decreased response Taselisib Phase I Actionable In a Phase I trial, Taselisib (GDC-0032) demonstrated activity in patients with PIK3CA-mutant advanced solid tumors, but preliminary data analysis suggested the presence of a KRAS mutation was associated with lack of response (Cancer Res October 1, 2014 74:915). detail...
KRAS mut PIK3CA mut colorectal cancer resistant BEZ235 Preclinical Actionable In a preclinical study, colon cancer cells harboring KRAS and PIK3CA mutations demonstrated resistance to BEZ235 in culture and xenograft models (PMID: 23475782). 23475782
KRAS mut PIK3CA mut colorectal cancer sensitive AZD8055 + Selumetinib Preclinical Actionable In a preclinical study, the combination of AZD8055 and Selumetinib (AZD6244) inhibited tumor growth in a colorectal cancer xenograft model harboring PIK3CA and KRAS mutations and had increased efficacy compared to either agent alone (PMID: 22271687). 22271687
KRAS mut PIK3CA mut colon cancer sensitive AT13148 Preclinical Actionable In a preclinical study, a colon cancer cell line harboring PIK3CA and KRAS mutations demonstrated sensitivity to AT13148 in culture (PMID: 22781553). 22781553
KRAS mut PIK3CA mut non-small cell lung carcinoma sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited the growth of an Iressa (gefitinib)-resistant NSCLC cell line with KRAS and PIK3CA mutations (PMID: 24939055). 24939055
KRAS mut PIK3CA mut stomach cancer sensitive Buparlisib Preclinical Actionable In a preclinical study, BKM120 suppressed growth of a gastric cancer cell line harboring PIK3CA and KRAS mutations in culture (PMID: 22159814). 22159814
KRAS mut PIK3CA mut stomach cancer predicted - sensitive Deguelin Preclinical Actionable In a preclinical study, Deguelin inhibited growth of the AGS gastric cancer cell line, which has been reported to harbor PIK3CA and KRAS mutations, in culture (PMID: 20811676, PMID: 24978597). 20811676 24978597
PIK3CA mutant PTEN loss prostate cancer sensitive PKI-179 Preclinical - Cell culture Actionable In a preclinical study, PKI-179 inhibited growth of prostate cancer cells harboring PIK3CA mutations and PTEN loss in culture (PMID: 20797855). 20797855
PIK3CA mutant PTEN loss breast cancer sensitive AZD6482 + BYL719 Preclinical - Pdx Actionable In a preclinical study, AZD6482 and Alpelisib (BYL719) combination treatment inhibited Akt signaling and growth in a breast cancer patient-derived xenograft (PDX) model harboring a PIK3CA mutation and PTEN loss (Cancer Res October 1, 2014 74; LB-327). detail...
PIK3CA mutant PTEN loss breast cancer sensitive Buparlisib Preclinical - Pdx Actionable In a preclinical study, Buparlisib (BKM120) inhibited Akt signaling and growth in a PDX model of breast cancer cells harboring a PIK3CA mutation and PTEN loss ( Cancer Res October 1, 2014 74; LB-327 ). detail...
PIK3CA mutant PTEN loss breast cancer resistant Alpelisib Clinical Study Actionable In a case study, a breast cancer patient harboring a PIK3CA mutation developed resistance to Alpelisib (BYL719) treatment and progressive disease after initial response, accompanied by a loss of PTEN (Cancer Res October 1, 2014 74; LB-327). detail...
PIK3CA mutant PTEN loss breast cancer resistant Alpelisib Preclinical - Pdx Actionable In a preclinical study, a breast cancer patient-derived xenograft (PDX) model harboring a PIK3CA mutation and PTEN loss was resistant to Alpelisib (BYL719)-induced inhibition of Akt signaling and growth (Cancer Res October 1, 2014 74; LB-327). detail...
APC mut BRAF mut PIK3CA mut SMAD4 mut TP53 mut colorectal cancer sensitive Sapanisertib Preclinical Actionable In a preclinical study, a rapamycin-resistant colorectal cancer cell line harboring mutations in APC, BRAF, PIK3CA, SMAD4 and TP53 was sensitive to Sapanisertib (MLN0128) resulting in inhibition of MTORC1 signaling (PMID: 25261369). 25261369
PIK3CA mutant KRAS G12X KRAS G13X colorectal cancer sensitive Temsirolimus + Bevacizumab Clinical Study Actionable In a clinical study, a colorectal cancer patient harboring a PIK3CA mutation and KRAS mutations at codons 12 and 13 demonstrated stable disease when treated with a combination of Torisel (temsirolimus) and Avastin (bevacizumab) (PMID: 21216929). 21216929
PIK3CA mutant stomach cancer sensitive BAY1082439 Preclinical Actionable In a preclinical study, BAY1082439 inhibited growth of gastric cancer cells harboring PIK3CA mutations in culture and xenograft models (AACR; 2015. Abstract nr 2674). detail...
PIK3CA mutant head and neck cancer sensitive Alpelisib Phase I Actionable In a Phase I trial, Alpelisib (BYL719) treatment resulted in a disease control rate of 68.4% (13/19, 0 complete response (CR), 0 partial response (PR), 13 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 10.5% (2/19) in patients with head and neck cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). 29401002
PIK3CA mutant head and neck squamous cell carcinoma sensitive Radiotherapy + Taselisib Preclinical - Pdx & cell culture Actionable In a preclinical study, Taselisib (GDC-0032) enhanced the effects of radiation induced apoptosis in HNSCC cell lines, cell line xenograft models, and a patient derived xenograft (PDX) model, all with PIK3CA mutations (PMID: 26589432). 26589432
PIK3CA mutant breast cancer no benefit Temsirolimus Phase II Actionable In a Phase II trial, Torisel (temsirolimus) treatment resulted in stable disease in 9.7% (3/31) of breast cancer patients positive for ER, PR or ERBB2 (HER2), however there was no association between PIK3CA mutational status and clinical benefits (PMID: 22245973). 22245973
PIK3CA mutant triple-receptor negative breast cancer predicted - sensitive Ipatasertib + Paclitaxel Phase II Actionable In a Phase II trial, Ipatasertib (GDC-0068) in combination with Abraxane (paclitaxel) resulted in improved progression free survival (6.2 vs 4.9 months) compared to placebo in triple-receptor negative breast cancer patients harboring mutations in PIK3CA, AKT1, or PTEN (J Clin Oncol 35, 2017 (suppl; abstr 1009)). detail...
PIK3CA mutant triple-receptor negative breast cancer sensitive Palbociclib + Pictilisib Preclinical Actionable In a preclinical study, Ibrance (palbociclib) and Pictilisib (GDC-0941) worked synergistically to inhibit the survival of triple-receptor negative breast cancer cell lines harboring PIK3CA mutations in culture (PMID: 27020857). 27020857
PIK3CA mutant hematologic cancer sensitive CUDC-907 Preclinical - Cell line xenograft Actionable In a preclinical study, CUDC-907 inhibited PIK3CA, blocked downstream AKT pathway activation, and induced apoptosis and cell cycle arrest in both PIK3CA wild-type and PIK3CA mutant human cancer cell lines and xenograft models of multiple solid and hematologic cancers (PMID: 22693356). 22693356
PIK3CA mutant Advanced Solid Tumor sensitive Sapanisertib Preclinical Actionable In a preclinical study, human cancer cell lines harboring PIK3CA mutations were sensitive to Sapanisertib (MLN0128) as demonstrated by significant growth inhibition (PMID: 25261369). 25261369
PIK3CA mutant Advanced Solid Tumor sensitive Carboxyamidotriazole Orotate Phase I Actionable In a Phase I clinical trial, carboxyamidotriazole orotate treatment demonstrated some efficacy in patients with various solid tumors, including patients harboring PIK3CA mutations (J Clin Oncol 31, 2013 (suppl; abstr 2518)). detail...
PIK3CA mutant cervical cancer decreased response Cetuximab Phase II Actionable In a Phase II clinical trial, Erbitux (cetuximab) treatment, in addition to radiochemotherapy, did not result in any complete responses (0/8) and demonstrated a worse disease free survival when compared to radiochemotherapy alone in cervical cancer patients harboring PIK3CA mutations (PMID: 25724520). 25724520
PIK3CA mutant Advanced Solid Tumor sensitive CUDC-907 Preclinical - Cell line xenograft Actionable In a preclinical study, CUDC-907 inhibited PIK3CA, blocked downstream AKT pathway activation, and induced apoptosis and cell cycle arrest in both PIK3CA wild-type and PIK3CA mutant human cancer cell lines and xenograft models of multiple tumor types (PMID: 22693356). 22693356
PIK3CA mutant ovarian cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of ovarian cancer cells with PIK3CA mutations in culture (PMID: 21558396). 21558396
PIK3CA mutant Advanced Solid Tumor sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited growth of a variety of advanced solid tumor models with Pik3ca mutations in culture (PMID: 26839307). 26839307
PIK3CA mutant breast cancer sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited tumor growth in breast cancer xenograft models harboring PIK3CA mutations (AACR; 2015. Abstract nr 2665). detail...
PIK3CA mutant estrogen-receptor positive breast cancer no benefit Fulvestrant + Pictilisib Phase II Actionable In a Phase II trial, Falsodex (fulvestrant) and Pictilisib (GDC-0941) combination treatment resulted in similar progression free survival in ER positive breast cancer patients harboring PIK3CA mutations and those who were PIK3CA wild-type (PMID: 27174596). 27174596
PIK3CA mutant female reproductive organ cancer predicted - sensitive Capivasertib Phase I Actionable In a Phase I trial, treatment with AZD5363 was well-tolerated and resulted in tumor shrinkage in 56% (14/25) patients with PIK3CA-mutant gynecological cancers, however, the response rate was modest with confirmed RECIST responses in 8% (2/26) of patients (PMID: 29066505; NCT01226316). 29066505
PIK3CA mutant stomach cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 demonstrated efficacy in promoting apoptosis of gastric cancer cells harboring a PIK3CA mutation in culture (PMID: 22543857). 22543857
PIK3CA mutant Advanced Solid Tumor sensitive MSC2363318A Preclinical Actionable In a preclinical study, MSC2363318A demonstrated anti-proliferative activity against many solid tumor cell lines with PI3K pathway genomic alterations, and inhibited tumor growth in several human cancer xenograft models of breast, pancreatic, glioblastoma and ovarian cancers (Mol Cancer Ther 2013;12(11 Suppl):A162). detail...
PIK3CA mutant non-small cell lung carcinoma sensitive PWT33597 Preclinical Actionable In a preclinical study, PWT33597 decreased signaling of mTOR and PIK3 pathways in non-small cell lung cancer cells with Pik3ca mutations (Cancer Res 2011;71(8 Suppl):Abstract nr 4485). detail...
PIK3CA mutant squamous cell carcinoma sensitive Carboxyamidotriazole Orotate Phase I Actionable In a Phase I clinical trial, carboxyamidotriazole orotate treatment demonstrated some efficacy in patients with various solid tumors including squamous cell carcinomas (tonsil) with PI3KCA and NRAS mutations (J Clin Oncol 31, 2013 (suppl; abstr 2518)). detail...
PIK3CA mutant endometrial cancer sensitive GDC-0980 Phase II Actionable In a Phase II trial, Apitolisib (GDC-0980) was poorly tolerated, but demonstrated efficacy in endometrial cancer patients harboring mutations in PIK3CA, PTEN, or AKT1 (J Clin Oncol 32:5s, 2014 (suppl; abstr 5513)). detail...
PIK3CA mutant breast cancer sensitive OSI-027 Preclinical - Cell line xenograft Actionable In a preclinical study, OSI-027 induced tumor regression in breast cancer cell line xenograft models harboring PIK3CA mutations (PMID: 21673091). 21673091
PIK3CA mutant breast cancer sensitive AT13148 Preclinical - Cell line xenograft Actionable In a preclinical study, a ERBB3 (HER3) positive breast cancer cell line xenograft model harboring a PIK3CA mutation was demonstrated decreased tumor growth when treated with AT13148 (PMID: 22781553). 22781553
PIK3CA mutant prostate cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of prostate cancer cells with PIK3CA mutations in culture (PMID: 21558396). 21558396
PIK3CA mutant endometrial cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of endometrial cancer cells with PIK3CA mutations in culture (PMID: 21558396). 21558396
PIK3CA mutant Advanced Solid Tumor sensitive Alpelisib Preclinical - Cell line xenograft Actionable In a preclinical study, PIK3CA mutations were associated with sensitivity to Alpelisib (BYL719) in human tumor cell lines in culture and in xenograft models (PMID: 24608574). 24608574
PIK3CA mutant Advanced Solid Tumor sensitive Alpelisib Phase I Actionable In a Phase I trial, Alpelisib (BYL719) demonstrated safety and efficacy in patients with advanced solid tumor harboring PIK3CA mutations, resulted in a disease control rate of 58.2% (78/134, 1 complete response (CR), 7 partial response (PR), 70 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 15.7% (21/134) (PMID: 29401002; NCT01219699). 29401002
PIK3CA mutant endometrioid ovary carcinoma sensitive Capivasertib Phase I Actionable In a Phase I clinical trial, AZD5363 demonstrated safety and efficacy in patients with advanced solid tumors, including prolonged stable disease in one patient with a PIK3CA-mutant endometrioid ovarian cancer (American Association for Cancer Research; 06 Apr 2013-10 Apr 2013; Abstract LB-66). detail...
PIK3CA mutant breast cancer predicted - sensitive Capivasertib Preclinical Actionable In a preclinical study, AZD5363 inhibited growth in breast cancer cell lines and xenograft models expressing PIK3CA mutations (PMID: 22294718). 22294718
PIK3CA mutant breast cancer predicted - sensitive Capivasertib Phase I Actionable In a Phase I trial, treatment with AZD5363 was well-tolerated and resulted in tumor shrinkage in 46% (12/26) patients with PIK3CA-mutant breast cancer, with confirmed RECIST responses in 4% (1/28) of patients (PMID: 29066505; NCT01226316). 29066505
PIK3CA mutant Advanced Solid Tumor sensitive PX-866 Phase I Actionable In a Phase I trial, PX-866 demonstrated efficacy and was well tolerated in patients with advanced solid tumor with both PIK3CA wild-type and mutant status (PMID: 22693357). 22693357
PIK3CA mutant Advanced Solid Tumor sensitive AT-7867 Preclinical Actionable In a preclinical study, AT-7867 inhibited proliferation in several human tumor cell lines harboring PIK3CA mutations in culture (PMID: 20423992). 20423992
PIK3CA mutant Her2-receptor negative breast cancer no benefit Capivasertib + Paclitaxel Phase II Actionable In a Phase II trial, the addition of AZD5363 to Taxol (paclitaxel) therapy did not improve progression-free survival compared to placebo (10.9 vs 10.8 months) in patients with PIK3CA-mutant, Esr1-positive, Erbb2 (Her2)-negative breast cancer (Ann Oncol 2017, Vol 28, Suppl 5, Abstract #241PD; NCT01625286). detail...
PIK3CA mutant ovarian cancer sensitive Temsirolimus Phase I Actionable In a Phase I clinical trial, Torisel (temsirolimus) demonstrated limited efficacy in ovarian cancer patients with PIK3CA mutations (PMID: 22271473). 22271473
PIK3CA mutant Her2-receptor positive breast cancer sensitive CCT128930 Preclinical - Cell line xenograft Actionable In a preclinical study, CCT128930 induced growth arrest and inhibited tumor growth in a xenograft model of a ERBB2 (HER2)-positive human breast cancer cell line harboring a PIK3CA mutation (PMID: 21191045). 21191045
PIK3CA mutant Her2-receptor negative breast cancer sensitive Alpelisib Phase I Actionable In a Phase I trial, Alpelisib (BYL719) treatment resulted in a disease control rate of 60.9% (14/23, 0 complete response (CR), 1 partial response (PR), 13 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 17.4% (4/23) in patients with ER-positive, ERBB2 (HER2)-negative breast cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). 29401002
PIK3CA mutant Advanced Solid Tumor sensitive BAY1082439 Preclinical Actionable In a preclinical study, BAY1082439 induced regression in xenograft models of advanced solid tumors with PIK3CA mutations (Cancer Res April 15, 2012 72; 2799). detail...
PIK3CA mutant colorectal cancer predicted - sensitive MS417 + Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) and MS417 in combination resulted in improved growth inhibition and increased cell death compared to either agent alone in colorectal cancer cell lines harboring PIK3CA mutations in culture (PMID: 26058079). 26058079
PIK3CA mutant breast cancer predicted - sensitive GDC-0077 Preclinical - Pdx & cell culture Actionable In a preclinical study, GDC-0077 inhibited proliferation and induced apoptosis in PIK3CA-mutant breast cancer cell lines in culture, and induced apoptosis and tumor regression in PIK3CA-mutant breast cancer cell line and patient-derived xenograft models (AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 156). detail...
PIK3CA mutant Advanced Solid Tumor sensitive VS-5584 Preclinical Actionable In preclinical studies, VS-5584 demonstrated efficacy in a variety of cancer cell lines, particularly those harboring PIK3CA mutations (PMID: 23270925). 23270925
PIK3CA mutant breast adenocarcinoma sensitive GS-9820 Preclinical - Cell line xenograft Actionable In a preclinical study, Acalisib (GS-9820) resulted in tumor growth inhibition in xenograft models of breast adenocarcinoma harboring a PIK3CA mutation (Mol Cancer Ther 2009;8(12 Suppl):B136). detail...
PIK3CA mutant stomach cancer predicted - sensitive MLN1117 Clinical Study Actionable In a Phase I trial, MLN1117 treatment resulted in partial response in 3 patients with gastric cancer harboring PI3CA mutations (PMID: 28490463). 28490463
PIK3CA mutant Advanced Solid Tumor sensitive MLN1117 Preclinical Actionable In a preclinical study, MLN1117 inhibited proliferation of tumor cells harboring oncogenic PIK3CA mutations in culture and inhibited tumor growth in PIK3CA mutant xenograft models (Cancer Ther 2011;10(11 Suppl):Abstract nr A171). detail...
PIK3CA mutant Advanced Solid Tumor sensitive MLN1117 Phase I Actionable In a Phase I trial, MLN1117 demonstrated safety and preliminary efficacy in a variety of patients with advanced solid tumors carrying PIK3CA mutations (Journal of Clinical Oncology, 2015 ASCO Annual Meeting Vol 33, No 15_suppl., 2015: 2501). detail...
PIK3CA mutant Advanced Solid Tumor predicted - sensitive GSK2141795 Phase I Actionable In a Phase I clinical trial, GSK2141795 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, with 4 patients with PIK3CA mutations and/or PTEN loss achieving stable disease for greater than 6 months (J Clin Oncol 29: 2011 (suppl; abstr 3003)). detail...
PIK3CA mutant endometrial cancer sensitive Pictilisib Preclinical Actionable In a preclinical study, endometrioid endometrial cancer cell lines harboring PIK3CA mutations demonstrated increased sensitivity to GDC-0941 (Pictilisib) induced growth inhibition comparing to PIK3CA wild-type cells in culture (PMID: 23674493). 23674493
PIK3CA mutant invasive bladder transitional cell carcinoma predicted - resistant Cisplatin + Gemcitabine + Sorafenib Phase II Actionable In a Phase II trial, PIK3CA mutations were more frequent in muscle-invasive urothelial bladder cancer patients that did not respond to Nexavar (sorafenib), Platinol (cisplatin) and Gemzar (gemcitabine) combination therapy than those who did respond (J Clin Oncol 35, 2017 (suppl 6S; abstract 345)). detail...
PIK3CA mutant breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, breast cancer cells with PIK3CA mutations, both with and without ERBB2 (HER2) amplification, demonstrated sensitivity to CH5132799 in culture (PMID: 21558396). 21558396
PIK3CA mutant colorectal cancer sensitive Alpelisib Phase I Actionable In a Phase I trial, Alpelisib (BYL719) treatment resulted in a disease control rate of 34.3% (12/35, 0 complete response (CR), 2 partial response (PR), 10 stable disease (SD)), and a clinical benefit rate (CR+PR+SD>24 weeks) of 8.6% (3/35) in patients with colorectal cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). 29401002
PIK3CA mutant cervical cancer predicted - sensitive Alpelisib Phase I Actionable In a Phase I trial, Alpelisib (BYL719) treatment resulted in partial response in 3 patients with cervical cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). 29401002
PIK3CA mutant Advanced Solid Tumor sensitive A-443654 Preclinical Actionable In a preclinical study, cells expressing mutant PIK3CA demonstrated increased sensitivity to A-443654 compared to cells expressing wild-type PIK3CA (PMID: 19208828). 19208828
PIK3CA mutant breast cancer sensitive VS-5584 Preclinical Actionable In a preclinical study, PIK3CA mutant breast cancer cells showed increased sensitivity to VS-5584 compared to PIK3CA wild-type cells in culture (PMID: 23270925). 23270925
PIK3CA mutant breast cancer sensitive CUDC-907 Preclinical Actionable In a preclinical study, CUDC-907 inhibited growth of human breast cancer cell lines harboring PIK3CA mutations in culture (PMID: 22693356). 22693356
PIK3CA mutant Advanced Solid Tumor sensitive GDC-0980 Phase I Actionable In a Phase I trial, Apitolisib (GDC-0980) treatment resulted in partial response in 21% (3/14) and stable disease in 57% (8/14) of patients with advanced solid tumors harboring PIK3CA mutations (PMID: 26787751). 26787751
PIK3CA mutant gastric adenocarcinoma sensitive PI-103 + 5-FU Preclinical Actionable In a preclinical study, PI-103 enhanced sensitivity to 5-FU in gastric cancer cells with mutant PIK3CA (PMID: 22336586). 22336586
PIK3CA mutant endometrial cancer sensitive Alpelisib Phase I Actionable In a Phase I trial, Alpelisib (BYL719) treatment resulted in complete response in 1 and partial response in 1patient with endometrial cancer harboring PIK3CA mutations (PMID: 29401002; NCT01219699). 29401002
PIK3CA mutant ovarian cancer sensitive OSI-027 Preclinical - Cell line xenograft Actionable In a preclinical study, OSI-027 inhibited tumor growth in ovarian cancer cell line xenograft models harboring PIK3CA mutations (PMID: 21673091). 21673091
PIK3CA mutant Her2-receptor negative breast cancer sensitive Alpelisib + Fulvestrant Phase III Actionable In a Phase III (SOLAR?1) trial, Alpelisib (BYL719) and Faslodex (fulvestrant) combination therapy significantly improved median progression-free survival (11.0 vs 5.7 months, HR=0.65, p=0.00065), and overall response rate (36% vs 16%, p=0.0002) compared to placebo in hormone receptor-positive, Erbb2 (Her2)-negative breast cancer patients harboring PIK3CA mutations (ESMO 2018 Congress, Oct 2018, Presidential Symposium 1, abstract LBA3; NCT02437318). detail...
PIK3CA mutant head and neck squamous cell carcinoma predicted - sensitive Carboplatin + Paclitaxel + Temsirolimus Phase II Actionable In a Phase II trial, two patients with head and neck squamous cell carcinoma harboring a PIK3CA mutation who had stable disease demonstrated some tumor regression when treated with the combination of Torisel (temsirolimus), Paraplatin (carboplatin), and Taxol (paclitaxel) (PMID: 28961834). 28961834
PIK3CA mutant estrogen-receptor positive breast cancer predicted - sensitive Letrozole Phase III Actionable In a Phase III trial, estrogen-receptor positive breast cancer patients harboring a PIK3CA mutation demonstrated a greater benefit when treated with Femara (letrozole) compared to Nolvadex (tamoxifen) (PMID: 29902286; NCT00004205). 29902286
PIK3CA mutant colon cancer sensitive PWT33597 Preclinical Actionable In a preclinical study, PWT33597 decreased signaling of mTOR and PIK3 pathways in colon cancer cells with Pik3ca mutations (Cancer Res 2011;71(8 Suppl):Abstract nr 4485). detail...
PIK3CA mutant breast cancer sensitive Sapanisertib Preclinical Actionable In a preclinical study, Sapanisertib (MLN0128) demonstrated efficacy in PIK3CA mutant breast cancer xenograft models (PMID: 23085766). 23085766
PIK3CA mutant Advanced Solid Tumor sensitive CC-223 Phase I Actionable In a Phase I trial, CC-223 demonstrated safety and preliminary efficacy in patients with solid tumors, including stable disease for greater than 110 days in 2 patients with PIK3CA mutation or PTEN deletion (PMID: 26177599). 26177599 detail...
PIK3CA mutant colon cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 demonstrated efficacy in promoting apoptosis of colon cancer cells harboring a PIK3CA mutation in culture (PMID: 22543857). 22543857
PIK3CA mutant breast cancer sensitive Alpelisib + GSK2334470 Preclinical - Cell line xenograft Actionable In a preclinical study, GSK2334470 resensitized Alpelisib (BYL719)-resistant breast cancer cell lines harboring PIK3CA mutations to Alpelisib (BYL719) in culture and in cell line xenograft models (PMID: 27451907). 27451907
PIK3CA mutant estrogen-receptor positive breast cancer sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA mutations in culture and suppressed tumor growth in xenograft models (PMID: 26839307). 26839307
PIK3CA mutant ovarian cancer sensitive BKM120 + Olaparib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Buparlisib (BKM120) and Lynparza (olaparib) worked synergistically to induce apoptosis and inhibit growth of ovarian cancer cell lines harboring PIK3CA mutations in culture, and induced apoptosis and decreased proliferation of PIK3CA-mutant ovarian cancer cell line xenograft models (PMID: 26909613). 26909613
PIK3CA mutant breast cancer no benefit GSK2126458 Phase I Actionable In a Phase I trial, GSK2126458 was well-tolerated and resulted in some efficacy in patients with breast cancer harboring a PIK3CA mutation including stable disease in 22% (2/9), however, objective response rate was not associated with PIK3CA mutations when compared to those without PIK3CA mutations (PMID: 26603258). 26603258
PIK3CA mutant Advanced Solid Tumor sensitive Taselisib Phase I Actionable In a Phase I trial, Taselisib (GDC-0032) demonstrated activity in patients with PIK3CA-mutant advanced solid tumors, in the absence of alterations in the MAPK or PTEN pathways (Cancer Res October 1, 2014 74:915). detail...
PIK3CA mutant breast cancer predicted - sensitive MLN1117 Phase I Actionable In a Phase I trial, MLN1117 treatment resulted in partial response in 3 patients with breast cancer harboring PI3CA mutations (PMID: 28490463). 28490463
PIK3CA mutant breast cancer sensitive Pictilisib Preclinical Actionable In a preclinical study, GDC-0941 inhibited growth and induced apoptosis in breast cancer cells expressing PIK3CA mutations (PMID: 24601221). 24601221
PIK3CA mutant endometrial cancer no benefit Temsirolimus Phase II Actionable In a retrospective study of a Phase II trial, mutation status of PIK3CA was not associated with progression-free survival or response rate in advanced endometrial cancer patients treated with Torisel (temsirolimus) (PMID: 27016228). 27016228
PIK3CA mutant Advanced Solid Tumor sensitive XL147 Preclinical Actionable In a preclinical study, tumor cell lines with PIK3CA mutations demonstrated sensitivity to XL147 in culture (PMID: 25637314). 25637314
PIK3CA mutant Advanced Solid Tumor sensitive XL147 Phase I Actionable In a Phase I clinical trial, XL147 (SAR24508) was shown to be safe and potentially efficacious, with clinical activity seen irrespective of tumor PI3K pathway molecular alterations (PMID: 24166903). 24166903
PIK3CA mutant triple-receptor negative breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, triple-receptor negative breast cancer cell lines harboring PIK3CA mutations demonstrated increased sensitivity to Pictilisib (GDC-0941) in culture (PMID: 27196766). 27196766
PIK3CA mutant Advanced Solid Tumor sensitive Bevacizumab + Temsirolimus + Doxil Clinical Study Actionable In a clinical study, the combination of Torisel (temisirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxirubicin) resulted in stable disease in patients with advanced solid tumors harboring PIK3CA mutations (PMID: 21216929). 21216929
PIK3CA mutant Advanced Solid Tumor sensitive Bevacizumab + Temsirolimus + Doxil Clinical Study Actionable In a clinical study, the combination of Torisel (temsirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxorubicin) resulted in a partial response in patients with advanced solid tumors harboring PIK3CA mutations (PMID: 21216929). 21216929
PIK3CA mutant estrogen-receptor positive breast cancer no benefit Fulvestrant Phase II Actionable In a Phase II trial, Falsodex (fulvestrant) treatment resulted in similar progression free survival in ER positive breast cancer patients harboring PIK3CA mutations and those who were PIK3CA wild-type (PMID: 27174596). 27174596
PIK3CA mutant non-small cell lung carcinoma sensitive PF-04691502 Preclinical - Cell line xenograft Actionable In a preclinical study, PF-04691502 inhibited tumor growth in non-small cell lung cancer cell line xenograft models harboring PIK3CA mutations (PMID: 21750219). 21750219
PIK3CA mutant breast cancer sensitive Letrozole + Taselisib Phase Ib/II Actionable In a Phase Ib trial, Taselisib (GDC-0032) and Femara (letrozole) combination therapy resulted in an overall response rate of 38% in breast cancer patients with PIK3CA mutations, compared to 9% in patients with wild-type PIK3CA (Cancer Res May 1, 2015 75; PD5-2). detail...
ERBB2 over exp PIK3CA mut breast cancer sensitive ARQ092 + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer xenograft model with ERBB2 (HER2) over expression and harboring a PIK3CA mutation was sensitive to the combination treatment of ARQ092 and Herceptin (trastuzumab), demonstrating greater inhibition of tumor growth when compared to treatment with either agent alone (PMID: 26469692). 26469692
ERBB2 over exp PIK3CA mut Her2-receptor positive breast cancer sensitive PKI-179 Preclinical - Cell line xenograft Actionable In a preclinical study, PKI-179 inhibited growth of breast cancer cells harboring PIK3CA mutations and ERBB2 (HER2) over expression in culture and cell line xenograft models (PMID: 20797855). 20797855
ERBB2 over exp PIK3CA mut breast cancer sensitive ARQ092 + Paclitaxel Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer xenograft model with ERBB2 (HER2) over expression and harboring a PIK3CA mutation was sensitive to the combination treatment of ARQ092 and Taxol (paclitaxel), demonstrating greater inhibition of tumor growth when compared to treatment with either agent alone (PMID: 26469692). 26469692
PIK3CA V952A colorectal cancer resistant Fluorouracil + Cetuximab Clinical Study Actionable In a clinical study, PIK3CA V952A was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in colorectal cancer patients, which is consistent with cell culture studies demonstrating moderate resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA V952A (PMID: 28424201). 28424201
BRAF V600E PIK3CA H1047K melanoma sensitive ARQ092 + Trametinib Preclinical - Pdx Actionable In a preclinical study, a melanoma patient-derived xenograft (PDX) model harboring BRAF V600E and PIK3CA H1047K was sensitive to the combination treatment of ARQ092 and Mekinist (trametinib), demonstrating a greater inhibition of tumor growth when compared to either agent alone (PMID: 26469692). 26469692
ERBB2 amp PIK3CA N345K breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA N345K and ERBB2 (HER2) amplification in culture (PMID: 21558396). 21558396
PIK3CA N345K breast cancer sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA N345K breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA N345K breast cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA N345K breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA N345K breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA N345K Advanced Solid Tumor sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
PIK3CA N345K breast cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). 26627007
KRAS G12D PIK3CA Q546R colorectal cancer sensitive Bevacizumab + Sorafenib Clinical Study Actionable In a clinical case study, a patient with colorectal cancer harboring KRAS G12D and PIK3CA Q546R demonstrated sensitivity to treatment with the combination of Nexavar (sorafenib) and Avastin (bevacizumab), resulting in stable disease for more than 6 months (PMID: 25363205). 25363205
PIK3CA Q546R prostate cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of prostate cancer cells harboring PIK3CA Q546R in culture (PMID: 21558396). 21558396
KRAS G12D PIK3CA G1049R endometrial cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of endometrial cancer cells harboring PIK3CA G1049R and KRAS G12D mutations in culture (PMID: 21558396). 21558396
PIK3CA G1049R breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R Advanced Solid Tumor sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R breast cancer sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R breast cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R breast cancer sensitive Alpelisib Preclinical Actionable In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). 26627007
PIK3CA G1049R breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA G1049R demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
EGFR L858R EGFR T790M PIK3CA G118D non-small cell lung carcinoma decreased response Pimasertib Preclinical - Cell culture Actionable In a preclinical study, non-small cell lung cancer cells harboring EGFR L858R, T790M, and PIK3CA G118D demonstrated decreased response to Pimasertib (MSC1936369B) in culture (PMID: 23629727). 23629727
EGFR L858R EGFR T790M PIK3CA G118D non-small cell lung carcinoma sensitive Pimasertib + BEZ235 Preclinical - Cell line xenograft Actionable In a preclinical study, Pimasertib (MSC1936369B) and BEZ235 combination treatment inhibited tumor growth in non-small cell lung cancer cell line xenograft models harboring EGFR L858R, EGFR T790M, and PIK3CA G118D in culture (PMID: 23629727). 23629727
EGFR L858R EGFR T790M PIK3CA G118D non-small cell lung carcinoma sensitive Everolimus + Pimasertib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Afinitor (everolimus) synergistically inhibited proliferation of non-small cell lung cancer cells harboring EGFR L858R, EGFR T790M, and PIK3CA G118D in culture (PMID: 23629727). 23629727
EGFR L858R EGFR T790M PIK3CA G118D non-small cell lung carcinoma sensitive Pimasertib + Regorafenib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) and Stivarga (regorafenib) synergistically inhibited proliferation of non-small cell lung cancer cells harboring EGFR L858R, EGFR T790M, and PIK3CA G118D in culture (PMID: 23629727). 23629727
EGFR L858R EGFR T790M PIK3CA G118D non-small cell lung carcinoma sensitive Pimasertib + Sorafenib Preclinical - Cell line xenograft Actionable In a preclinical study, Pimasertib (MSC1936369B) and Nexavar (sorafenib) synergistically inhibited Mapk and Akt signaling, resulted in growth inhibition of non-small cell lung cancer cells harboring EGFR L858R, EGFR T790M, and PIK3CA G118D in culture and in cell line xenograft models (PMID: 23629727). 23629727
PIK3CA G118D non-small cell lung carcinoma sensitive LY3023414 Preclinical - Cell line xenograft Actionable In a preclinical study, LY3023414 inhibited proliferation of non-small cell lung cancer cells harboring PIK3CA G118D in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 27439478). 27439478
KRAS G13D PIK3CA H1047R TP53 wild-type colorectal cancer sensitive MLN0128 + PD-0325901 Preclinical - Cell line xenograft Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 synergistically inhibited Erk and PI3K signaling and proliferation, induced apoptosis in TP53-wild-type colorectal cancer cells harboring KRAS G13D and PIK3CA H1047R in culture and in cell line xenograft models (PMID: 26272063). 26272063
KRAS G12C PIK3CA H1047R TP53 R248W colorectal cancer no benefit MLN0128 + PD-0325901 Preclinical - Pdx Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 combination treatment did not result in tumor growth stabilization in patient-derived xenograft models of colorectal cancer harboring KRAS G12C, PIK3CA H1047R, and TP53 R248W (PMID: 26272063). 26272063
KRAS G13D PIK3CA H1047R colon cancer sensitive CC-223 Preclinical Actionable In a preclinical study, CC-223 inhibited proliferation of HCT-116 colon cancer cells, which have been reported to harbor KRAS G13D and PIK3CA H1047R mutations, in culture (PMID: 25855786, PMID: 24978597). 25855786 24978597
KRAS G13D PIK3CA H1047R colon cancer sensitive Irinotecan Preclinical Actionable In a preclinical study, Camptostar (irinotecan) suppressed the growth of a human colon cancer cell line harboring KRAS G13D and PIK3CA H1047R in xenograft models (PMID: 21325073, PMID: 16707468). 21325073 16707468
KRAS G13D PIK3CA H1047R colon cancer sensitive AT-7867 Preclinical Actionable In a preclinical study, AT-7867 inhibited proliferation of cultured HCT-116 colon cancer cells, which have been reported to harbor KRAS G13D and PIK3CA H1047R mutations (PMID: 20423992, PMID: 24978597). 24978597 20423992
KRAS G13D PIK3CA H1047R colon cancer sensitive Gedatolisib + Irinotecan Preclinical - Cell line xenograft Actionable In a preclinical study, Gedatolisib (PKI-587) and Camptostar (irinotecan) synergistically suppressed the growth of a human colon cancer cell line harboring KRAS G13D and PIK3CA H1047R (PMID: 24042735) in xenograft models (PMID: 21325073). 21325073 24042735
KRAS G13D PIK3CA H1047R colon cancer sensitive PD-0325901 + Gedatolisib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Gedatolisib (PF-05212384) and PD-0325901 inhibited tumor growth in colon cancer cell line xenograft models harboring KRAS G13D and PIK3CA H1047R (PMID: 21325073). 21325073
KRAS G13D PIK3CA H1047R colon cancer sensitive Gedatolisib + Camptothecin Preclinical Actionable In a preclinical study, Gedatolisib (PKI-587) and Camptothecin in combination synergistictically enhanced Parp cleavage in a human colon cancer cell line harboring KRAS G13D and PIK3CA H1047R in culture (PMID: 21325073, PMID: 24042735). 25688157 24042735
KRAS G13D PIK3CA H1047R colorectal cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) decreased viability of a colorectal cancer cell line harboring KRAS G13D and PIK3CA H1047R in culture (PMID: 27602501). 27602501
KRAS G13D PIK3CA H1047R colorectal cancer resistant Regorafenib Preclinical Actionable In a preclinical study, human colorectal cancer cells harboring KRAS G13D and PIK3CA H1047R were resistant to Stivarga (regorafenib) in culture (PMID: 25838391). 25838391
KRAS G13D PIK3CA H1047R colon cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited tumor growth in xenograft models of a human colon cancer cell line harboring KRAS G13D and PIK3CA H1047R mutations (PMID: 21558396). 21558396
KRAS G13D PIK3CA H1047R colon cancer sensitive CUDC-907 Preclinical Actionable In a preclinical study, CUDC-907 induced caspase activation in a human colon cancer cell line harboring KRAS G13D and PIK3CA H1047R in culture (PMID: 20570890, PMID: 22693356). 20570890 22693356
KRAS G13D PIK3CA H1047R colon cancer sensitive Gedatolisib Preclinical Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human colon cancer cells harboring KRAS G13D and PIK3CA H1047R in culture (PMID: 21325073, PMID: 24042735). 21325073 24042735
KRAS G13D PIK3CA H1047R colorectal cancer sensitive Regorafenib + Cetuximab Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Erbitux (cetuximab) and Stivarga (regorafenib) inhibited growth, reduced Akt and Mapk phosphorylation, and induced apoptosis of human colorectal cancer cell lines harboring KRAS G13D and PIK3CA H1047R in culture, and reduced tumor growth in cell line xenograft models (PMID: 25838391). 25838391
PIK3CA H1047R PTEN E307K breast cancer sensitive BAY1125976 Preclinical - Cell culture Actionable In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA H1047R and PTEN E307K in culture (PMID: 27699769). 27699769
KRAS mutant PIK3CA H1047R colon cancer sensitive BKM120 + Cetuximab Preclinical Actionable In a preclinical study, Buparlisib (BKM120) worked synergistically with Erbitux (cetuximab) to inhibit proliferation of colon cancer cell lines harboring mutant KRAS and PIK3CA H1047R in culture (PMID: 26715098). 26715098
KRAS mutant PIK3CA H1047R colon cancer no benefit Cetuximab Preclinical Actionable In a preclinical study, Erbitux (cetuximab) did not inhibit proliferation of colon cancer cell lines harboring mutant KRAS and PIK3CA H1047R in culture (PMID: 26715098). 26715098
KRAS mutant PIK3CA H1047R colon cancer sensitive Buparlisib Preclinical Actionable In a preclinical study, Buparlisib (BKM120) inhibited proliferation of colon cancer cell lines harboring mutant KRAS and PIK3CA H1047R in culture (PMID: 26715098). 26715098
BRAF V600X PIK3CA H1047R PTEN Y86fs melanoma resistant Vemurafenib Clinical Study Actionable In a clinical study, a melanoma patient harboring PTEN Y86fs and BRAF V600X developed the resistance mutation, PIK3CA H1047R, after treatment with Zelboraf (vemurafenib) (PMID: 24265153). 24265153
KRAS G12F PIK3CA H1047R lung adenocarcinoma sensitive Dasatinib + Demcizumab Preclinical - Pdx Actionable In a preclinical study, combination of Sprycel (dasatinib) and Demcizumab (OMP-21M18) treatment resulted in durable tumor inhibition in patient-derived animal models of lung adenocarcinoma harboring KRAS G12F and PIK3CA H1047R (PMID: 26855149). 26855149
KRAS G12D PIK3CA H1047R TP53 wild-type colorectal cancer no benefit Selumetinib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) and BEZ235 combination treatment did not improve tumor growth stabilization compared to single agent in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12D and PIK3CA H1047R (PMID: 26272063). 26272063
KRAS G12D PIK3CA H1047R TP53 wild-type colorectal cancer predicted - sensitive BEZ235 Preclinical - Pdx Actionable In a preclinical study, BEZ235 inhibited tumor growth in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12D and PIK3CA H1047R (PMID: 26272063). 26272063
KRAS G12D PIK3CA H1047R TP53 wild-type colorectal cancer decreased response Selumetinib Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) delayed tumor growth in patient-derived xenograft models of TP53 wild-type colorectal cancer harboring KRAS G12D and PIK3CA H1047R (PMID: 26272063). 26272063
PIK3CA H1047R breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R breast cancer sensitive Taselisib Phase I Actionable In a Phase I trial, four patients with breast cancer harboring PIK3CA H1047R demonstrated a confirmed partial response when treated with Taselisib (GDC-0032) (PMID: 28331003). 28331003
PIK3CA H1047R ovarian cancer sensitive A66 Preclinical - Cell line xenograft Actionable In a preclinical study, A66 delayed tumor growth in an ovarian cancer cell line xenograft model harboring PIK3CA H1047R (PMID: 21668414). 21668414
PIK3CA H1047R breast cancer sensitive ARQ092 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R demonstrated sensitivity to treatment with ARQ092 in culture, resulting in inhibition of cell proliferation (PMID: 26469692). 26469692
PIK3CA H1047R colorectal cancer sensitive Metformin Preclinical - Cell line xenograft Actionable In a preclinical study, Glucophage (metformin) demonstrated efficacy in treating dietary restriction-resistant human colorectal cancer cell line xenograft tumors harboring PIK3CA H1047R (PMID: 23986086). 23986086
PIK3CA H1047R breast cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R demonstrated sensitivity to treatment with ARQ 751 in culture, resulting in inhibition of cell proliferation (PMID: 26469692). 26469692
PIK3CA H1047R stomach cancer sensitive Capivasertib Preclinical - Pdx Actionable In a preclinical study, AZD5363 inhibited growth in a patient-derived xenograft model of gastric cancer harboring a PIK3CA H1047R mutation (PMID: 24088382). 24088382
PIK3CA H1047R head and neck squamous cell carcinoma sensitive Gedatolisib Preclinical - Cell culture Actionable In a preclinical study, head and neck squamous cell carcinoma cell lines harboring PIK3CA H1047R demonstrated sensitivity to treatment with Gedatolisib (PF-05212384) in culture (PMID: 25977343). 25977343
PIK3CA H1047R breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21558396). 21558396
PIK3CA H1047R lung cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 reduced tumor size in mouse models of lung cancer carrying PIK3CA H1047R (PMID: 19029981). 19029981
PIK3CA H1047R colorectal cancer resistant Fluorouracil + Cetuximab Preclinical - Cell culture Actionable In a preclinical study, colorectal cancer cells over expressing PIK3CA H1047R were resistant to Erbitux (cetuximab) and Fluorouracil combination treatment in culture (PMID: 28424201). 28424201
PIK3CA H1047R lung adenocarcinoma sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 promoted tumor regression in a mouse lung adenocarcinoma model expressing PIK3CA H1047R (PMID: 19029981). 19029981
PIK3CA H1047R head and neck squamous cell carcinoma sensitive Radiotherapy + Taselisib Preclinical Actionable In a preclinical study, Taselisib (GDC-0032) enhanced the effects of radiation induced apoptosis of head and neck squamous carcinoma cells harboring PIK3CA H1047R (PMID: 26589432). 26589432
PIK3CA H1047R lung adenocarcinoma no benefit Sirolimus Preclinical Actionable In a preclinical study, Sirolimus (rapamycin) failed to inhibit tumor growth in a mouse lung adenocarcinoma model expressing the PIK3CA H1047R mutation (PMID: 19029981). 19029981
PIK3CA H1047R colorectal cancer sensitive Cetuximab Clinical Study Actionable In a retrospective study, Erbitux (cetuximab) combined with radiation therapy resulted in stable disease for 6 months in a colorectal carcinoma patient harboring a PIK3CA H1047R mutation (PMID: 25714871). 25714871
PIK3CA H1047R ovarian cancer sensitive CH5132799 Phase I Actionable In a Phase I trial, CH5132799 demonstrated safety and preliminary efficacy in patients with advanced solid tumors, including a partial response in a patient with ovarian cancer harboring PIK3CA H1047R (PMID: 25231405). 25231405
PIK3CA H1047R breast cancer sensitive Buparlisib Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer cell line xenograft model harboring PIK3CA H1047R demonstrated tumor regression within the mammary fat pad when treated with Buparlisib (BKM120) (PMID: 28539475). 28539475
PIK3CA H1047R Advanced Solid Tumor sensitive Sirolimus Preclinical Actionable In a preclinical study, transformed cells expressing PIK3CA H1047R were sensitive to Rapamune (sirolimus), resulting in inhibition of transformation in culture (PMID: 15647370). 15647370
PIK3CA H1047R breast cancer sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R Advanced Solid Tumor sensitive A66 Preclinical Actionable In a preclinical study, A66 delayed tumor growth in human tumor xenograft models harboring PIK3CA H1047R mutations (PMID: 21668414). 21668414
PIK3CA H1047R breast cancer sensitive Alpelisib Preclinical Actionable In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R thyroid cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 inhibited AKT activation, proliferation, and growth of thyroid cancer cell lines with PI3K/AKT pathway alterations in culture, including an anaplastic thyroid cancer cell line harboring PIK3CA H1047R (PMID: 21289267). 21289267
PIK3CA H1047R breast cancer sensitive MSC2363318A Preclinical - Cell line xenograft Actionable In a preclinical study, a breast cancer xenograft model harboring PIK3CA H1047R was sensitive to M2698 (MSC2363318A), demonstrating inhibition of tumor growth (PMID: 27186432). 27186432
PIK3CA H1047R lung squamous cell carcinoma sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA H1047R in culture (PMID: 26013318). 26013318
PIK3CA H1047R ovarian cancer sensitive PF-04691502 Preclinical - Cell line xenograft Actionable In a preclinical study, PF-04691502 inhibited Pi3k signaling, resulted in growth inhibition of ovarian cancer cells harboring PIK3CA H1047R in culture and in cell line xenograft models (PMID: 21750219). 21750219
PIK3CA H1047R ovarian cancer sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited tumor growth in mouse xenografts of ovarian cancer with a Pik3ca H1047R mutation (AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2830). detail...
PIK3CA H1047R breast cancer sensitive DHM25 Preclinical - Cell culture Actionable In a preclinical study, DHM25 increased cell death in breast cancer cell lines harboring PIK3CA H1047R in culture (PMID: 26237138). 26237138
PIK3CA H1047R Advanced Solid Tumor sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R breast cancer sensitive Metformin Preclinical - Cell line xenograft Actionable In a preclinical study, Glucophage (metformin) inhibited cell proliferation of a dietary restriction-resistant PIK3CA H1047R-harboring human breast cancer cell line in culture, and inhibited tumor growth in xenograft models (PMID: 23986086). 23986086
PIK3CA H1047R thyroid cancer sensitive MK2206 + Temsirolimus Preclinical - Cell culture Actionable In a preclinical study, MK2206 and Torisel (temsirolimus) demonstrated synergy in inhibiting growth of an anaplastic thyroid cancer cell line harboring PIK3CA H1047R in culture (PMID: 21289267). 21289267
PIK3CA H1047R urinary bladder cancer sensitive Pictilisib Preclinical - Pdx Actionable In a preclinical study, Pictilisib (GDC-0941) inhibited Akt phosphorylation and tumor growth, prolonged survival in patient-derived xenograft (PDX) models of bladder cancer harboring PIK3CA H1047R (PMID: 28808038). 28808038
PIK3CA H1047R breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R lung squamous cell carcinoma sensitive BEZ235 Preclinical - Cell culture Actionable In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA H1047R in culture (PMID: 26013318). 26013318
PIK3CA H1047R lung cancer no benefit Sirolimus Preclinical Actionable In a preclinical study, Sirolimus (rapamycin) did not induce tumor shrinkage in mouse lung cancer models carrying PIK3CA H1047R (PMID: 19029981). 19029981
PIK3CA H1047R lung squamous cell carcinoma sensitive Buparlisib Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). 26013318
PIK3CA H1047R breast cancer sensitive Gedatolisib Preclinical Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21325073, PMID: 17314276). 17314276 21325073
PIK3CA H1047R breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). 26627007
PIK3CA H1047R urinary bladder cancer sensitive BEZ235 Preclinical - Pdx Actionable In a preclinical study, BEZ235 inhibited tumor growth in a patient-derived xenograft (PDX) model of bladder cancer harboring PIK3CA H1047R (PMID: 26270481). 26270481
PIK3CA H1047R breast cancer sensitive BAY1125976 Preclinical - Cell line xenograft Actionable In a preclinical study, BAY1125976 inhibited proliferation of breast cancer cell lines harboring PIK3CA H1047R in culture, and inhibited AKT signaling and tumor growth in a PIK3CA H1047R-mutant cell line xenograft model (PMID: 27699769). 27699769
PIK3CA H1047R head and neck squamous cell carcinoma sensitive Sirolimus + Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, Rapamune (sirolimus) worked synergistically with Mekinist (trametinib) to inhibit proliferation of head and neck squamous carcinoma cell lines harboring PIK3CA H1047R in culture and to reduce tumor growth in cell line xenograft models (PMID: 26882569). 26882569
PIK3CA H1047R urinary bladder cancer sensitive Cisplatin + Pictilisib Preclinical - Pdx Actionable In a preclinical study, combination of or sequential treatment with Pictilisib (GDC-0941) and Platinol (cisplatin) significantly delayed tumor growth and prolonged survival in patient-derived xenograft (PDX) models of bladder cancer harboring PIK3CA H1047R (PMID: 28808038). 28808038
PIK3CA H1047R Advanced Solid Tumor sensitive rigosertib Preclinical - Cell culture Actionable In a preclinical study, Estybon (rigosertib) inhibited oncogenic transformation in fibroblast cells over-expressing PIK3CA H1047R in culture (PMID: 27104980). 27104980
PIK3CA H1047R PTEN loss triple-receptor negative breast cancer predicted - sensitive ABT-737 + MLN0128 Preclinical - Cell line xenograft Actionable In a preclinical study, ABT-737 and Sapanisertib (MLN0128) combination treatment resulted in inhibition of tumor growth in cell line xenograft models of triple-receptor negative breast cancer harboring PIK3CA H1047R and PTEN loss (PMID: 27974663). 27974663
PIK3CA H1047R PTEN loss breast cancer predicted - sensitive BEZ235 + WEHI-539 Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 sensitized breast cancer cell lines harboring PIK3CA H1047R and PTEN loss to WEHI-539 in culture (PMID: 27974663). 27974663
PIK3CA H1047R PTEN loss breast cancer no benefit BEZ235 + Venetoclax Preclinical - Cell culture Actionable In a preclinical study, inhibition of Pi3k signaling by BEZ235 did not sensitize breast cancer cell lines harboring PIK3CA H1047R and PTEN loss to Venclexta (venetoclax) in culture (PMID: 27974663). 27974663
PIK3CA H1047R PTEN loss triple-receptor negative breast cancer predicted - sensitive ABT-737 + BEZ235 Preclinical - Cell line xenograft Actionable In a preclinical study, ABT-737 and BEZ235 combination treatment resulted in tumor regression in cell line xenograft models of triple-receptor negative breast cancer harboring PIK3CA H1047R and PTEN loss (PMID: 27974663). 27974663
KRAS G12D PIK3CA H1047R PTEN R130G endometrial cancer sensitive Selumetinib Preclinical - Pdx Actionable In a preclinical study, treatment with Selumetinib (AZD6244) slowed growth of tumors in patient-derived xenograft models of endometrial cancer harboring KRAS G12D, PIK3CA H1047R, PTEN R130G (PMID: 26232337). 26232337
KRAS G12D PIK3CA H1047R PTEN R130G endometrial cancer sensitive Selumetinib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, treatment with the combination of Selumetinib (AZD6244) and BEZ235 resulted in stable disease in patient-derived xenograft (PDX) models of endometrial cancer harboring KRAS G12D, PIK3CA H1047R, and PTEN R130G, and demonstrated improved efficacy over either agent alone (PMID: 26232337). 26232337
KRAS G12D PIK3CA H1047R PTEN R130G endometrial cancer sensitive BEZ235 Preclinical - Pdx Actionable In a preclinical study, treatment with BEZ235 slowed growth of tumors in patient-derived xenograft models of endometrial cancer harboring KRAS G12D, PIK3CA H1047R, PTEN R130G (PMID: 26232337). 26232337
ERBB2 over exp PIK3CA H1047R SRC over exp urinary bladder cancer no benefit Lapatinib Preclinical - Pdx Actionable In a preclinical study, treatment with Tykerb (lapatinib) was not effective in inhibiting tumor growth in a patient-derived xenograft (PDX) model of bladder cancer with ERBB2 (HER2) over expression, which also over expressed SRC and harbored PIK3CA H1047R (PMID: 26270481). 26270481
ERBB2 over exp PIK3CA H1047R SRC over exp urinary bladder cancer no benefit Ponatinib Preclinical - Pdx Actionable In a preclinical study, treatment with Iclusig (ponatinib) was not effective in inhibiting tumor growth in a patient-derived xenograft (PDX) model of bladder cancer with SRC over expression, which also over expressed ERBB2 (HER2) and harbored PIK3CA H1047R (PMID: 26270481). 26270481
BRAF V600E PIK3CA H1047R thyroid carcinoma resistant Trametinib + Dabrafenib Clinical Study Actionable In a clinical case study, a patient with anaplastic thyroid carcinoma co-harboring BRAF V600E and PIK3CA H1047R demonstrated resistance to the combination therapy, Mekinist (trametinib) and Tafinlar (dabrafenib) (PMID: 27797976). 27797976
BRAF V600E PIK3CA H1047R thyroid carcinoma sensitive Dabrafenib + Everolimus + Trametinib Clinical Study Actionable In a clinical case study, a patient with anaplastic thyroid carcinoma co-harboring BRAF V600E and PIK3CA H1047R demonstrated tumor regression when treated with the triple combination, Tafinlar (dabrafenib), Mekinist (trametinib), and Afinitor (everolimus) (PMID: 27797976). 27797976
BRAF V600E PIK3CA H1047R thyroid carcinoma resistant Everolimus Clinical Study Actionable In a clinical case study, a patient with anaplastic thyroid carcinoma co-harboring BRAF V600E and PIK3CA H1047R demonstrated resistance to treatment with Afinitor (everolimus) (PMID: 27797976). 27797976
AKT1 over exp PIK3CA H1047R breast cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Akt1 over expression in breast cancer cells harboring PIK3CA H1047R resulted in resistance to Alpelisib (BYL719) in culture (PMID: 27604488). 27604488
ERBB2 pos PIK3CA H1047R Her2-receptor positive breast cancer sensitive trastuzumab emtansine Preclinical - Cell line xenograft Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited survival of Herceptin (trastuzumab)-resistant ERBB2 (HER2) positive breast cancer cells harboring PIK3CA H1047R in culture, and induced tumor regression in cell line xenograft models (PMID: 26920887). 26920887
ERBB2 amp PIK3CA H1047R breast cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth and Akt phosphorylation, and promoted apoptosis in a human breast cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
ERBB2 amp PIK3CA H1047R breast cancer sensitive Gedatolisib Preclinical Actionable In a preclinical study, Gedatolisib (PKI-587) inhibited growth of human breast cancer cells harboring ERBB2 (HER2) amplification and PIK3CA H1047R in culture (PMID: 21325073, PMID: 17314276). 17314276 21325073
ERBB2 amp PIK3CA H1047R breast cancer sensitive CH5132799 + Trastuzumab Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of CH5132799 and Herceptin (trastuzumab) inhibited tumor growth and overcame Herceptin (trastuzumab) insensitivity in xenograft models of a human breast cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification (PMID: 21558396). 21558396
ERBB2 amp PIK3CA H1047R ovarian cancer sensitive CH5132799 Preclinical - Cell line xenograft Actionable In a preclinical study, CH5132799 inhibited cell growth in a human ovarian cancer cell line harboring PIK3CA H1047R and ERBB2 (HER2) amplification, and inhibited tumor growth in xenograft models (PMID: 21558396). 21558396
KRAS G12D PIK3CA H1047R TP53 R248W colorectal cancer resistant Selumetinib Preclinical - Pdx Actionable In a preclinical study, patient-derived xenograft models of colorectal cancer harboring KRAS G12D, PIK3CA H1047R, and TP53 R248W did not respond to Selumetinib (AZD6244) treatment (PMID: 26272063). 26272063
KRAS G12D PIK3CA H1047R TP53 R248W colorectal cancer no benefit Selumetinib + BEZ235 Preclinical - Pdx Actionable In a preclinical study, Selumetinib (AZD6244) and BEZ235 combination treatment did not improve tumor growth stabilization compared to single agent in patient-derived xenograft models of colorectal cancer harboring KRAS G12D, PIK3CA H1047R and TP53 R248W (PMID: 26272063). 26272063
KRAS G12D PIK3CA H1047R TP53 R248W colorectal cancer predicted - sensitive BEZ235 Preclinical - Pdx Actionable In a preclinical study, BEZ235 stabilized tumor growth of patient-derived xenograft models of colorectal cancer harboring KRAS G12D, PIK3CA H1047R, and TP53 R248W (PMID: 26272063). 26272063
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer resistant Trastuzumab + Lapatinib Preclinical Actionable In a preclinical study, a mouse breast cancer model with mammary ERBB2 (HER2) over-expression that also expressed the PIK3CA H1047R mutation showed resistance to the combination of Herceptin (trastuzumab) and Tykerb (lapatinib) (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer sensitive BKM120 + Trastuzumab Preclinical Actionable In a preclinical study, the combination of Herceptin (trastuzumab) and Buparlisib (BKM120) inhibited tumor growth in mouse ERBB2 (HER2)-over expressing breast cancer models expressing PIK3CA H1047R, with moderate efficacy over Buparlisib (BKM120) alone (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer no benefit BKM120 + Trastuzumab + Lapatinib Preclinical Actionable In a preclinical study, the combination of Buparlisib (BKM120), Herceptin (trastuzumab), and Tykerb (lapatinib) inhibited tumor growth in mouse models of ERBB2 (HER2)-over expressing breast cancer expressing PIK3CA H1047R, but efficacy was not significantly improved over Buparlisib (BKM120) alone (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer resistant Trastuzumab Preclinical Actionable In a preclinical study, mouse breast cancer models over expressing ERBB2 (HER2) and expressing PIK3CA H1047R were resistant to Herceptin (trastuzumab) (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer resistant Pertuzumab + Trastuzumab Preclinical Actionable In a preclinical study, a mouse breast cancer model with ERBB2 (HER2) over-expression that also expressed the PIK3CA H1047R mutation showed resistance to the combination of Heceptin (trastuzumab) and Perjeta (pertuzumab) (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer sensitive BKM120 + Trastuzumab + Pertuzumab Preclinical Actionable In a preclinical study, the combination of Buparlisib (BKM120), Herceptin (trastuzumab), and Perjeta (pertuzumab) inhibited tumor growth in mouse models of ERBB2 (HER2)-over expressing breast cancer expressing PIK3CA H1047R, with improved efficacy over Buparlisib (BKM120) alone (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R Her2-receptor positive breast cancer sensitive BKM120 + Bevacizumab Preclinical Actionable In a preclinical study, treatment with Buparlisib (BKM120) resulted in decreased tumor growth, but not tumor regression, in mouse models of ERBB2 (HER2)-over expressing breast cancer expressing PIK3CA H1047R (PMID: 23940356). 23940356
ERBB2 over exp PIK3CA H1047R stomach cancer predicted - resistant Trastuzumab Clinical Study Actionable In a clinical study (AMNESIA-1), assessment of pre-treatment tumor samples from ERBB2 (HER2)-positive gastric or gastroesophageal cancer patients (defined as HER2 IHC 3+ or HER2 IHC 2+/ISH+) identified PIK3CA mutations in 15% (3/20) of patients demonstrating primary resistance to Herceptin (trastuzumab), including 1 patient harboring PIK3CA H1047R (PMID: 29208673). 29208673
BRAF V600E PIK3CA H1047R TP53 wild-type colorectal cancer sensitive MLN0128 + PD-0325901 Preclinical - Cell culture Actionable In a preclinical study, Sapanisertib (MLN0128) and PD-0325901 synergistically inhibited Erk and PI3K signaling and proliferation, induced apoptosis in TP53-wild-type colorectal cancer cells harboring BRAF V600E and PIK3CA H1047R in culture (PMID: 26272063). 26272063
KRAS wild-type PIK3CA H1047R colorectal cancer no benefit Palbociclib + Trametinib Preclinical - Pdx Actionable In a preclinical study, Mekinist (trametinib) and Ibrance (palbociclib) combination treatment did not result in enhanced antitumor activity compared to Ibrance (palbociclib) alone in PDX models of KRAS wild-type colorectal cancer harboring PIK3CA H1047R (PMID: 26369631). 26369631
PIK3CA H1047R TP53 S90fs ovarian clear cell adenocarcinoma decreased response DS-7423 Preclinical - Cell culture Actionable In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring PIK3CA H1047R and TP53 S90fs*33 demonstrated reduced sensitivity to DS-7423 in culture (PMID: 24504419). 24504419
PIK3CA over exp lung squamous cell carcinoma sensitive Alpelisib Preclinical - Cell line xenograft Actionable In a preclinical study, Alpelisib (BYL719) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type PIK3CA in culture, and inhibited tumor growth in cell line xenograft models (PMID: 26013318). 26013318
PIK3CA over exp lung squamous cell carcinoma sensitive BEZ235 Preclinical - Cell culture Actionable In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). 26013318
PIK3CA over exp lung squamous cell carcinoma sensitive Buparlisib Preclinical - Cell culture Actionable In a preclinical study, Buparlisib (BKM120) induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). 26013318
PIK3CA over exp head and neck squamous cell carcinoma sensitive Gedatolisib Preclinical - Cell culture Actionable In a preclinical study, some head and neck squamous cell carcinoma cell lines over expressing PIK3CA demonstrated sensitivity to treatment with Gedatolisib (PF-05212384) (PMID: 25977343). 25977343
PIK3CA over exp glioblastoma multiforme sensitive YM-024 Preclinical Actionable In a preclinical study, YM-024 inhibited proliferation and anchorage-independent growth of glioblastoma cell lines with elevated Pik3ca protein level in culture (PMID: 24718026). 24718026
ERBB2 amp PIK3CA C420R breast cancer sensitive CH5132799 Preclinical Actionable In a preclinical study, CH5132799 inhibited proliferation of a breast cancer cell line harboring PIK3CA C420R and ERBB2 (HER2) amplification (PMID: 21558396). 21558396
ERBB2 pos PIK3CA C420R Her2-receptor positive breast cancer sensitive trastuzumab emtansine Preclinical - Cell culture Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited survival of ERBB2 (HER2) positive breast cancer cells harboring PIK3CA C420R in culture (PMID: 26920887). 26920887
PIK3CA C420R Advanced Solid Tumor sensitive Sirolimus Preclinical Actionable In a preclinical study, cells expressing PIK3CA C420R were sensitive to Rapamune (sirolimus) in culture (PMID: 17376864). 17376864
PIK3CA C420R ovarian clear cell adenocarcinoma sensitive DS-7423 Preclinical - Cell culture Actionable In a preclinical study, an ovarian clear cell adenocarcinoma cell line harboring PIK3CA C420R was sensitive to DS-7423 in culture, demonstrating inhibition of cell proliferation (PMID: 24504419). 24504419
ERBB2 pos PIK3CA I391M Her2-receptor positive breast cancer sensitive trastuzumab emtansine Preclinical - Cell culture Actionable In a preclinical study, Kadcyla (trastuzumab emtansine) inhibited survival of ERBB2 (HER2) positive breast cancer cells harboring PIK3CA K111N in culture (PMID: 26920887). 26920887
PIK3CA I391M uterine cancer sensitive Sirolimus Clinical Study Actionable In a clinical study, a uterine cancer patient harboring PIK3CA I391M demonstrated stable disease when treated with Rapamune (sirolimus) (PMID: 28514312). 28514312
KRAS G12D PIK3CA Q546L colorectal cancer sensitive Palbociclib + Trametinib Preclinical - Pdx Actionable In a preclinical study, Mekinist (trametinib) and Ibrance (palbociclib) combination treatment resulted in partial tumor regression in PDX models of colorectal cancer cells harboring KRAS G12D and PIK3CA Q546L (PMID: 26369631). 26369631
PIK3CA E542V colorectal cancer sensitive Cetuximab Clinical Study Actionable In a retrospective study, Erbitux (cetuximab) treatment resulted in stable disease in a colorectal carcinoma patient harboring a PIK3CA E542V mutation (PMID: 25714871). 25714871
ERBB2 over exp PIK3CA H1047L stomach cancer predicted - resistant Trastuzumab Clinical Study Actionable In a clinical study (AMNESIA-1), assessment of pre-treatment tumor samples from ERBB2 (HER2)-positive gastric or gastroesophageal cancer patients (defined as HER2 IHC 3+ or HER2 IHC 2+/ISH+) identified PIK3CA mutations in 15% (3/20) of patients demonstrating primary resistance to Herceptin (trastuzumab), including 1 patient harboring PIK3CA H1047L (PMID: 29208673). 29208673
PIK3CA H1047L breast cancer sensitive MK2206 Preclinical Actionable In a preclinical study, MK2206 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PIK3CA H1047L breast cancer sensitive Trametinib Preclinical Actionable In a preclinical study, Mekinist (trametinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PIK3CA H1047L breast cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PIK3CA H1047L breast cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Alpelisib (BYL719) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PIK3CA H1047L breast cancer sensitive Lapatinib Preclinical Actionable In a preclinical study, Tykerb (lapatinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PIK3CA H1047L breast cancer sensitive Neratinib Preclinical Actionable In a preclinical study, Nerlynx (neratinib) inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). 26627007
PIK3CA H1047X endometrial adenocarcinoma sensitive Temsirolimus Clinical Study Actionable In a clinical study, a patient with endometrial adenocarcinoma harboring a PIK3CA H1047 mutation demonstrated a partial response when treated with Torisel (temsirolimus) (PMID: 21216929). 21216929
PIK3CA H1047X colorectal cancer resistant Temsirolimus + Bevacizumab Clinical Study Actionable In a clinical study, a colorectal cancer patient harboring a mutation at PIK3CA H1047 demonstrated progressive disease when treated with Torisel (temsirolimus) and Avastin (bevacizumab) (PMID: 21216929). 21216929
PIK3CA H1047X non-small cell lung carcinoma sensitive Taselisib Phase I Actionable In a Phase I trial, a non-small cell lung carcinoma patient harboring a mutation at PIK3CA H1047 demonstrated a confirmed partial response when treated with Taselisib (GDC-0032) (PMID: 28331003). 28331003
PIK3CA H1047X small intestine adenocarcinoma resistant Bortezomib + Temsirolimus + Topotecan Clinical Study Actionable In a clinical study, the combination of Torisel (temsirolimus) plus Velcade (bortezomib) and Hycamtin (topotecan) resulted in progressive disease in a patient with small intestine adenocarcinoma harboring a PIK3CA H1047 mutation (PMID: 21216929). 21216929
PIK3CA H1047X BRAF V600X ovarian carcinoma sensitive Bevacizumab + Temsirolimus + Doxil Clinical Study Actionable In a clinical study, the combination of Torisel (temsirolimus) plus Avastin (bevacizumab) and Doxil (pegylated liposomal-doxorubicin) resulted in a partial response in a patient with ovarian clear cell carcinoma harboring PIK3CA H1047 and BRAF V600 mutations (PMID: 21216929). 21216929
PIK3CA H1047X KRAS G12X colorectal cancer resistant XL147 + Carboplatin + Paclitaxel Clinical Study Actionable In a clinical study, the combination of XL147 plus Paraplatin (carboplatin) and Taxol (paclitaxel) resulted in progressive disease in a patient with colorectal cancer harboring a PIK3CA H1047 mutation and KRAS G12 mutation (PMID: 21216929). 21216929
PIK3CA K944N colorectal cancer resistant Fluorouracil + Cetuximab Clinical Study Actionable In a clinical study, PIK3CA K944N was identified as a potential mechanism for acquired Erbitux (cetuximab) resistance in colorectal cancer patients, which is supported by cell culture studies demonstrating resistance to Erbitux (cetuximab) and Fluorouracil combination treatment in colorectal cancer cells over expressing PIK3CA K944N (PMID: 28424201). 28424201
ERBB2 A775_G776insYVMA PIK3CA R425L non-small cell lung carcinoma predicted - resistant Trastuzumab Clinical Study Actionable In a clinical study, the PIK3CA R425L mutation was identified as a potential resistance mechanism in a non-small cell lung carcinoma patient harboring ERBB2 (HER2) A775_G776insYVMA, that progressed during Herceptin (trastuzumab) treatment (PMID: 28167203). 28167203
PIK3CA E39K breast cancer resistant Buparlisib Preclinical - Cell culture Actionable In a preclinical study, breast cancer cells expressing PIK3CA E39K demonstrated resistance to treatment with Buparlisib (BKM120) in culture (PMID: 29636477). 29636477
KRAS G12V PIK3CA wild-type colorectal cancer sensitive Palbociclib + Trametinib Preclinical - Pdx Actionable In a preclinical study, Mekinist (trametinib) and Ibrance (palbociclib) combination treatment resulted in partial tumor regression in PDX models of PIK3CA wild-type colorectal cancer cells harboring KRAS G12V (PMID: 26369631). 26369631
BRAF mut PIK3CA wild-type colorectal cancer predicted - sensitive TAK-733 Preclinical - Pdx & cell culture Actionable In a preclinical study, mutations in BRAF, KRAS, or NRAS were associated with sensitivity to TAK-733 in colorectal cancer cell lines in culture, and patient-derived xenograft models harboring KRAS or BRAF mutations with wild-type PIK3CA demonstrated a trend toward higher tumor growth inhibition following TAK-733 treatment (PMID: 26439693). 26439693
BRAF V600E/K PIK3CA wild-type melanoma no benefit TGX-221 Preclinical Actionable In a preclinical study, TGX-221 did not inhibit proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture (PMID: 26137449). 26137449
BRAF V600E/K PIK3CA wild-type melanoma sensitive Selumetinib + BEZ235 Preclinical - Cell line xenograft Actionable In a preclinical study, Selumetinib (AZD6244) and BEZ235 combination treatment inhibited proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture, and synergitically inhibited tumor growth in cell line xenograft models (PMID: 26137449). 26137449
BRAF V600E/K PIK3CA wild-type melanoma sensitive Selumetinib + ZSTK474 Preclinical - Cell line xenograft Actionable In a preclinical study, Selumetinib (AZD6244) and ZSTK474 combination treatment inhibited proliferation of melanoma cell lines harboring BRAF V600E/K and wild-type PIK3CA in culture, and synergistically inhibited tumor growth in cell line xenograft models (PMID: 26137449). 26137449
BRAF V600E/K PIK3CA wild-type melanoma