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

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

This study assesses the mass balance recovery, pharmacokinetics, metabolite profile and metabolite identification of defactinib.

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: defactinib

• Study Type: Interventional
• Enrollment (Actual): 5
• Phase: Phase 1

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 40 years to 65 years (Adult, Older Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Other
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

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

What is the study measuring?

Primary Outcome Measures

Outcome Measure	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	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

Collaborators and Investigators

• Sponsor: Verastem, Inc.
• Investigators: Study Chair: Hagop Youssoufian, Verastem, Inc.

Study record dates

Study Major Dates

• Study Start: August 1, 2015
• Primary Completion (Actual): September 1, 2015
• Study Completion (Actual): September 1, 2015

Study Registration Dates

• First Submitted: September 19, 2016
• First Submitted That Met QC Criteria: September 23, 2016
• First Posted (Estimate): September 26, 2016

Study Record Updates

• Last Update Posted (Estimate): January 30, 2017
• Last Update Submitted That Met QC Criteria: January 26, 2017
• Last Verified: September 1, 2016

More Information

Terms related to this study

• Other Study ID Numbers: VS-6063-106

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO