Therapy Detail

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Therapy Name Pictilisib
Synonyms
Therapy Description

Pictilisib (GDC-0941) inhibits isoforms of PI3K, which inhibits PI3K/AKT signaling resulting in antitumor activity, including inhibition of tumor growth (PMID: 19584227).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Pictilisib GDC-0941|GDC0941|GDC 0941 PI3K Inhibitor (Pan) 40 Pictilisib (GDC-0941) inhibits isoforms of PI3K, which inhibits PI3K/AKT signaling resulting in antitumor activity, including inhibition of tumor growth (PMID: 19584227).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PTEN loss STK11 loss endometrial cancer sensitive Pictilisib Preclinical Actionable In a preclinical study, the PI3K inhibitor GDC-0941 reduced tumor growth rate in immunodeficient mice engrafted with endometrial tumors from PTEN/STK11 (LKB1) deficient mice (PMID: 24322983). 24322983
PTEN loss RB1 loss triple-receptor negative breast cancer resistant Pictilisib Preclinical Actionable In a preclinical study, a triple-receptor negative breast cancer line harboring PTEN and RB1 loss was resistant to Pictilisib (GDC-0941) induced growth inhibition in culture (PMID: 27020857). 27020857
PIK3CA E726K PIK3CA H1047R breast cancer resistant Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA E726K was resistant to Pictilisib (GDC-0941) in culture (PMID: 37916958). 37916958
PTEN L152P PTEN neg salivary gland carcinoma sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) inhibited Akt phosphorylation and proliferation of salivary ductal carcinoma cells harboring PTEN L152P and loss of Pten protein expression in culture (PMID: 30289966). 30289966
PIK3CA E545K PIK3CA E726K breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA E726K in culture (PMID: 37916958). 37916958
PIK3CA E545K PIK3CA Q859H breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA Q859H in culture (PMID: 37916958). 37916958
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
FGFR2 amp stomach cancer no benefit Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a gastric cancer cell line harboring an FGFR2 amplification was not sensitive to Pictilisib (GDC-0941) treatment in culture (PMID: 30045926). 30045926
PTEN loss lung non-small cell carcinoma sensitive Pictilisib Preclinical - Cell line xenograft Actionable In preclinical studies, the PI3K inhibitor GDC-0941 demonstrated efficacy against NSCLC tumor cell lines in both culture and xenograft models harboring alterations in the PI3K pathway (PMID: 23136191). 23136191
PIK3CA Q859H PIK3CA H1047R breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859H in culture (PMID: 37916958). 37916958
PIK3CA act mut lung non-small cell 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
ARID1A dec exp urinary bladder cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) inhibited viability of bladder cancer cell lines with ARID1A knockdown in culture (PMID: 35852858). 35852858
BRAF mut PTEN inact mut melanoma sensitive Pictilisib Preclinical Actionable In a preclincal study, Pictilisib (GDC-0941) inhibited Akt activation and proliferation in melanoma cell lines harboring BRAF mutations and PTEN inactivating mutations in culture (PMID: 26577700). 26577700
ARID1A inact mut urinary bladder cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) inhibited viability of bladder cancer cell lines harboring ARID1A inactivating mutations in culture (PMID: 35852858). 35852858
PIK3CA E545K PIK3CA W780R breast cancer resistant Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA W780R was resistant to Pictilisib (GDC-0941) in culture (PMID: 37916958). 37916958
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 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 F977Y head and neck squamous cell carcinoma resistant Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a head and neck squamous cell carcinoma cell line harboring PIK3CA F977Y demonstrated resistance to growth inhibition by Pictilisib (GDC-0941) in culture (PMID: 30108165). 30108165
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 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 I817F PIK3CA H1047R breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA I817F in culture (PMID: 37916958). 37916958
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
PIK3CA E545K PIK3CA I817F breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA E545K and expressing PIK3CA I817F in culture (PMID: 37916958). 37916958
PTEN N48I 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 PTEN N48I in culture (PMID: 28808038). 28808038
PIK3CA Q859K PIK3CA H1047R breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) decreased viability of a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA Q859K in culture (PMID: 37916958). 37916958
PIK3CA W780R PIK3CA H1047R breast cancer resistant Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA H1047R and expressing PIK3CA W780R was resistant to Pictilisib (GDC-0941) in culture (PMID: 37916958). 37916958
PTEN inact mut estrogen-receptor positive breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a PTEN deficient estrogen-receptor (ER) positive breast cancer cell line demonstrated increased sensitivity to treatment in culture when Pictilisib (GDC-0941) was given at a higher dose for a shorter duration, resulting in inhibition of cell growth (PMID: 26733612). 26733612
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 E545K 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 E545K in culture (PMID: 34544753). 34544753
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

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT01493843 Phase II Carboplatin Pictilisib Bevacizumab Study Evaluating the Safety and Efficacy of Carboplatin/Paclitaxel and Carboplatin/Paclitaxel/Bevacizumab With and Without GDC-0941 in Patients With Previously Untreated Advanced or Recurrent Non-small Cell Lung Cancer Completed USA | ITA | GBR | FRA | ESP | DEU | CAN | AUS 8
NCT01437566 Phase II Apitolisib Fulvestrant Pictilisib Study of GDC-0941 or GDC-0980 With Fulvestrant Versus Fulvestrant in Advanced or Metastatic Breast Cancer in Patients Resistant to Aromatase Inhibitor Therapy Completed USA | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS 14


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