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) 42 | 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 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 |
| 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 |
| 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 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 |
| 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 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 |
| 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 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 |
| 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 |
| 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 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 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 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 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 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 |
| 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 |
| 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 |
| 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 |
| 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 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 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 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 |
| 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 |
| HRAS G13R PTEN loss | Advanced Solid Tumor | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, HRAS-null, NRAS-null, and KRAS knockout cells with PTEN loss and expressing HRAS G13R were not sensitive to treatment with Pictilisib (GDC-0941) in culture (PMID: 39152269). | 39152269 |
| 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 | 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 |
| HRAS G13R PIK3CA H1047R | Advanced Solid Tumor | resistant | Pictilisib | Preclinical - Cell culture | Actionable | In a preclinical study, HRAS-null, NRAS-null, and KRAS knockout cells expressing HRAS G13R and PIK3CA H1047R were resistant to Pictilisib (GDC-0941) in culture (PMID: 39152269). | 39152269 |
| 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 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 |
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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 | NLD | ITA | ISR | HUN | GBR | FRA | ESP | DEU | CAN | BRA | AUS | ARG | 3 |
| 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 | NZL | ITA | ISR | GBR | FRA | ESP | DNK | DEU | CAN | BEL | AUS | ARG | 10 |
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