Gene Variant Detail

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Gene PIK3CA
Variant H1047R
Impact List missense
Protein Effect gain of function
Gene Variant Descriptions PIK3CA H1047R is a hotspot mutation that lies within the kinase domain of the Pik3ca protein (UniProt.org). H1047R results in increased phosphorylation of Akt and Mek1/2, growth factor-independent cell survival, and transformation in cell culture (PMID: 26627007, PMID: 29533785).
Associated Drug Resistance
Category Variants Paths

PIK3CA mutant PIK3CA act mut PIK3CA H1047R

PIK3CA mutant PIK3CA exon21 PIK3CA H1047X PIK3CA H1047R

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Transcript NM_006218.4
gDNA chr3:g.179234297A>G
cDNA c.3140A>G
Protein p.H1047R
Source Database RefSeq
Genome Build GRCh38/hg38
Transcript gDNA cDNA Protein Source Database Genome Build
XM_011512894 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
XM_006713658 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
XM_011512894.2 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
NM_006218 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
XM_006713658.4 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
NM_006218.3 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
XM_006713658.5 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38
NM_006218.4 chr3:g.179234297A>G c.3140A>G p.H1047R RefSeq GRCh38/hg38

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA H1047R lung adenocarcinoma sensitive Dactolisib Preclinical Actionable In a preclinical study, BEZ235 promoted tumor regression in a mouse lung adenocarcinoma model expressing PIK3CA H1047R (PMID: 19029981). 19029981
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 lung cancer sensitive Dactolisib Preclinical Actionable In a preclinical study, BEZ235 reduced tumor size in mouse models of lung cancer carrying PIK3CA H1047R (PMID: 19029981). 19029981
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 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 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 stomach cancer sensitive Capivasertib Preclinical - Pdx Actionable In a preclinical study, Truqap (capivasertib) inhibited growth in a patient-derived xenograft model of gastric cancer harboring a PIK3CA H1047R mutation (PMID: 24088382). 24088382
PIK3CA H1047R ovarian cancer predicted - sensitive MEN1611 Case Reports/Case Series Actionable In a Phase I trial, MEN1611 (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 MEN1611 Preclinical Actionable In a preclinical study, MEN1611 (CH5132799) inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 21558396). 21558396
PIK3CA H1047R breast cancer sensitive MEN1611 Preclinical - Cell culture Actionable In a preclinical study, MEN1611 (CH5132799) inhibited viability and induced degradation of p110alpha in breast cancer cell lines harboring PIK3CA H1047R in culture (PMID: 36913051). 36913051
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 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 colorectal cancer sensitive Cetuximab Case Reports/Case Series Actionable In a retrospective analysis, 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 breast cancer sensitive Dactolisib 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 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 breast cancer sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Piqray (alpelisib) inhibited growth of breast cancer organoids harboring PIK3CA H1047R in culture (PMID: 37272756). 37272756
PIK3CA H1047R breast cancer sensitive MK2206 Preclinical - Cell culture 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 MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
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 breast cancer sensitive Neratinib Preclinical - Cell culture Actionable In a preclinical study, Nerlynx (neratinib) inhibited growth of breast cancer organoids harboring PIK3CA H1047R in culture (PMID: 37272756). 37272756
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 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 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 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 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 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 urinary bladder cancer sensitive Dactolisib 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 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 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 expressing PIK3CA H1047R in culture (PMID: 26013318). 26013318
PIK3CA H1047R lung squamous cell carcinoma sensitive Dactolisib 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 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 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 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 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 Advanced Solid Tumor sensitive Rigosertib Sodium Preclinical - Cell culture Actionable In a preclinical study, Rigosertib (ON 01910.Na) inhibited oncogenic transformation in fibroblast cells over-expressing Pik3ca H1047R in culture (PMID: 27104980). 27104980
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 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 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 Miransertib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R demonstrated sensitivity to treatment with Miransertib (ARQ092) in culture, resulting in inhibition of cell proliferation (PMID: 26469692). 26469692
PIK3CA H1047R breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
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 breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
PIK3CA H1047R breast cancer sensitive M2698 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 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 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 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 colorectal cancer resistant Cetuximab + Fluorouracil 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 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 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 breast metaplastic carcinoma predicted - sensitive Buparlisib + Paclitaxel Case Reports/Case Series Actionable In a clinical case study, Buparlisib (BKM120) in combination with Taxol (paclitaxel) resulted in a durable partial response in a patient with breast metaplastic carcinoma harboring PIK3CA H1047R, with a total response period of 70 weeks and an overall survival of 42 months (PMID: 30577988). 30577988
PIK3CA H1047R lung squamous cell carcinoma no benefit Taselisib Case Reports/Case Series Actionable In a Phase I (SWOG S1400B) trial, Taselisib (GDC-0032) treatment did not meet primary endpoint in patients with lung squamous cell carcinoma harboring PIK3CA mutations, resulting in no responses in patients harboring PIK3CA H1047R (n=4) (PMID: 31158500; NCT02785913). 31158500
PIK3CA H1047R estrogen-receptor positive breast cancer predicted - sensitive Everolimus Clinical Study - Cohort Actionable In a retrospective analysis, combination of Afinitor (everolimus) and hormone therapy resulted in improved median progression-free survival (8.8 vs 4.1 months, p=0.02) in patients with hormone receptor-positive metastatic breast cancer harboring PIK3CA H1047R (n=6) compared to patients without PIK3CA H1047R (n=10) (PMID: 31088410). 31088410
PIK3CA H1047R progesterone-receptor positive breast cancer predicted - sensitive Everolimus Clinical Study - Cohort Actionable In a retrospective analysis, combination of Afinitor (everolimus) and hormone therapy resulted in improved median progression-free survival (8.8 vs 4.1 months, p=0.02) in patients with hormone receptor-positive metastatic breast cancer harboring PIK3CA H1047R (n=6) compared to patients without PIK3CA H1047R (n=10) (PMID: 31088410). 31088410
PIK3CA H1047R head and neck squamous cell carcinoma predicted - sensitive SHR-A1307 Preclinical - Cell culture Actionable In a preclinical study, head and neck squamous cell carcinoma cells harboring PIK3CA H1047R treated with SHR-A1307 demonstrated inhibition of cell growth in culture (PMID: 30962319). 30962319
PIK3CA H1047R head and neck squamous cell carcinoma resistant Cetuximab Preclinical - Cell culture Actionable In a preclinical study, head and neck squamous cell carcinoma cells harboring PIK3CA H1047R were resistant to Erbitux (cetuximab) in culture (PMID: 30962319). 30962319
PIK3CA H1047R Advanced Solid Tumor predicted - sensitive Alpelisib Preclinical - Cell culture Actionable In a preclinical study, Piqray (Alpelisib) decreased Akt phosphorylation and inhibited PI3K signaling, and demonstrated dose-dependent inhibition of survival in human pluripotent stem cells harboring PIK3CA H1047R in culture (PMID: 30948643). 30948643
PIK3CA H1047R breast cancer sensitive CYH33 Preclinical - Cell line xenograft Actionable In a preclinical study, CYH33 inhibited proliferation of breast cancer cell lines harboring PIK3CA H1047R in culture, inhibited tumor progression in a transgenic mouse model, and induced cell cycle arrest, and inhibited PI3K signaling and tumor growth in cell line xenograft models (PMID: 30003928). 30003928
PIK3CA H1047R Her2-receptor negative breast cancer no benefit Everolimus Phase III Actionable In a retrospective analysis of a Phase III trial (BOLERO-2), Afinitor (everolimus) demonstrated comparable progression-free survival benefit in patients with hormone receptor-positive, Erbb2 (Her2)-negative breast cancer harboring wild-type (HR=0.43) or mutant (HR=0.37) PIK3CA, similar benefit was observed in subgroups harboring PIK3CA H1047R (HR=0.37) and PIK3CA E545K/E542K (HR=0.30) (PMID: 28183140; NCT00863655). 28183140
PIK3CA H1047R breast cancer sensitive Borussertib Preclinical - Cell culture Actionable In a preclinical study, borussertib inhibited proliferation of a breast cancer cell line harboring PIK3CA H1047R in culture (PMID: 30858154). 30858154
PIK3CA H1047R high grade glioma sensitive Buparlisib + Selumetinib Preclinical - Cell culture Actionable In a preclinical study, the combination therapy of Buparlisib (BKM120) and Koselugo (selumetinib) led to a synergistic effect, resulting in growth inhibition of astrocytoma cells expressing PIK3CA H1047R, but did not result in an effect as high as that seen in cells expressing PIK3CA R88Q or PIK3CA E542K in culture (PMID: 29975751). 29975751
PIK3CA H1047R head and neck squamous cell carcinoma predicted - sensitive Sulindac Preclinical - Cell culture Actionable In a preclinical study, head and neck squamous cell carcinoma cell lines harboring PIK3CA H1047R demonstrated increased sensitivity to Clinoril (sulindac) compared to cell lines with wild-type PIK3CA, resulting in decreased proliferation in culture (PMID: 30683736). 30683736
PIK3CA H1047R oral squamous cell carcinoma resistant Palbociclib Preclinical - Cell culture Actionable In a preclinical study, oral squamous cell carcinoma cells expressing PIK3CA H1047R demonstrated resistance to Ibrance (palbociclib) treatment in culture (PMID: 31516747). 31516747
PIK3CA H1047R oral squamous cell carcinoma decreased response Ribociclib Preclinical - Cell culture Actionable In a preclinical study, oral squamous cell carcinoma cells expressing PIK3CA H1047R demonstrated reduced sensitivity to Kisqali (ribociclib) treatment compared to cells expressing wild-type PIK3CA in culture (PMID: 31516747). 31516747
PIK3CA H1047R oral squamous cell carcinoma decreased response Abemaciclib Preclinical - Cell culture Actionable In a preclinical study, oral squamous cell carcinoma cells expressing PIK3CA H1047R demonstrated reduced sensitivity to Verzenio (abemaciclib) treatment compared to cells expressing wild-type PIK3CA in culture (PMID: 31516747). 31516747
PIK3CA H1047R transitional cell carcinoma no benefit Buparlisib Case Reports/Case Series Actionable In a Phase II trial, Buparlisib (BKM120) treatment resulted in progressive disease in a patient with metastatic urothelial carcinoma harboring PIK3CA H1047R (PMID: 32767682; NCT01551030). 32767682
PIK3CA H1047R colon cancer sensitive T-2143 Preclinical - Cell line xenograft Actionable In a preclinical study, T-2143 treatment inhibited Akt phosphorylation and proliferation of colon cancer cells harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 32499300). 32499300
PIK3CA H1047R breast cancer predicted - sensitive TAS-117 Case Reports/Case Series Actionable In a Phase II trial, TAS-117 treatment in a breast cancer patient harboring PIK3CA H1047R led to initial stable disease, however, disease progression was observed at 12 weeks after treatment along with an increase of non-target lesions, following which treatment was discontinued (PMID: 33723724; NCT03017521). 33723724
PIK3CA H1047R breast cancer predicted - sensitive GSK690693 Preclinical - Cell culture Actionable In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
PIK3CA H1047R breast cancer predicted - sensitive Ipatasertib Preclinical - Cell culture Actionable In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of breast cancer cells harboring PIK3CA H1047R in culture (PMID: 32439931). 32439931
PIK3CA H1047R colon cancer sensitive Taselisib Preclinical - Cell culture Actionable In a preclinical study, Taselisib (GDC-0032) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). 34544753
PIK3CA H1047R colon cancer no benefit Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) treatment did not affect cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). 34544753
PIK3CA H1047R colon cancer sensitive Inavolisib Preclinical - Cell culture Actionable In a preclinical study, Inavolisib (GDC-0077) treatment led to decreased cell viability in a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 34544753). 34544753
PIK3CA H1047R breast cancer predicted - sensitive LOXO-783 Preclinical - Pdx & cell culture Actionable In a preclinical study, LOXO-783 (LOX-22783) treatment led to growth inhibition in breast cancer cell lines harboring PIK3CA H1047R, and led to tumor regression in cell line xenograft and patient-derived xenograft (PDX) models (Mol Cancer Ther 2021;20(12 Suppl):Abstract nr P142). detail...
PIK3CA H1047R colon cancer sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Koselugo (selumetinib) inhibited viability of a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 27636997). 27636997
PIK3CA H1047R colon cancer sensitive Pimasertib Preclinical - Cell culture Actionable In a preclinical study, Pimasertib (MSC1936369B) inhibited viability of a colon cancer cell line expressing PIK3CA H1047R in culture (PMID: 27636997). 27636997
PIK3CA H1047R endometrial cancer predicted - sensitive Alpelisib Case Reports/Case Series Actionable In a clinical case study, Piqray (alpelisib) resulted in a partial response after 4 months in a patient with endometrial endometrioid cancer harboring PIK3CA H1047R, with treatment ongoing at 7 months (PMID: 36713525). 36713525
PIK3CA H1047R estrogen-receptor positive breast cancer predicted - sensitive Alpelisib + Everolimus Preclinical - Patient cell culture Actionable In a preclinical study, combination treatment with Piqray (albelisib) and Afinitor (everolimus) synergistically inhibited cell viability of patient-derived ESR1 (ER)-positive breast cancer cells harboring PIK3CA H1047R and ESR1 (ER alpha) Y537S in culture (PMID: 36900375). 36900375
PIK3CA H1047R estrogen-receptor positive breast cancer predicted - sensitive Afatinib + Alpelisib Preclinical - Patient cell culture Actionable In a preclinical study, combination treatment with Piqray (albelisib) and Gilotrif (afatinib) synergistically inhibited cell viability of patient-derived ESR1 (ER)-positive breast cancer cells harboring PIK3CA H1047R and ESR1 (ER alpha) Y537S in culture (PMID: 36900375). 36900375
PIK3CA H1047R ovarian cancer predicted - sensitive Temsirolimus Case Reports/Case Series Actionable In a Phase II trial (TAPUR), Torisel (temsirolimus) treatment resulted in a partial response ongoing at 86 weeks in a patient with ovarian cancer harboring PIK3CA H1047R (J Clin Oncol 41, 2023 (suppl 16; abstr 3117); NCT02693535). detail...
PIK3CA H1047R bone ameloblastoma predicted - sensitive Copanlisib Case Reports/Case Series Actionable In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in a partial response and progression-free survival of 24.6 months and an overall survival of 25.8 months in a patient with ameloblastoma of the mandible harboring PIK3CA H1047R (PMID: 35133871; NCT02465060). 35133871
PIK3CA H1047R myxoid liposarcoma predicted - sensitive Copanlisib Case Reports/Case Series Actionable In a Phase II trial (NCI MATCH EAY131-Z1F), Aliqopa (copanlisib) treatment resulted in a partial response and progression-free survival of 23.7 months and an overall survival of 25.8 months in a patient with myxoid liposarcoma harboring PIK3CA H1047R (PMID: 35133871; NCT02465060). 35133871
PIK3CA H1047R head and neck squamous cell carcinoma sensitive Alpelisib + Tipifarnib Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of Piqray (alpelisib) and Zarnestra (tipifarnib) inhibited Mtor and Rsk phosphorylation, induced cell cycle arrest and apoptosis, and synergistically inhibited viability of head and neck cancer squamous cell carcinoma cell lines harboring PIK3CA H1047R in culture and inhibited Mtor signaling, induced cell cycle arrest and apoptosis, inhibited proliferation, and induced tumor regression in a cell line xenograft model (PMID: 37339176). 37339176
PIK3CA H1047R colorectal cancer resistant Alpelisib Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring PIK3CA H1047R was resistant to Piqray (alpelisib) in culture (PMID: 37493631). 37493631
PIK3CA H1047R head and neck squamous cell carcinoma sensitive STX-478 Preclinical - Cell line xenograft Actionable In a preclinical study, STX-478 inhibited viability in head and neck squamous cell cancer cell lines harboring PIK3CA H1047R in culture, and inhibited tumor growth and induced tumor regression in a cell line xenograft model (PMID: 37623743). 37623743
PIK3CA H1047R Her2-receptor positive breast cancer sensitive STX-478 Preclinical - Cell line xenograft Actionable In a preclinical study, STX-478 inhibited viability in a hormone receptor-negative, ERBB2 (HER2)-positive breast cancer cell line harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37623743). 37623743
PIK3CA H1047R Her2-receptor negative breast cancer sensitive STX-478 Preclinical - Pdx & cell culture Actionable In a preclinical study, STX-478 inhibited viability in an ESR1-positive, ERBB2 (HER2)-negative breast cancer cell line harboring PIK3CA H1047R in culture and inhibited tumor growth and induced tumor regression with high-dose STX-478 in a cell line xenograft model and inhibited tumor growth in a patient-derived xenograft (PDX) model (PMID: 37623743). 37623743
PIK3CA H1047R Her2-receptor negative breast cancer predicted - sensitive HS-10352 Case Reports/Case Series Actionable In a Phase I trial, HS-10352 treatment resulted in an objective response rate (ORR) of 27.8% (5/18, all partial responses), disease control rate (DCR) of 55.6%, and median progression-free survival (mPFS) of 3.9 mo in HR-positive, ERBB2 (HER2)-negative advanced breast cancer patients overall, and in the 6mg group led to an ORR of 66.7% and DCR of 83.3%, with an ORR of 75.0% (3/4) and DCR of 100% in patients with PIK3CA mutations (E542K, E545K, E545D, H1047L, H1047R) (PMID: 38037839; NCT04631835). 38037839
PIK3CA H1047R breast cancer sensitive RLY-2608 Preclinical - Cell line xenograft Actionable In a preclinical study, RLY-2608 inhibited viability of hormone receptor-positive breast cancer cells harboring PIK3CA H1047R in culture, and inhibited tumor growth in a cell line xenograft model (PMID: 37916956). 37916956
PIK3CA H1047R Advanced Solid Tumor predicted - sensitive OKI-219 Preclinical - Pdx Actionable In a preclinical study, OKI-219 decreased Akt phosphorylation and proliferation in tumor cell lines harboring PIK3CA H1047R in culture and inhibited tumor growth in cell line xenograft models and patient-derived xenograft (PDX) models (Mol Cancer Ther (2023) 22 (12_Supplement): B163). detail...