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

Healthy Subjects Clinical Trial

Official title:

A Phase I, Single-center, Open-label, Randomized, Parallel, Relative Bioavailability Study Comparing a Capsule and Tablet Formulations of Enzalutamide Following a Single 160 mg Dose Under Fasted Conditions in Healthy Male Subjects

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT01911741
• Other study ID #: 9785-CL-0010
• Secondary ID: 2012-002502-49
• Status: Completed
• Phase: Phase 1
• First received: July 26, 2013
• Last updated: July 26, 2013
• Start date: November 2012
• Est. completion date: March 2013

Study information

• Verified date: July 2013
• Source: Astellas Pharma Inc
• Contact: n/a
• Is FDA regulated: No
• Health authority: Germany: Federal Institute for Drugs and Medical Devices
• Study type: Interventional

Clinical Trial 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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 55
• Est. completion date: March 2013
• Est. primary completion date: March 2013
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Male
• Age group: 18 Years to 55 Years

Eligibility

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

Allocation: Randomized, Endpoint Classification: Bio-availability Study, Intervention Model: Parallel Assignment, Masking: Open Label, Primary Purpose: Basic Science

Related Conditions & MeSH terms

• Castration Resistant Prostate Cancer (CRPC)
• Healthy Subjects
• MDV3100
• Relative Bioavailability

Intervention

Drug:
• MDV3100
Oral

Locations

Country	Name	City	State
Germany	Parexel International GmbH	Berlin

Sponsors (2)

Lead Sponsor	Collaborator
Astellas Pharma Europe B.V.	Medivation, Inc.

Country where clinical trial is conducted

Germany, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Relative BA of capsule and tablet formulations of enzalutamide following a single dose of enzalutamide under fasted conditions	AUC0-t (Area Under Curve from time zero to last quantifiable sample), AUC0-inf (AUC extrapolated to infinity), Cmax (Maximum concentration)	Day 1 through Day 50 (26 times)	No
Secondary	Relative BA of capsule and tablet formulations of enzalutamide following a single dose of enzalutamide under fasted conditions	AUC0-72h (AUC from time zero to 72h post dose), AUC0-t, AUC0-inf, %AUC (Percentage of AUC), Cmax, tmax (Time to attain Cmax), ?z (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)	Day 1 through Day 50 (26 times)	No
Secondary	Safety and tolerability of oral formulations of enzalutamide	adverse events, physical examination, vital signs, clinical laboratory tests, 12-lead Electrocardiogram (ECG)	Screening through ESV (7-10 days after the last pharmacokinetic (PK) sampling or after early withdrawal)	Yes