A Phase 1 interventional study of Proellex and CYP1A2 probe in Drug Interactions, sponsored by Repros Therapeutics Inc.. Completed at 1 site in United States. Open to female participants aged 18 Years to 48 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2014-08-22.
Sponsored by Repros Therapeutics Inc. · Phase 1, Interventional, and Treatment
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.
Repros Therapeutics Inc. is the lead sponsor of 57 studies on the registry; none are open to participants now.
Counted across the registry records on this site, refreshed daily.
Exclusion Criteria:
Proellex 50 mg CYP1A2 probe CYP2C9 probe CYP2C19 probe CYP2D6 probe CYP3A4 probe
Drug: Proellex · Drug: CYP1A2 probe · Drug: CYP2C9 probe · Drug: CYP2C19 probe · Drug: CYP2D6 probe · Drug: CYP3A4 probe
2, 25 mg Proellex capsules administered daily
Also known as: Telapristone acetate
Caffeine (200 mg)
Also known as: Caffeine (200 mg)
Tolbutamide (250 mg)
Also known as: Tolbutamide (250 mg)
Omeprazole (20 mg)
Also known as: Omeprazole (20 mg)
Dextromethorphan (30 mg)
Also known as: Dextromethorphan (30 mg)
Midazolam (2mg)
Also known as: Midazolam (2mg)
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
| Milestone | All Participants |
|---|---|
| Started | 18 |
| Completed | 18 |
| Not completed | 0 |
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.
| Ratio of geometric means Day 8 to Day 1 | CYP1A2 | CYP2C9 | CYP2C19 | CYP2D6 | CYP3A4 |
|---|---|---|---|---|---|
| Plasma AUC Ratio of Day 1 and Day 8 | 1.093 (1.006 to 1.188) | 1.029 (0.960 to 1.103) | 1.104 (0.936 to 1.303) | 1.914 (1.463 to 2.504) | 2.245 (2.019 to 2.495) |
Non-serious events are listed at a 5% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| All Subjects | — | 0/18 (0%) | 13/18 (72.2%) |
| Event | All Subjects |
|---|---|
| Early menstruationReproductive system and breast disorders | 5/18 |
| DizzinessNervous system disorders | 5/18 |
| HeadacheNervous system disorders | 3/18 |
| Lower back painMusculoskeletal and connective tissue disorders | 2/18 |
| Bilateral leg crampsMusculoskeletal and connective tissue disorders | 2/18 |
| Loose stoolsGastrointestinal disorders | 2/18 |
| Vaginal spottingReproductive system and breast disorders | 1/18 |
| Bilateral foot crampsMusculoskeletal and connective tissue disorders | 1/18 |
| Epigastric painGastrointestinal disorders | 1/18 |
| RestlessnessPsychiatric disorders | 1/18 |
All subjects enrolled
| Age, Continuous(years) | All Subjects |
|---|---|
| Mean | 33.4 ± 8.3 |
| Sex: Female, Male(Participants) | All Subjects |
|---|---|
| Female | 18 |
| Male | 0 |
| Region of Enrollment(participants) | All Subjects |
|---|---|
| United States | 18 |
This study is completed, as verified in Aug 2014. You cannot join it, but the record below documents what was studied.
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Repros Therapeutics Inc.