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Ref Type Journal Article
PMID (33723724)
Authors Lee JB, Jung M, Beom SH, Kim GM, Kim HR, Choi HJ, Sohn JH, Ahn JB, Rha SY, Chung HC
Title Phase 2 study of TAS-117, an allosteric akt inhibitor in advanced solid tumors harboring phosphatidylinositol 3-kinase/v-akt murine thymoma viral oncogene homolog gene mutations.
Abstract Text TAS-117 is a potent and selective allosteric pan-v-akt murine thymoma viral oncogene homolog (Akt) inhibitor. We conducted a single-arm single-center phase 2 study of TAS-117 in heavily treated patients with tumors refractory to systemic chemotherapy and harboring phosphatidylinositol 3-kinase (PI3K)/Akt mutations. Patients with gastrointestinal (GI) cancers were orally administered 16 mg TAS-117 daily, and those with non-GI tumors were administered 24 mg on a 4 days on/3 days off schedule. The primary endpoint was overall response rate (ORR). Secondary endpoints included disease control rate (DCR), progression-free survival (PFS), overall survival (OS), PFS ratio, safety, and tolerability. Thirteen patients were enrolled: eight with non-GI (breast, ovarian, endometrial, and non-small cell lung) and five with GI (colon, rectal, gastric, and gallbladder) cancers. Ten patients were treated with TAS-117 after ≥ 4 lines of therapy. Twelve patients showed PIK3 catalytic subunit alpha (PIK3CA) mutations; one harbored an Akt1E17K mutation. The median treatment duration was 1.4 months; the median number of treatment cycles was 2. The ORR was 8 %, and DCR was 23 %. The median PFS and OS were 1.4 and 4.8 months, respectively. Grade 3-4 treatment-related adverse events were anorexia (grade 3, 8 %) and hyperglycemia (grade 3, 8 %; grade 4, 8 %).Grade 3-4 treatment-related adverse events occurred in 27 % of grade 3 anorexia (9 %) and hyperglycemia (grade 3, 8 %; grade 4, 9\%). TAS-117 showed limited antitumor activity and manageable toxicity. Clinical efficacy was observed in patients with ovarian cancer harboring PIK3CA E545K mutations and in patients with breast cancer harboring PIK3CA H1047R and Akt1E17K mutations.Trial registration: This study was retrospectively registered with (NCT03017521 on January 11, 2017).


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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
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