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

Drug Interactions Clinical Trial

Official title:

An Open-Label, Multiple-Dose, Non-Randomized Study to Assess the Drug-Drug Interactions of Proellex® (CDB-4124) With Cytochrome P450 Isoenzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 in Healthy Female Subjects

Clinical Trial Details — Status: Completed

Administrative data

• NCT number: NCT00741468
• Other study ID #: ZP-007
• Status: Completed
• Phase: Phase 1
• First received: August 25, 2008
• Last updated: August 20, 2014
• Start date: July 2008
• Est. completion date: October 2008

Study information

• Verified date: August 2014
• Source: Repros Therapeutics Inc.
• Contact: n/a
• Is FDA regulated: No
• Health authority: United States: Food and Drug Administration
• Study type: Interventional

Clinical Trial 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.

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.

Recruitment information / eligibility

• Status: Completed
• Enrollment: 18
• Est. completion date: October 2008
• Est. primary completion date: September 2008
• Accepts healthy volunteers: Accepts Healthy Volunteers
• Gender: Female
• Age group: 18 Years to 48 Years

Eligibility

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

Endpoint Classification: Pharmacodynamics Study, Intervention Model: Single Group Assignment, Masking: Open Label, Primary Purpose: Treatment

Related Conditions & MeSH terms

• Drug Interactions

Intervention

Drug:
• Proellex
2, 25 mg Proellex capsules administered daily
• CYP1A2 probe
Caffeine (200 mg)
• CYP2C9 probe
Tolbutamide (250 mg)
• CYP2C19 probe
Omeprazole (20 mg)
• CYP2D6 probe
Dextromethorphan (30 mg)
• CYP3A4 probe
Midazolam (2mg)

Locations

Country	Name	City	State
United States	Clinical Research Center Advanced Biomedical Research Inc.	Hackensack	New Jersey

Sponsors (1)

Lead Sponsor	Collaborator
Repros Therapeutics Inc.

Country where clinical trial is conducted

United States, 

Outcome

Type	Measure	Description	Time frame	Safety issue
Primary	Plasma AUC Ratio of Day 1 and Day 8	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.	8 days	Yes