Therapy Detail

Therapy Name XL147
Synonym
Therapy Description

Pilaralisib (XL147) is an inhibitor of all class I PI3Ks, thereby blocking activation of the PI3K signaling pathway and potentially resulting in antitumor activity including inhibition of cell proliferation, cell invasion, and tumor growth (PMID: 25637314).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
XL147 SAR245408|Pilaralisib PI3K Inhibitor (Pan) 34 Pilaralisib (XL147) is an inhibitor of all class I PI3Ks, thereby blocking activation of the PI3K signaling pathway and potentially resulting in antitumor activity including inhibition of cell proliferation, cell invasion, and tumor growth (PMID: 25637314).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KRAS G12S STK11 inact mut non-small cell lung carcinoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited tumor growth in xenograft models of a human non-small cell lung cancer cell line harboring KRAS G12S and an STK11(LKB) inactivating mutation (PMID: 25637314). 25637314
BRAF V600E PTEN loss melanoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited tumor growth in xenograft models of a PTEN-deficient human melanoma cell line harboring BRAF V600E (PMID: 25637314). 25637314
BRAF V600D PTEN loss melanoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited tumor growth in xenograft models of a PTEN-deficient human melanoma cell line harboring BRAF V600D (PMID: 25637314). 25637314
ERBB2 T798M breast cancer sensitive XL147 Preclinical Actionable In a preclinical study, breast cancer cell lines expressing ERBB2 (HER2) T798M demonstrated sensitivity to XL147 (SAR245408) in cell culture (PMID: 23948973). 23948973
KRAS Q61K non-small cell lung carcinoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited tumor growth and vascularization in xenograft models of a human non-small cell lung cancer cell line harboring KRAS Q61K (PMID: 25637314). 25637314
PTEN V54fs glioblastoma multiforme sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited tumor growth in xenograft models of a human glioblastoma cell line harboring PTEN V54fs (PMID: 25637314). 25637314
PTEN inact mut prostate adenocarcinoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited PI3K signaling, growth, and migration of a human prostate adenocarcinoma cell line harboring a PTEN inactivating mutation in culture, and inhibited tumor growth and vascularization in xenograft models (PMID: 25637314). 25637314
Unknown unknown colon adenocarcinoma not applicable XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 (SAR245408) demonstrated modest efficacy as a single agent in human cancer cell line xenograft models (PMID: 23002019). 23002019
Unknown unknown Advanced Solid Tumor not applicable XL147 Phase I Actionable In a Phase I study, 25/56 (43.9%) of patients with advanced solid tumors had stable disease as a best response to treatment with XL147, and one patient with NSCLC showed a partial response to XL147 (PMID: 24166903). 24166903
BRAF mutant Advanced Solid Tumor decreased response XL147 Preclinical Actionable In a preclinical study, tumor cell lines harboring BRAF mutations demonstrated limited sensitivity to XL147 treatment in culture (PMID: 25637314). 25637314
MET over exp melanoma sensitive XL147 Preclinical Actionable In a preclinical study, XL147 inhibited migration and growth of mouse melanoma cells with MET over expression in culture (PMID: 25637314). 25637314
Unknown unknown non-small cell lung carcinoma not applicable XL147 Phase I Actionable In a Phase I study, 25/56 (43.9%) of patients with advanced solid tumors had stable disease as a best response to treatment with XL147, and one patient with NSCLC showed a partial response to XL147 (PMID: 24166903). 24166903
Unknown unknown endometrial carcinoma not applicable XL147 Phase II Actionable In a Phase II trial, Pilaralisib (XL147) treatment resulted in an objective response rate of 6% (4/67) in patients with endometrial carcinoma, although anti-tumor activity is not associated with molecular alterations in PTEN and PIK3R1 (PMID: 25528496). 25528496
Clinical Trial Phase Therapies Title Recruitment Status
NCT01587040 Phase Ib/II XL147 SAR245409 Open Label Treatment Extension Study With SAR245408 or SAR245409 as a Monotherapy or as a Combination Regimen Completed