Therapy Detail

Therapy Name BEZ235
Therapy Description

BEZ235 inhibits PI3K kinase, mTOR kinase, and ATR, which may result in tumor cell apoptosis and growth inhibition of tumor cells (PMID: 18606717, PMID: 21552262).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
BEZ235 NVP-BEZ235|Dactolisib ATR Inhibitor 9 mTOR Inhibitor 48 PI3K Inhibitor (Pan) 34 BEZ235 inhibits PI3K kinase, mTOR kinase, and ATR, which may result in tumor cell apoptosis and growth inhibition of tumor cells (PMID: 18606717, PMID: 21552262).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown endometrial cancer not applicable BEZ235 Preclinical Actionable In a preclinical study, BEZ235 suppressed tumor growth in endometrial xenografts (PMID: 22662154). 22662154
APC inact mut PTEN inact mut colorectal cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited PI3K/mTOR signaling in tumors and increased survival in transgenic animal models of colorectal cancer driven by APC and PTEN inactivation (PMID: 26206338). 26206338
KRAS mutant colorectal cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited growth of colorectal cancer cells harboring KRAS mutations in culture and in xenograft models (PMID: 23475782). 23475782
Unknown unknown leiomyosarcoma not applicable BEZ235 Preclinical Actionable In a preclinical study, leiomyosarcoma cells treated with BEZ235 in culture and in mouse models demonstrated increased levels of apoptosis and a 42% reduction in tumor volume (PMID: 26952093). 26952093
MET amp non-small cell lung carcinoma sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 suppressed the growth of an Iressa (gefitinib)-resistant NSCLC cell line with MET amplification (PMID: 24939055). 24939055
Unknown unknown peritoneal mesothelioma not applicable BEZ235 Preclinical Actionable In a preclinical study, BEZ235 treatment resulted in suppression of PI3K and mTOR signaling and growth inhibition in patient-derived malignant peritoneal mesothelioma cell lines in culture (PMID: 20839315). 20839315
KRAS G12D lung cancer no benefit BEZ235 Preclinical Actionable In a preclinical study, BEZ235 did not induce tumor shrinkage in mouse lung cancer models carrying KRAS G12D (PMID: 19029981). 19029981
PTEN mutant endometrial cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 decreased growth of endometrial cancer cells harboring a PTEN nonsense mutation in culture and in xenograft models (PMID: 22662154). 22662154
Unknown unknown pancreatic endocrine carcinoma no benefit BEZ235 Phase II Actionable In a Phase II clinical trial, BEZ235 was not well-tolerated and demonstrated modest anti-tumor activity in pancreatic neuroendocrine tumor patients who had progressed on Afinitor (everolimus), with a 51.6% (16/31) progression-free survival rate at 16 weeks (PMID: 26851029). 26851029
Unknown unknown prostate carcinoma not applicable BEZ235 Preclinical Actionable In a preclinical study, treatment with BEZ235 resulted in a decrease in prostate cancer progenitor cells in culture and reduced tumor growth in prostate carcinoma xenograft models (PMID: 21138868). 21138868
APC inact mut KRAS G12D PTEN inact mut colorectal cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited mTOR signaling in tumors and increased survival in transgenic animal models of colorectal cancer driven by APC and PTEN inactivation, and KRAS G12D (PMID: 26206338). 26206338
HRAS inact mut thyroid cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited growth of thyroid cancer cells harboring an HRAS pathway activating mutation in cell culture (PMID: 21831957). 21831957
PTEN loss head and neck squamous cell carcinoma predicted - sensitive BEZ235 Preclinical - Cell culture Actionable In a preclinical study, BEZ235 resulted in antiproliferative activity in head and neck squamous cell carcinoma cells harboring PTEN loss in culture (PMID: 28446642). 28446642
APC inact mut KRAS G12D colorectal cancer sensitive BEZ235 Preclinical Actionable In a preclinical study, BEZ235 inhibited PI3K/mTOR signaling in tumors and increased survival in transgenic animal models of colorectal cancer driven by APC inactivation and KRAS G12D (PMID: 26206338). 26206338
Clinical Trial Phase Therapies Title Recruitment Status