Trial Outcomes & Findings for Open-Label, Multiple-Dose, Non-Randomized Study to Assess Drug-Drug Interactions of Proellex® in Female Subjects (NCT NCT00741468)
NCT ID: NCT00741468
Last Updated: 2014-08-22
Results Overview
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.
COMPLETED
PHASE1
18 participants
8 days
2014-08-22
Participant Flow
Participant milestones
| Measure |
All Participants
CYP1A2, Day 8 relative to Day 1 AUC (caffeine probe) CYP2C19, Day 8 relative to Day 1 AUC (omeprazole probe) CYP 2C9, Day 8 relative to Day 1 AUC (tolbutamide probe) CYP2D6, Day 8 relative to Day 1 AUC (dextromethorphan probe) CYP3A4, Day 8 relative to Day 1 AUC (midazolam probe)
|
|---|---|
|
Overall Study
STARTED
|
18
|
|
Overall Study
COMPLETED
|
18
|
|
Overall Study
NOT COMPLETED
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
Open-Label, Multiple-Dose, Non-Randomized Study to Assess Drug-Drug Interactions of Proellex® in Female Subjects
Baseline characteristics by cohort
| Measure |
All Subjects
n=18 Participants
Proellex 50 mg
Proellex: 2, 25 mg Proellex capsules administered daily
|
|---|---|
|
Age, Continuous
|
33.4 years
STANDARD_DEVIATION 8.3 • n=5 Participants
|
|
Sex: Female, Male
Female
|
18 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
0 Participants
n=5 Participants
|
|
Region of Enrollment
United States
|
18 participants
n=5 Participants
|
PRIMARY outcome
Timeframe: 8 daysPopulation: One subject had concentrations of Proellex (CDB-4124 and CDB-4453) that were below the lower level of quantitation at all time points tested and was excluded from the pharmacokinetic analyses.
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.
Outcome measures
| Measure |
CYP1A2
n=17 Participants
Day 8 relative to Day 1 AUC (caffeine probe)
|
CYP2C9
n=17 Participants
Day 8 relative to Day 1 AUC (tolbutamide probe)
|
CYP2C19
n=17 Participants
Day 8 relative to Day 1 AUC (omeprazole probe)
|
CYP2D6
n=17 Participants
Day 8 relative to Day 1 AUC (dextromethorphan probe)
|
CYP3A4
n=17 Participants
Day 8 relative to Day 1 AUC (midazolam probe)
|
|---|---|---|---|---|---|
|
Plasma AUC Ratio of Day 1 and Day 8
|
1.093 Ratio of geometric means Day 8 to Day 1
Interval 1.006 to 1.188
|
1.029 Ratio of geometric means Day 8 to Day 1
Interval 0.96 to 1.103
|
1.104 Ratio of geometric means Day 8 to Day 1
Interval 0.936 to 1.303
|
1.914 Ratio of geometric means Day 8 to Day 1
Interval 1.463 to 2.504
|
2.245 Ratio of geometric means Day 8 to Day 1
Interval 2.019 to 2.495
|
Adverse Events
All Subjects
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
All Subjects
n=18 participants at risk
Proellex 50 mg
Proellex: 2, 25 mg Proellex capsules administered daily
|
|---|---|
|
Reproductive system and breast disorders
Early menstruation
|
27.8%
5/18 • Number of events 5
|
|
Nervous system disorders
Headache
|
16.7%
3/18 • Number of events 3
|
|
Nervous system disorders
Dizziness
|
27.8%
5/18 • Number of events 5
|
|
Musculoskeletal and connective tissue disorders
Lower back pain
|
11.1%
2/18 • Number of events 2
|
|
Musculoskeletal and connective tissue disorders
Bilateral leg cramps
|
11.1%
2/18 • Number of events 2
|
|
Gastrointestinal disorders
Loose stools
|
11.1%
2/18 • Number of events 2
|
|
Reproductive system and breast disorders
Vaginal spotting
|
5.6%
1/18 • Number of events 1
|
|
Musculoskeletal and connective tissue disorders
Bilateral foot cramps
|
5.6%
1/18 • Number of events 1
|
|
Gastrointestinal disorders
Epigastric pain
|
5.6%
1/18 • Number of events 1
|
|
Psychiatric disorders
Restlessness
|
5.6%
1/18 • Number of events 1
|
|
Gastrointestinal disorders
Lower abdominal cramps
|
5.6%
1/18 • Number of events 1
|
|
Reproductive system and breast disorders
Menstrual cramps
|
5.6%
1/18 • Number of events 1
|
|
Musculoskeletal and connective tissue disorders
Back pain
|
5.6%
1/18 • Number of events 1
|
|
Gastrointestinal disorders
Heartburn
|
5.6%
1/18 • Number of events 1
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee Prior to publication, Investigator shall submit to the Sponsor a copy of any proposed publication. Sponsor shall have sixty (60) days to review the proposed publication for possible disclosure of Sponsor's Confidential Information and, upon request of Sponsor, Investigator shall delete any of Sponsor's Confidential Information or withhold submission of such publication to allow Sponsor to protect its intellectual property rights
- Publication restrictions are in place
Restriction type: OTHER