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

Astellas

Status and phase: Completed; Phase 1

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

Treatments: Drug: MDV3100

Study type: Interventional

Funder types: Industry

Identifiers

NCT01911741

2012-002502-49 (EudraCT Number)

9785-CL-0010

Details and patient eligibility

About

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.

Enrollment: 55 patients

Sex: Male

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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.

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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55 participants in 3 patient groups

Treatment A

Experimental group

Description:

Single dose of 4 liquid-filled capsules of MDV3100 reference formulation

Treatment:

Drug: MDV3100

Treatment B

Experimental group

Description:

Single dose of 2 tablets of MDV3100 formulation tablet B

Treatment:

Drug: MDV3100

Treatment C

Experimental group

Description:

Single dose of 2 tablets of MDV3100 formulation tablet C

Treatment:

Drug: MDV3100