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

Repros Therapeutics Inc.18 enrolled

Overview

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.

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 Type

INTERVENTIONAL

Allocation

Purpose

TREATMENT

Masking

NONE

Enrollment

Conditions

Drug Interactions

Interventions

ProellexDRUG

2, 25 mg Proellex capsules administered daily

CYP1A2 probeDRUG

Caffeine (200 mg)

CYP2C9 probeDRUG

Tolbutamide (250 mg)

CYP2C19 probe

Eligibility

Sex: FEMALEMin age: 18 YearsMax age: 48 YearsHealthy volunteers:

Medical Language ↔ Plain English

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"

Locations (1)

Clinical Research Center Advanced Biomedical Research Inc.

Hackensack, New Jersey, United States

Outcomes

Primary Outcomes

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.

Time frame: 8 days

Data from ClinicalTrials.gov

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