Table 3. . Primary, secondary and exploratory objectives in TAS-117-201.

Part A	Part B (including dose and regimen confirmation in part A)
Primary objectives • To investigate the safety and tolerability and to determine the MTD and the RP2D of TAS-117	Primary objective • To evaluate the ORR in patients with solid tumors harboring germline PTEN-inactivating mutations based on ICR
Secondary objectives • To characterize:   ○ PK profile of TAS-117   ○ PD profile of TAS-117 • To evaluate:   ○ ORR (investigator assessment)   ○ DCR, DOR (investigator assessments) (ICR assessment will be also performed)   ○ OS	Secondary objectives • To evaluate the safety profile of TAS-117 • To evaluate:   ○ ORR (investigator assessment)   ○ DCR, DOR (investigator assessments) (ICR assessment will be also performed)   ○ OS
Exploratory objective • To confirm PTEN-inactivating mutations and explore other potential predictive biomarkers of TAS-117	Exploratory objectives • To confirm PTEN-inactivating mutations and explore other potential predictive biomarkers of TAS-117 • To evaluate TAS-117 exposure-response relationship • To assess PROs:   ○ Severity of pain and the impact of pain on daily function and assess analgesic use   ○ Disease-related symptoms, impact of treatment and HRQoL based on patient-reported data   ○ Current severity and overall change in health status from the start of study treatment

DCR: Disease control rate; DOR: Duration of response; HRQoL: Health-related quality of life; ICR: Independent central review; MTD: Maximum tolerated dose; ORR: Overall response rate; OS: Overall survival; PD: Pharmacodynamic; PK: Pharmacokinetic; PRO: Patient-reported outcome; PTEN: Phosphatase and tensin homolog deleted on chromosome 10; RP2D: Recommended phase II dose.