Clinical trial NCT02913716: A Phase I, Open-label Study of Absorption, Metabolism, and Excretion of Defactinib (VS-6063) in Healthy Male Subjects
Official title: A Phase I, Open-label Study of the Absorption, Metabolism and Excretion of Defactinib (VS-6063-106) in Healthy Male Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy Subjects
Lead sponsor: Verastem, Inc.
Sponsor class: INDUSTRY
First posted: 2016-09-26
Enrollment: 5
Sex: MALE
Minimum age (years): 40
Maximum age (years): 65
Standard ages: ADULT
OLDER_ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: OTHER

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


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)

Primary outcomes:
measure: Urine amount excreted (Ae)
timeFrame: Screening to 168h post-dose
measure: Urine fraction of the dose excreted (Fe)
timeFrame: Screening to 168h post-dose
measure: Urine cumulative amount excreted (Cum Ae)
timeFrame: Screening to 168h post-dose
measure: Urine cumulative fraction of the dose excreted (Cum Fe)
timeFrame: Screening to 168h post-dose
measure: Urine renal clearance (CLr)
timeFrame: Screening to 168h post-dose
measure: Faeces Ae
timeFrame: Screening to 168h post-dose
measure: Faeces Fe
timeFrame: Screening to 168h post-dose
measure: Faeces Cum Ae
timeFrame: Screening to 168h post-dose
measure: Faeces Cum Fe
timeFrame: Screening to 168h post-dose
measure: All excreta Ae
timeFrame: Screening to 168h post-dose
measure: All excreta Fe
timeFrame: Screening to 168h post-dose
measure: All excreta Cum Ae
timeFrame: Screening to 168h post-dose
measure: All excreta Cum Fe
timeFrame: Screening to 168h post-dose
measure: All excreta non-renal clearance (CLnr)
timeFrame: Screening to 168h post-dose
Secondary outcomes:
measure: Time at which the analyte is first quantifiable (Tlag)
timeFrame: Screening to 168h post-dose
measure: Time from dosing at which Cmax is apparent (Tmax)
timeFrame: Screening to 168h post-dose
measure: Maximum observed concentration (Cmax)
timeFrame: Screening to 168h post-dose
measure: Area under the concentration vs. time curve from time zero extrapolated to last measurable concentration (AUC(0-last))
timeFrame: Screening to 168h post-dose
measure: Area under the concentration vs. time curve from time zero to infinity (AUC (0-inf))
timeFrame: Screening to 168h post-dose
measure: Percentage of AUC(0-inf) accounted for by extrapolation (AUC%extrap)
timeFrame: Screening to 168h post-dose
measure: lamdba-z
timeFrame: Screening to 168h post-dose
measure: Apparent elimination half-life (T1/2)
timeFrame: Screening to 168h post-dose
measure: Mean residence time
timeFrame: Screening to 168h post-dose
measure: Apparent clearance after oral administration (CL/F)
timeFrame: Screening to 168h post-dose
measure: Apparent volume of distribution after oral administration (Vz/F)
timeFrame: Screening to 168h post-dose
Other outcomes:
Locations:
Study officials:
affiliation: Verastem, Inc.
name: Hagop Youssoufian
role: STUDY_CHAIR
References: