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MLN1117 (INK1117) selectively inhibits PI3K alpha kinase, including mutations of PIK3CA, and therefore, targets the PI3K/Akt/mTOR pathway with potentially less toxicity than pan-PI3K inhibitors (NCI Drug Dictionary).
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|MLN1117||INK1117|TAK-117|Serabelisib|MLN-1117||PIK3CA inhibitor 16||Serabelisib (MLN1117) selectively inhibits PI3K alpha kinase, including mutations of PIK3CA, and therefore, targets the PI3K/Akt/mTOR pathway with potentially less toxicity than pan-PI3K inhibitors (PMID: 28490463, PMID: 30168905).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|PIK3CA mutant||stomach cancer||predicted - sensitive||MLN1117||Case Reports/Case Series||Actionable||In a Phase I trial, MLN1117 (INK1117) treatment resulted in a partial response in one patient with gastric cancer harboring a PIK3CA mutation (PMID: 28490463; NCT01449370).||28490463|
|Unknown unknown||breast cancer||not applicable||MLN1117||Phase I||Actionable||In a Phase I trial, treatment with MLN1117 resulted in antitumor activity, demonstrating partial responses in patients with advanced solid tumors including breast and gastric cancer (J Clin Oncol, May 2015 vol. 33 no. 15_suppl 2501).||detail...|
|PIK3CA mutant||Advanced Solid Tumor||sensitive||MLN1117||Phase I||Actionable||In a Phase I trial, MLN1117 demonstrated safety and preliminary efficacy in a variety of patients with advanced solid tumors carrying PIK3CA mutations (Journal of Clinical Oncology, 2015 ASCO Annual Meeting Vol 33, No 15_suppl., 2015: 2501).||detail...|
|PIK3CA mutant||Advanced Solid Tumor||sensitive||MLN1117||Preclinical||Actionable||In a preclinical study, MLN1117 inhibited proliferation of tumor cells harboring oncogenic PIK3CA mutations in culture and inhibited tumor growth in PIK3CA mutant xenograft models (Cancer Ther 2011;10(11 Suppl):Abstract nr A171).||detail...|
|PIK3CA mutant||breast cancer||predicted - sensitive||MLN1117||Case Reports/Case Series||Actionable||In a Phase I trial, MLN1117 (INK1117) treatment resulted in partial response in 3 patients with breast cancer harboring PI3CA mutations (PMID: 28490463; NCT01449370).||28490463|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|
|NCT02551055||Phase I||Docetaxel Paclitaxel Alisertib Mivavotinib MLN1117||MLN1117 in Combination With Docetaxel, Paclitaxel, and Other Investigational Anticancer Agents to Treat Participants With Gastric and Gastroesophageal Adenocarcinoma||Terminated||USA||1|
|NCT01449370||Phase I||MLN1117||Dose Escalation Study of MLN1117 in Subjects With Advanced Cancer||Completed||USA||2|