Missing content? – Request curation!
Request curation for specific Genes, variants, or PubMed publications.
Have questions, comments or suggestions? - Let us know!
Email us at : firstname.lastname@example.org
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).
|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).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|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||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 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|
|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||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|
|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|
|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||3|