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|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|TAS-117||TAS117|TAS 117||Akt Inhibitor (Pan) 21||TAS-117 is a selective allosteric inhibitor of Akt that inhibits Akt phosphorylation and downstream signaling, potentially leading to cytoxicity in tumor cells and decreased tumor growth (PMID: 24934808).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|PIK3CA E545K||ovarian cancer||predicted - sensitive||TAS-117||Case Reports/Case Series||Actionable||In a Phase II trial, TAS-117 treatment in an ovarian cancer patient harboring PIK3CA E545K led to a partial response at 6 weeks after treatment and a 39% decrease in tumor size, but subsequently progression was observed at 12 weeks in non-target lesions and an increase in tumor markers at 18 weeks, and TAS-117 treatment was discontinued (PMID: 33723724; NCT03017521).||33723724|
|PTEN inact mut||breast cancer||predicted - sensitive||TAS-117||Case Reports/Case Series||Actionable||In a Phase II trial, TAS-117 treatment demonstrated tolerability in patients with advanced solid tumors harboring germline inactivating PTEN mutations, and resulted in an unconfirmed partial response in one patient with breast cancer and target tumor lesion shrinkage of approximately 15% and stable disease lasting more than 8 months in another breast cancer patient (Ann Oncol (2022) 33 (suppl_7): S754-S755; NCT04770246).||detail...|
|PIK3CA H1047R||breast cancer||predicted - sensitive||TAS-117||Case Reports/Case Series||Actionable||In a Phase II trial, TAS-117 treatment in a breast cancer patient harboring PIK3CA H1047R led to initial stable disease, however, disease progression was observed at 12 weeks after treatment along with an increase of non-target lesions, following which treatment was discontinued (PMID: 33723724; NCT03017521).||33723724|
|PIK3CA act mut||Advanced Solid Tumor||no benefit||TAS-117||Phase II||Actionable||In a Phase II trial, TAS-117 treatment in advanced solid tumor patients with PIK3CA activating mutations (n=12) or AKT1 E17K (n=1) refractory to standard treatment had minimal activity, and led to an overall response rate of 8% (1/13), disease control rate of 23% (3/13), median progression-free survival of 1.4 months (mo), and a median overall survival of 4.8 mo, however due to poor accrual and lack of durable response to TAS-117 early termination of study was recommended (PMID: 33723724; NCT03017521).||33723724|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|
|NCT04770246||Phase II||TAS-117||TAS-117 in Patients With Advanced Solid Tumors Harboring Germline PTEN Mutations||Active, not recruiting||USA | FRA | AUT||1|