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

Phase 1

Completed

• Conditions: Healthy Subjects
• Interventions: Drug: defactinib

• 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

Study Timeline

• Study Start: 2015-08
• Primary Completion: 2015-09
• Study Completion: 2015-09
• Status Verified: 2016-09
• Study First Submitted: 2016-09-19
• Study First Submitted QC: 2016-09-23
• Study First Posted: 2016-09-26
• Last Update Submitted: 2017-01-26
• Last Update Posted: 2017-01-30

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