Therapy Detail

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Therapy Name Dactolisib
Synonyms
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
Dactolisib NVP-BEZ235|BEZ235 ATR Inhibitor 13 mTOR Inhibitor 51 PI3K Inhibitor (Pan) 39 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).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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 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
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
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 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 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 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 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 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 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 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
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
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
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 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 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 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
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
HRAS inact mut thyroid gland 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
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 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 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 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
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 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 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 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

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

Sorting

  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
  • Click on any column header arrows to sort by that column
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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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