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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, PMID: 29593099).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
XL147		SAR245408\|Pilaralisib\|XL-147	PI3K Inhibitor (Pan) 42	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
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
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
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
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
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
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
PTEN V54fs	glioblastoma	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
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
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

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
NCT01587040	Phase Ib/II	XL147 Voxtalisib	Open Label Treatment Extension Study With SAR245408 or SAR245409 as a Monotherapy or as a Combination Regimen	Completed	USA \| FRA \| ESP \| BEL	0

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