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Therapy Name | MLN1117 |
Synonyms | |
Therapy Description |
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 |