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
Study Details
Study Description
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.
Condition or Disease | Intervention/Treatment | Phase |
---|---|---|
Phase 1 |
Study Design
Arms and Interventions
Arm | Intervention/Treatment |
---|---|
Experimental: Treatment A Single dose of 4 liquid-filled capsules of MDV3100 reference formulation |
Drug: MDV3100
Oral
Other Names:
|
Experimental: Treatment B Single dose of 2 tablets of MDV3100 formulation tablet B |
Drug: MDV3100
Oral
Other Names:
|
Experimental: Treatment C Single dose of 2 tablets of MDV3100 formulation tablet C |
Drug: MDV3100
Oral
Other Names:
|
Outcome Measures
Primary Outcome Measures
- 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
- 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)
Eligibility Criteria
Criteria
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).
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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.
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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.
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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.
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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.
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Use of grapefruit or marmalade in the week prior to admission to the Clinical Unit, as reported by the subject.
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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.
Contacts and Locations
Locations
Site | City | State | Country | Postal Code | |
---|---|---|---|---|---|
1 | Parexel International GmbH | Berlin | Germany | 14050 |
Sponsors and Collaborators
- Astellas Pharma Europe B.V.
- Medivation, Inc.
Investigators
- Study Chair: Study Manager, Astellas Pharma Europe B.V.
Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- 9785-CL-0010
- 2012-002502-49