A Phase I, Open-label Study of Absorption, Metabolism, and Excretion of Defactinib (VS-6063) in Healthy Male Subjects

Study Overview
=================
Brief Summary
-----------------
This study assesses the mass balance recovery, pharmacokinetics, metabolite profile and metabolite identification of defactinib.

Official Title
-----------------
A Phase I, Open-label Study of the Absorption, Metabolism and Excretion of Defactinib (VS-6063-106) in Healthy Male Subjects

Conditions
-----------------
Healthy Subjects

Intervention / Treatment
-----------------
* Drug: defactinib


Participation Criteria
=================
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)

Ages Eligible for Study
-----------------
Minimum Age: 40 Years
Maximum Age: 65 Years

Sexes Eligible for Study
-----------------
Male

Accepts Healthy Volunteers
-----------------
Accepts Healthy Volunteers

Study Plan
=================
How is the study designed?
-----------------

Design Details

Primary Purpose: Other
Intervention Model: Single Group Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Defactinib treatment<br>Single dose of 400 mg [14C]-defactinib, oral suspension | Drug: defactinib<br>* Single oral dose of 400 mg [14C]-defactinib<br>* Other names: VS-6063;|

What is the study measuring?
-----------------
Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Urine amount excreted (Ae) |  | 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 | 
| 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 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

| Outcome Measure | Measure Description | 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 |