Therapy Detail

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Therapy Name XL147
Synonyms
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|XL-147 PI3K Inhibitor (Pan) 38 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, PMID: 29593099).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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
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
PIK3CA mutant Advanced Solid Tumor sensitive XL147 Preclinical Actionable In a preclinical study, tumor cell lines with PIK3CA mutations demonstrated sensitivity to XL147 in culture (PMID: 25637314). 25637314
PIK3CA mutant Advanced Solid Tumor sensitive XL147 Phase I Actionable In a Phase I clinical trial, XL147 (SAR24508) was shown to be safe and potentially efficacious, with clinical activity seen irrespective of tumor PI3K pathway molecular alterations (PMID: 24166903). 24166903
Unknown unknown lung non-small cell 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
PIK3CA amp ovarian cancer sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited PI3K signaling and proliferation of a PIK3CA amplified human ovarian cancer cell line in culture, and inhibited tumor growth 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 trial, 43.9% (25/56) of patients with advanced solid tumors had stable disease as a best response to treatment with Pilaralisib (XL147), and one patient with NSCLC showed a partial response, and in a separate therapy arm, Pilaralisib (XL147) in tablet formulation demonstrated safety and some antitumor activity in advanced solid tumor patients, including 11.1% (2/18) of patients with a partial response (PMID: 29593099, PMID: 24166903; NCT00486135). 29593099 24166903
PIK3CA E545K breast carcinoma sensitive XL147 Preclinical - Cell line xenograft Actionable In a preclinical study, XL147 inhibited PI3K signaling and proliferation of a human breast carcinoma cell line harboring PIK3CA E545K in culture and inhibited tumor growth in xenograft models (PMID: 25637314). 25637314

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Clinical Trial Phase Therapies Title Recruitment Status
NCT01587040 Phase Ib/II XL147 Voxtalisib Open Label Treatment Extension Study With SAR245408 or SAR245409 as a Monotherapy or as a Combination Regimen Completed


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