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 | PI3K Inhibitor (Pan) 37 | 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 |
|---|---|---|---|---|---|---|---|
| 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 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 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 |
| Unknown unknown | islet cell tumor | not applicable | Pictilisib | Preclinical | Actionable | In a preclinical study, Pictilisib (GDC-0941) inhibited AKT activation, reduced tumor burden, and increased lifespan in a transgenic mouse model of pancreatic neuroendocrine tumor (PMID: 27225693). | 27225693 |
| 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 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status |
|---|---|---|---|---|
| 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 |
| NCT01437566 | Phase II | GDC-0980 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 |
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