Healthy Subjects
Conditions
Brief summary
This study assesses the mass balance recovery, pharmacokinetics, metabolite profile and metabolite identification of defactinib.
Interventions
DRUGdefactinib
Single oral dose of 400 mg \[14C\]-defactinib
Sponsors
Verastem, Inc.
Study design
Allocation
NA
Intervention model
SINGLE_GROUP
Primary purpose
OTHER
Masking
NONE
Eligibility
Sex/Gender
MALE
Age
40 Years to 65 Years
Healthy volunteers
Yes
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)
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| All excreta 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 |
| Urine renal clearance (CLr) | Screening to 168h post-dose |
| Faeces Ae | Screening to 168h post-dose |
| All excreta Cum Fe | Screening to 168h post-dose |
| Faeces 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 non-renal clearance (CLnr) | Screening to 168h post-dose |
| All excreta Cum Ae | Screening to 168h post-dose |
| Urine amount excreted (Ae) | Screening to 168h post-dose |
Secondary
| Measure | Time frame |
|---|---|
| Time at which the analyte is first quantifiable (Tlag) | 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 |
| Area under the concentration vs. time curve from time zero extrapolated to last measurable concentration (AUC(0-last)) | 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 |
| 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 |
| Apparent clearance after oral administration (CL/F) | Screening to 168h post-dose |
| Apparent volume of distribution after oral administration (Vz/F) | Screening to 168h post-dose |
Outcome results
None listed