biostudies-literatureRodon JNCATS NIH HHSNational Cancer InstituteNCI NIH HHSNational Institutes of HealthTaiho Oncology105932https://www.ebi.ac.uk/biostudies/studies/S-EPMC12804367biostudies-literatureUnknown11(1)<h4>Background</h4>Protein kinase B (AKT)-directed therapies offer promise for patients with cancers harboring germline and somatic phosphatase and tensin homolog (PTEN) mutations. TAS-117 is an oral, selective, non-adenosine triphosphate-competitive allosteric AKT inhibitor that showed encouraging antitumor activity in a phase I study. This phase II study aimed to evaluate safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of TAS-117 in patients with advanced/metastatic solid tumors, including those harboring germline PTEN-inactivating mutations (EudraCT: 2020-004770-22).<h4>Materials and methods</h4>In this open-label, multicenter, single-arm phase II study, the 3 + 3 phase I-like dose escalation lead-in part A enrolled patients with advanced/metESMO openA phase II study of the AKT inhibitor TAS-117 in patients with advanced solid tumors and germline PTEN mutations.PMC12804367P30 CA008748UL1 TR000457K12 CA184746R01 CA279264Chawla SPArkenau HTWacheck VMurciano-Goroff YRLaetsch TWRodon JFunchain PHe YHervieu AAnthony KSinger CFMina MDelaloge SfalseA phase II study of the AKT inhibitor TAS-117 in patients with advanced solid tumors and germline PTEN mutations.<h4>Background</h4>Protein kinase B (AKT)-directed therapies offer promise for patients with cancers harboring germline and somatic phosphatase and tensin homolog (PTEN) mutations. TAS-117 is an oral, selective, non-adenosine triphosphate-competitive allosteric AKT inhibitor that showed encouraging antitumor activity in a phase I study. This phase II study aimed to evaluate safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of TAS-117 in patients with advanced/metastatic solid tumors, including those harboring germline PTEN-inactivating mutations (EudraCT: 2020-004770-22).<h4>Materials and methods</h4>In this open-label, multicenter, single-arm phase II study, the 3 + 3 phase I-like dose escalation lead-in part A enrolled patients with advanced/met2026-01-01T00:00:00Z2026 Jan2026-06-16T07:29:30.881Z2026-06-16T03:10:13.046ZS-EPMC128043674147524110.1016/j.esmoop.2025.105932