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Therapy Name TAS-117
Synonyms
Therapy Description

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).

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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).

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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
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
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...

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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 Terminated USA | GBR | FRA | AUT 0


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