A Study to Evaluate How a Drug That Alters Liver Enzymes (Rifampin) Affects the Metabolism of Enzalutamide in Men

NCT02138799 | Completed Phase 1

• 2 other identifiers: 9785-CL-04052012-004841-34
• Study Type: interventional
• Target: 28
• Locations: 1 country
• Sites: 1

Brief Summary

This study evaluates how a drug that alters liver enzymes (rifampin) affects the metabolism of enzalutamide in men by measuring concentrations of enzalutamide and its metabolites in plasma.

Conditions

Drug-Drug Interaction (DDI); Healthy Subjects; Pharmacokinetics of Enzalutamide

Keywords

Phase I; Pharmacokinetics; Safety; Drug-drug interactions; Enzalutamide; Rifampin; CYP3A4; CYP2D8; Enzyme induction

Outcome Measures

Primary Outcomes (2)

• PK of enzalutamide and the sum of enzalutamide + M2 in plasma measured by area under the curve (AUC) from time 0 to 336 hours after dosing (AUC0-336h)

  Days 1 to 50 (29 times)

• PK of enzalutamide and the sum of enzalutamide + M2 in plasma measured by AUC extrapolated to infinity (AUCinf)

  Days 1 to 50 (29 times)

Secondary Outcomes (3)

• PK of enzalutamide, M2, M1 and the sum of enzalutamide + M2 in plasma

  Days 8 to 57 (49 times)

• PK of rifampin in plasma

  Days 6 to 21 (20 times)

• Safety and tolerability of enzalutamide, alone or in the presence of rifampin

  Screening (Day -28 to -7) to End of Study Visit (ESV) (>34 times)

Study Arms (2)

1: single dose of enzalutamide

EXPERIMENTAL

Drug: enzalutamide

2: multiple doses of rifampin and single dose of enzalutamide

EXPERIMENTAL

Drug: enzalutamide; Drug: rifampin

Interventions

enzalutamide DRUG

oral

Also known as: ASP9785,, MDV3100,, Xtandi

1: single dose of enzalutamide; 2: multiple doses of rifampin and single dose of enzalutamide

rifampin DRUG

oral

2: multiple doses of rifampin and single dose of enzalutamide

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Subject has a Body Mass Index (BMI) of at least 18.5 and no greater than 29.9 kg/m2 at screening.
• Subject must use a condom when having sex with a pregnant woman.
• Male subject and their female spouse/partners who are of childbearing potential must be using highly effective contraception consisting of two forms of birth control.
• Male subject must not donate sperm starting at screening and throughout the study period and for 90 days after the final study drug administration.

You may not qualify if:

• Subject has a confirmed CYP2C8 poor metabolizer status based on genotyping analysis.
• Subject has a history of seizure or any condition that may predispose to seizure. Historically or currently on any convulsive medication or drugs that may lower the seizure threshold. History of any central nervous system (CNS) infections. Also history of transient ischemic attack or cerebrovascular accident with or without head trauma within 12 months of enrollment (Day -1 visit).
• Subject has 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.

Sponsors & Collaborators

• Astellas Pharma Europe B.V.: lead
• Medivation, Inc.: collaborator

Study Sites (1)

Parexel International GmbH

Berlin, 14050, Germany

Location

MeSH Terms

Interventions

enzalutamide; Rifampin

Intervention Hierarchy (Ancestors)

Rifamycins; Heterocyclic Compounds, 4 or More Rings; Heterocyclic Compounds, Fused-Ring; Heterocyclic Compounds; Lactams, Macrocyclic; Macrocyclic Compounds; Polycyclic Compounds

Study Officials

• Central Contact

  Astellas Pharma Europe B.V.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: BASIC SCIENCE
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: May 13, 2014
• First Posted: May 15, 2014
• Study Start: July 1, 2013
• Primary Completion: September 1, 2013
• Study Completion: September 1, 2013
• Last Updated: October 15, 2014

Record last verified: 2014-10

Locations

DE (1)