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Therapy Name | Dactolisib |
Synonyms | |
Therapy Description |
Dactolisib (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, PMID: 32088816). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Dactolisib | NVP-BEZ235|BEZ235 | ATR Inhibitor 16 mTOR Inhibitor 51 PI3K Inhibitor (Pan) 42 | Dactolisib (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, PMID: 32088816). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
BRAF L525R | Advanced Solid Tumor | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, Dactolisib (BEZ235) inhibited viability of cells expressing BRAF L525R in culture (PMID: 36856908). | 36856908 |
PIK3CA H1047R | lung squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA H1047R in culture (PMID: 26013318). | 26013318 |
PIK3CA R38C PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 decreased growth of endometrial cancer cells harboring PIK3CA R38C and PTEN mutations in culture and in xenograft models (PMID: 22662154). | 22662154 |
PIK3CA over exp | lung squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing wild-type Pik3ca in culture (PMID: 26013318). | 26013318 |
PTEN mutant | endometrial cancer | sensitive | Dactolisib | 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 |
PIK3CA G1049R | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA G1049R in culture (PMID: 26627007). | 26627007 |
PIK3CA act mut | ovarian clear cell adenocarcinoma | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 demonstrated efficacy in mouse xenograft models of ovarian clear cell adenocarcinoma with PIK3CA mutations (PMID: 24927217). | 24927217 |
PIK3CA E545K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E545K in culture (PMID: 26627007). | 26627007 |
APC inact mut PTEN inact mut | colorectal cancer | sensitive | Dactolisib | 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 |
PIK3CA E545K | colorectal cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 decreased cell proliferation in colorectal cancer cells harboring a PIK3CA E545K mutation in cell culture (PMID: 21966435). | 21966435 |
PIK3CA E542K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA E542K in culture (PMID: 26627007). | 26627007 |
PIK3CA mutant | stomach cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 demonstrated efficacy in promoting apoptosis of gastric cancer cells harboring a PIK3CA mutation in culture (PMID: 22543857). | 22543857 |
PIK3CA mutant | colon cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 demonstrated efficacy in promoting apoptosis of colon cancer cells harboring a PIK3CA mutation in culture (PMID: 22543857). | 22543857 |
PIK3CA H1047L | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047L in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | lung adenocarcinoma | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 promoted tumor regression in a mouse lung adenocarcinoma model expressing PIK3CA H1047R (PMID: 19029981). | 19029981 |
PIK3CA R88Q PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA R88Q and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA Q546K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA Q546K in culture (PMID: 26627007). | 26627007 |
PIK3CA amp | head and neck squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 resulted in antiproliferative activity in head and neck squamous cell carcinoma cells harboring PIK3CA amplification in culture (PMID: 28446642). | 28446642 |
PIK3CA H1047R | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA H1047R in culture (PMID: 26627007). | 26627007 |
PIK3CA E365K PTEN mut | endocervical carcinoma | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA E365K and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA R108H PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA R108H and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA H1047R | urinary bladder cancer | sensitive | Dactolisib | Preclinical - Pdx | Actionable | In a preclinical study, BEZ235 inhibited tumor growth in a patient-derived xenograft (PDX) model of bladder cancer harboring PIK3CA H1047R (PMID: 26270481). | 26270481 |
HRAS inact mut | thyroid cancer | sensitive | Dactolisib | 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 |
PIK3CA N345K | breast cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited survival of transformed breast epithelial cell lines overexpressing PIK3CA N345K in culture (PMID: 26627007). | 26627007 |
PIK3CA H1047R | lung cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 reduced tumor size in mouse models of lung cancer carrying PIK3CA H1047R (PMID: 19029981). | 19029981 |
PTEN loss | head and neck squamous cell carcinoma | predicted - sensitive | Dactolisib | 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 |
PIK3CA E365K PTEN mut | endometrial cancer | sensitive | Dactolisib | Preclinical | Actionable | In a preclinical study, BEZ235 inhibited proliferation of endometrial cancer cells harboring PIK3CA E365K and PTEN mutations in culture (PMID: 22662154). | 22662154 |
PIK3CA E545K | lung squamous cell carcinoma | sensitive | Dactolisib | Preclinical - Cell culture | Actionable | In a preclinical study, BEZ235 induced apoptosis, inhibited cell proliferation, migration, and invasion of lung squamous cell carcinoma cells over expressing PIK3CA E545K in culture (PMID: 26013318). | 26013318 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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