Therapy Detail

Therapy Name BEZ235
Synonym
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 10 mTOR Inhibitor 49 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
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
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
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 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
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 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
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
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
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 lung non-small cell 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 endometrial cancer not applicable BEZ235 Preclinical Actionable In a preclinical study, BEZ235 suppressed tumor growth in endometrial xenografts (PMID: 22662154). 22662154
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
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
Clinical Trial Phase Therapies Title Recruitment Status