Open-Label, Multiple-Dose, Non-Randomized Study to Assess Drug-Drug Interactions of Proellex® in Female Subjects

Phase 1

Completed

• Conditions: Drug Interactions
• Interventions: Drug: Proellex; Drug: CYP1A2 probe; Drug: CYP2C9 probe; Drug: CYP2C19 probe; Drug: CYP2D6 probe; Drug: CYP3A4 probe

• Registration Number: NCT00741468
• Lead Sponsor: Repros Therapeutics Inc.

Brief Summary

This study will assess possible drug-drug interactions with specific isoenzymes over a total study duration of 6-8 weeks. Blood samples collected pre and post-dose, and urine samples collected post dose will be analyzed.

Detailed Description

This is an open-label, multiple-dose, non-randomized study to assess the drug-drug interactions of Proellex® with cytochrome P450 isoenzymes in healthy female subjects. On Day 1, following an overnight fast and morning void of the bladder, subjects will be administered CYP probe drugs orally. Serial blood samples will be collected at pre-dose and post-dose. Subjects will be administered two Proellex® 25 mg capsules (50 mg total dose) at approximately 0800 hours on Day 2 and 0700 hours on Days 3 through 8. One hour after administration of Proellex® on Day 8, the five CYP probe drugs will be administered and blood and urine samples collected as on Day 1. Blood samples for the determination of plasma concentrations of CDB-4124 and its metabolite CDB-4453 will be collected at pre-dose (trough) on Days 6, 7, and 8 to determine if steady-state conditions have been achieved. Samples will also be collected on Day 8 at 1, 2, 8 and 24 hour after administration of Proellex® to determine the plasma concentrations of CDB-4124 and CDB-4453.

Study Timeline

• Study Start: 2008-07
• Study First Submitted: 2008-08-25
• Study First Submitted QC: 2008-08-25
• Study First Posted: 2008-08-26
• Primary Completion: 2008-09
• Study Completion: 2008-10
• Results First Submitted: 2014-07-03
• Status Verified: 2014-08
• Results First Submitted QC: 2014-08-20
• Last Update Submitted: 2014-08-20
• Results First Posted: 2014-08-22
• Last Update Posted: 2014-08-22

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Female
• Target Recruitment: 18

Inclusion Criteria

• Healthy adult females
• A body mass index between 18 and 30 kg/m2, inclusive
• Negative urine drug and alcohol screen .

Exclusion Criteria

• Significant medical condition,
• Significant physical examination finding
• Clinical laboratory
• ECG abnormality
• CYP2D6 "poor metabolizer"

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
All subjects	Proellex	Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
All subjects	CYP3A4 probe	Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
All subjects	CYP2C9 probe	Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
All subjects	CYP1A2 probe	Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
All subjects	CYP2C19 probe	Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
All subjects	CYP2D6 probe	Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe

Primary Outcome Measures

Name	Time	Method
Plasma AUC Ratio of Day 1 and Day 8	8 days	Assessment of the drug-drug interactions of Proellex® (CDB-4124) with cytochrome P450 isoenzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 in healthy female subjects administered 50 mg Proellex® once daily (QD). The Day 8 AUC was compared to the Day 1 AUC to determine inhibition.; For CYP1A2 the plasma paraxanthine/caffeine MR ratio (metabolic ratio) was used. For CYP2D6 the MR ratio of dextromethorphan/dextrorphan was used.

Trial Locations

Locations (1)

Clinical Research Center Advanced Biomedical Research Inc.; 🇺🇸 Hackensack, New Jersey, United States