Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : ckbsupport@jax.org
Therapy Name | Gedatolisib |
Synonyms | |
Therapy Description |
Gedatolisib (PF-05212384) is an ATP-competitive inhibitor that targets phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, and may result in antitumor activity, including inhibition of tumor growth and tumor regression (PMID: 21325073). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Gedatolisib | PKI-587|PF-05212384|PF 05212384 | mTOR Inhibitor 51 PI3K Inhibitor (Pan) 38 | Gedatolisib (PF-05212384) is an ATP-competitive inhibitor that targets phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, and may result in antitumor activity, including inhibition of tumor growth and tumor regression (PMID: 21325073, PMID: 31822716). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
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 |
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 |
Unknown unknown | head and neck squamous cell carcinoma | not applicable | Gedatolisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gedatolisib (PF-05212384) increased the the sensitivity of head and neck squamous cancer cells to radiation as indicated by decreased downstream signaling of the PI3K/mTOR pathway and reduced growth both in culture and in cell line xenograft models (PMID: 25724523). | 25724523 |
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 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 | 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 |
Unknown unknown | Advanced Solid Tumor | not applicable | Gedatolisib | Phase I | Actionable | In a Phase I trial, Gedatolisib (PF-05212384) demonstrated safety and efficacy, which resulted in antitumor activity and stable disease greater than six months in 10.4% (8/27) of patients with solid malignant tumors (PMID: 25652454). | 25652454 |
Unknown unknown | breast cancer | not applicable | Gedatolisib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Gedatolisib (PF-05212384) suppressed phosphorylation of PI3K/mTOR effectors and induced apoptosis in human breast cancer cell lines with elevated PI3K/mTOR signaling in culture and in cell line xenograft models (PMID: 21325073). | 21325073 |
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 |
BRAF V600E | colon cancer | sensitive | Gedatolisib | Preclinical | Actionable | In a preclinical study, Gedatolisib (PKI-587) inhibited Braf V600E in vitro and inhibited growth of human colon cancer cells harboring BRAF V600E in culture (PMID: 21325073, PMID: 24042735). | 24042735 21325073 |
STK11 mutant | lung non-small cell carcinoma | sensitive | Gedatolisib | Preclinical | Actionable | In a preclinical study, Gedatolisib (PF-05212384) inhibited growth of human non-small cell lung carcinoma cells harboring an STK11 mutation in culture (PMID: 21325073). | 21325073 |
NRAS Q61K | lung non-small cell carcinoma | decreased response | Gedatolisib | Preclinical | Actionable | In a preclinical study, human non-small cell lung cancer cells harboring NRAS Q61K had a decreased response to Gedatolisib (PKI-587) in culture (PMID: 21325073, PMID: 12068308). | 21325073 12068308 |
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 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01937715 | Phase II | Bevacizumab Gedatolisib Fluorouracil + Irinotecan + Leucovorin | A Study Of PF-05212384 Plus FOLFIRI Versus Bevacizumab Plus FOLFIRI In Metastatic Colorectal Cancer | Terminated | USA | CAN | 1 |
NCT01347866 | Phase I | Gedatolisib PD-0325901 Irinotecan | Clinical Study Of PI3K/mTOR Inhibitors In Combination With An Oral MEK Inhibitor Or Irinotecan In Patients With Advanced Cancer | Terminated | USA | CAN | 2 |
NCT02626507 | Phase I | Palbociclib Gedatolisib Goserelin Fulvestrant | Phase I Study of Combination of Gedatolisib With Palbociclib and Faslodex in Patients With ER+/HER2- Breast Cancer | Recruiting | USA | 0 |