A Phase I, Open-label Study of the Absorption, Metabolism and Excretion of Defactinib (VS-6063-106) in Healthy Male Subjects
Overview
- Phase
- Phase 1
- Intervention
- defactinib
- Conditions
- Healthy Subjects
- Sponsor
- Verastem, Inc.
- Enrollment
- 5
- Primary Endpoint
- Urine amount excreted (Ae)
- Status
- Completed
- Last Updated
- 9 years ago
Overview
Brief Summary
This study assesses the mass balance recovery, pharmacokinetics, metabolite profile and metabolite identification of defactinib.
Investigators
Eligibility Criteria
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)
Arms & Interventions
Defactinib treatment
Single dose of 400 mg \[14C\]-defactinib, oral suspension
Intervention: defactinib
Outcomes
Primary Outcomes
Urine amount excreted (Ae)
Time Frame: Screening to 168h post-dose
Urine renal clearance (CLr)
Time Frame: Screening to 168h post-dose
Faeces Ae
Time Frame: Screening to 168h post-dose
Faeces Fe
Time Frame: Screening to 168h post-dose
Urine fraction of the dose excreted (Fe)
Time Frame: Screening to 168h post-dose
Urine cumulative amount excreted (Cum Ae)
Time Frame: Screening to 168h post-dose
Urine cumulative fraction of the dose excreted (Cum Fe)
Time Frame: Screening to 168h post-dose
Faeces Cum Ae
Time Frame: Screening to 168h post-dose
Faeces Cum Fe
Time Frame: Screening to 168h post-dose
All excreta Ae
Time Frame: Screening to 168h post-dose
All excreta Fe
Time Frame: Screening to 168h post-dose
All excreta Cum Ae
Time Frame: Screening to 168h post-dose
All excreta Cum Fe
Time Frame: Screening to 168h post-dose
All excreta non-renal clearance (CLnr)
Time Frame: Screening to 168h post-dose
Secondary Outcomes
- 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)