A Phase I, Open-label Study of Absorption, Metabolism, and Excretion of Defactinib (VS-6063) in Healthy Male Subjects
- Registration Number
- NCT02913716
- Lead Sponsor
- Verastem, Inc.
- Brief Summary
This study assesses the mass balance recovery, pharmacokinetics, metabolite profile and metabolite identification of defactinib.
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- COMPLETED
- Sex
- Male
- Target Recruitment
- 5
Inclusion Criteria
- Body mass index (BMI) 18.0 to 35.0 kg/m2
- History (Hx) regular bowel movements
- Creatinine clearance >80 mL/min
Exclusion Criteria
- Hx alcohol abuse in past 2 yrs
- Current smoker
- Systolic blood pressure (S) or diastolic blood pressure (DBP) above upper limit of reference range (age 40-44 >90/140; age 45-65 >90/150)
Study & Design
- Study Type
- INTERVENTIONAL
- Study Design
- SINGLE_GROUP
- Arm && Interventions
Group Intervention Description Defactinib treatment defactinib Single dose of 400 mg \[14C\]-defactinib, oral suspension
- Primary Outcome Measures
Name Time Method Urine amount excreted (Ae) Screening to 168h post-dose Urine renal clearance (CLr) Screening to 168h post-dose Faeces Ae Screening to 168h post-dose Faeces Fe Screening to 168h post-dose Urine fraction of the dose excreted (Fe) Screening to 168h post-dose Urine cumulative amount excreted (Cum Ae) Screening to 168h post-dose Urine cumulative fraction of the dose excreted (Cum Fe) Screening to 168h post-dose Faeces Cum Ae Screening to 168h post-dose Faeces Cum Fe Screening to 168h post-dose All excreta Ae Screening to 168h post-dose All excreta Fe Screening to 168h post-dose All excreta Cum Ae Screening to 168h post-dose All excreta Cum Fe Screening to 168h post-dose All excreta non-renal clearance (CLnr) Screening to 168h post-dose
- Secondary Outcome Measures
Name Time Method Percentage of AUC(0-inf) accounted for by extrapolation (AUC%extrap) Screening to 168h post-dose lamdba-z Screening to 168h post-dose Apparent elimination half-life (T1/2) Screening to 168h post-dose Mean residence time Screening to 168h post-dose Time at which the analyte is first quantifiable (Tlag) Screening to 168h post-dose Area under the concentration vs. time curve from time zero extrapolated to last measurable concentration (AUC(0-last)) Screening to 168h post-dose Time from dosing at which Cmax is apparent (Tmax) Screening to 168h post-dose Maximum observed concentration (Cmax) Screening to 168h post-dose Apparent volume of distribution after oral administration (Vz/F) Screening to 168h post-dose Area under the concentration vs. time curve from time zero to infinity (AUC (0-inf)) Screening to 168h post-dose Apparent clearance after oral administration (CL/F) Screening to 168h post-dose