Therapy Detail

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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).

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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).

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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

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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


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