A Study to Compare Capsule and Tablet Forms of MDV3100 (Enzalutamide) After Administration of a Single Set Dose Under Fasted Conditions in Healthy Male Subjects

Phase 1

Completed

• Conditions: Healthy Subjects; Castration Resistant Prostate Cancer (CRPC); Relative Bioavailability; MDV3100
• Interventions: Drug: MDV3100

• Registration Number: NCT01911741
• Lead Sponsor: Astellas Pharma Europe B.V.

Brief Summary

A study to evaluate the bioavailability (BA) of a single oral dose of MDV3100 (enzalutamide) formulated as a solid spray dried tablet compared to oral liquid-filled capsules, and the safety and tolerability of oral formulations.

Subjects are admitted to the clinic from days 1 to 5, followed by outpatient assessments up to Day 50. They return to the clinic for an end of study visit (ESV) 7-10 days after the last pharmacokinetic (PK) sampling or after early withdrawal.

Detailed Description

Not available

Study Timeline

• Study Start: 2012-11
• Primary Completion: 2013-03
• Study Completion: 2013-03
• Status Verified: 2013-07
• Study First Submitted: 2013-07-26
• Study First Submitted QC: 2013-07-26
• Last Update Submitted: 2013-07-26
• Study First Posted: 2013-07-30
• Last Update Posted: 2013-07-30

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 55

Inclusion Criteria

• The subject has a body mass index (BMI) range of 18.5 - 29.9 kg/m2, inclusive. The subject weighs at least 50 kg (screening).
• Male subject and his female spouse/partner who is of childbearing potential must be using highly effective contraception consisting of two forms of birth control (one of which must be a barrier method) starting at screening and continue throughout the study period and for 3 months after final study drug administration.
• Male subject must not donate sperm starting at screening and throughout the study period and for at least 3 months after final study drug administration.

Exclusion Criteria

• Known or suspected hypersensitivity to enzalutamide, or any components of the formulation used.
• Confirmed CYP2C8 poor metabolizer status based on genotyping analysis.
• Any history of seizure including a febrile seizure in childhood, loss of consciousness, transient ischemic attack, or any condition that may pre-dispose to seizure.
• The subject has/had febrile illness or symptomatic, viral, bacterial (including upper respiratory infection), or fungal (non-cutaneous) infection within 1 week prior to first clinic check in.
• Use of grapefruit or marmalade in the week prior to admission to the Clinical Unit, as reported by the subject.
• Any significant blood loss, donated one unit (450 mL) of blood or more, or received a transfusion of any blood or blood products within 60 days or donated plasma within 7 days prior to clinic admission on Day -1.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Treatment A	MDV3100	Single dose of 4 liquid-filled capsules of MDV3100 reference formulation
Treatment B	MDV3100	Single dose of 2 tablets of MDV3100 formulation tablet B
Treatment C	MDV3100	Single dose of 2 tablets of MDV3100 formulation tablet C

Primary Outcome Measures

Name	Time	Method
Relative BA of capsule and tablet formulations of enzalutamide following a single dose of enzalutamide under fasted conditions	Day 1 through Day 50 (26 times)	AUC0-t (Area Under Curve from time zero to last quantifiable sample), AUC0-inf (AUC extrapolated to infinity), Cmax (Maximum concentration)

Secondary Outcome Measures

Name	Time	Method
Relative BA of capsule and tablet formulations of enzalutamide following a single dose of enzalutamide under fasted conditions	Day 1 through Day 50 (26 times)	AUC0-72h (AUC from time zero to 72h post dose), AUC0-t, AUC0-inf, %AUC (Percentage of AUC), Cmax, tmax (Time to attain Cmax), λz (Terminal elimination rate constant), t1/2 (Terminal elimination half life), (MPR) metabolites to parent ratio, MPR(molecular weight corrected \[MWC\]), %AUC, CL/F (apparent oral clearance), Vz/F (apparent volume of distribution)
Safety and tolerability of oral formulations of enzalutamide	Screening through ESV (7-10 days after the last pharmacokinetic (PK) sampling or after early withdrawal)	adverse events, physical examination, vital signs, clinical laboratory tests, 12-lead Electrocardiogram (ECG)

Trial Locations

Locations (1)

Parexel International GmbH; 🇩🇪 Berlin, Germany