Open-Label, Multiple-Dose, Non-Randomized Study to Assess Drug-Drug Interactions of Proellex® in Female Subjects
This study has been completed.
Sponsor:
Repros Therapeutics Inc.
ClinicalTrials.gov Identifier:
NCT00741468
First Posted: August 26, 2008
Last Update Posted: August 22, 2014
Information provided by (Responsible Party):
Repros Therapeutics Inc.
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Purpose
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.
| Condition | Intervention | Phase |
|---|---|---|
| Drug Interactions | Drug: Proellex Drug: CYP1A2 probe Drug: CYP2C9 probe Drug: CYP2C19 probe Drug: CYP2D6 probe Drug: CYP3A4 probe | Phase 1 |
| Study Type: | Interventional |
| Study Design: | Intervention Model: Single Group Assignment Masking: None (Open Label) Primary Purpose: Treatment |
| 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 |
Resource links provided by NLM:
Further study details as provided by Repros Therapeutics Inc.:
Primary Outcome Measures:
- Plasma AUC Ratio of Day 1 and Day 8 [ Time Frame: 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.
| Enrollment: | 18 |
| Study Start Date: | July 2008 |
| Study Completion Date: | October 2008 |
| Primary Completion Date: | September 2008 (Final data collection date for primary outcome measure) |
| Arms | Assigned Interventions |
|---|---|
|
Experimental: All subjects
Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
|
Drug: Proellex
2, 25 mg Proellex capsules administered daily
Other Name: Telapristone acetate
Drug: CYP1A2 probe
Caffeine (200 mg)
Other Name: Caffeine (200 mg)
Drug: CYP2C9 probe
Tolbutamide (250 mg)
Other Name: Tolbutamide (250 mg)
Drug: CYP2C19 probe
Omeprazole (20 mg)
Other Name: Omeprazole (20 mg)
Drug: CYP2D6 probe
Dextromethorphan (30 mg)
Other Name: Dextromethorphan (30 mg)
Drug: CYP3A4 probe
Midazolam (2mg)
Other Name: Midazolam (2mg)
|
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.
Eligibility
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| Ages Eligible for Study: | 18 Years to 48 Years (Adult) |
| Sexes Eligible for Study: | Female |
| Accepts Healthy Volunteers: | Yes |
Criteria
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"
Contacts and Locations
Information from the National Library of Medicine
To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.
Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT00741468
Locations
| United States, New Jersey | |
| Clinical Research Center Advanced Biomedical Research Inc. | |
| Hackensack, New Jersey, United States, 07601 | |
Sponsors and Collaborators
Repros Therapeutics Inc.
Investigators
| Study Director: | Ronald Wiehle, PhD | Repros Therapeutics Inc. |
More Information
| Responsible Party: | Repros Therapeutics Inc. |
| ClinicalTrials.gov Identifier: | NCT00741468 History of Changes |
| Other Study ID Numbers: |
ZP-007 |
| First Submitted: | August 25, 2008 |
| First Posted: | August 26, 2008 |
| Results First Submitted: | July 3, 2014 |
| Results First Posted: | August 22, 2014 |
| Last Update Posted: | August 22, 2014 |
| Last Verified: | August 2014 |
Keywords provided by Repros Therapeutics Inc.:
|
Drug-drug interactions DDI |
Additional relevant MeSH terms:
|
Midazolam Caffeine Dextromethorphan Omeprazole Tolbutamide Adjuvants, Anesthesia Hypnotics and Sedatives Central Nervous System Depressants Physiological Effects of Drugs Anti-Anxiety Agents Tranquilizing Agents Psychotropic Drugs Anesthetics, Intravenous Anesthetics, General Anesthetics |
GABA Modulators GABA Agents Neurotransmitter Agents Molecular Mechanisms of Pharmacological Action Central Nervous System Stimulants Phosphodiesterase Inhibitors Enzyme Inhibitors Purinergic P1 Receptor Antagonists Purinergic Antagonists Purinergic Agents Anti-Ulcer Agents Gastrointestinal Agents Proton Pump Inhibitors Antitussive Agents Respiratory System Agents |