Trial Outcomes & Findings for Evaluate the Safety and PK of Proellex® in Female Patients With Impaired Hepatic Function and Healthy Adults (NCT NCT00741273)

Last Updated: 2014-08-28

Results Overview

Cmax of a single dose of 25mg and 50mg of Proellex® in female patients with impaired hepatic function and in volunteers with normal hepatic function, assessed from samples collected at: 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 5, 7, 9, 12, 16, 20, 24, 32, 36, 40 and 48 hours post dose..

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

16 participants

Primary outcome timeframe

48 hours

Results posted on

2014-08-28

Participant Flow

Participant milestones

Participant milestones
Measure	Healthy Proellex single dose each of 25 mg and 50 mg in healthy females	Impaired Proellex single dose each of 25 mg and 50 mg in hepatically impaired females
Overall Study STARTED	8	8
Overall Study COMPLETED	8	8
Overall Study NOT COMPLETED	0	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Evaluate the Safety and PK of Proellex® in Female Patients With Impaired Hepatic Function and Healthy Adults

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	Healthy n=8 Participants Healthy females	Mpaired n=8 Participants Hepatically impaired females	Total n=16 Participants Total of all reporting groups
Age, Continuous	41.4 years STANDARD_DEVIATION 4.1 • n=5 Participants	54.1 years STANDARD_DEVIATION 4.8 • n=7 Participants	47.8 years STANDARD_DEVIATION 7.9 • n=5 Participants
Sex: Female, Male Female	8 Participants n=5 Participants	8 Participants n=7 Participants	16 Participants n=5 Participants
Sex: Female, Male Male	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants
Region of Enrollment United States	8 participants n=5 Participants	8 participants n=7 Participants	16 participants n=5 Participants

PRIMARY outcome

Timeframe: 48 hours

Outcome measures

Outcome measures
Measure	Proellex 25 mg Healthy n=8 Participants Proellex 25 mg in healthy females Proellex: Proellex 25 mg capsule, single dose	Proellex 25 mg Impaired n=8 Participants Proellex 50 mg in hepatically impaired females Proellex: Proellex 25 mg capsule, single dose	Proellex 50 mg Healthy n=8 Participants Proellex 50 mg in healthy females Proellex: Proellex 50 mg capsule, single dose	Proellex 50 mg Impaired n=8 Participants Proellex 50 mg in impaired females Proellex: Proellex 50 mg capsule, single dose
Maximum Blood Concentration (Cmax)	827.5 ng/L Standard Deviation 312.9	587.6 ng/L Standard Deviation 261.3	1589.5 ng/L Standard Deviation 482.3	974.0 ng/L Standard Deviation 400.2

PRIMARY outcome

Timeframe: 48 hours

Time for Proellex concentration to decrease by half (T1/2) of a single dose of 25mg and 50mg of Proellex® in female patients with impaired hepatic function and in volunteers with normal hepatic function,measured from samples collected at: 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 5, 7, 9, 12, 16, 20, 24, 32, 36, 40 and 48 hours post dose..

Outcome measures

Outcome measures
Measure	Proellex 25 mg Healthy n=8 Participants Proellex 25 mg in healthy females Proellex: Proellex 25 mg capsule, single dose	Proellex 25 mg Impaired n=8 Participants Proellex 50 mg in hepatically impaired females Proellex: Proellex 25 mg capsule, single dose	Proellex 50 mg Healthy n=8 Participants Proellex 50 mg in healthy females Proellex: Proellex 50 mg capsule, single dose	Proellex 50 mg Impaired n=8 Participants Proellex 50 mg in impaired females Proellex: Proellex 50 mg capsule, single dose
Proellex Half-life (T1/2)	24.5 Hours Standard Deviation 8.4	37.9 Hours Standard Deviation 18.9	24.2 Hours Standard Deviation 10.1	30.9 Hours Standard Deviation 10.8

SECONDARY outcome

Timeframe: 48 hours

AUC0-t of a single dose of 25mg and 50mg of Proellex® in female patients with impaired hepatic function and in volunteers with normal hepatic function, measured from samples collected at: 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 5, 7, 9, 12, 16, 20, 24, 32, 36, 40 and 48 hours post dose.

Outcome measures

Outcome measures
Measure	Proellex 25 mg Healthy n=8 Participants Proellex 25 mg in healthy females Proellex: Proellex 25 mg capsule, single dose	Proellex 25 mg Impaired n=8 Participants Proellex 50 mg in hepatically impaired females Proellex: Proellex 25 mg capsule, single dose	Proellex 50 mg Healthy n=8 Participants Proellex 50 mg in healthy females Proellex: Proellex 50 mg capsule, single dose	Proellex 50 mg Impaired n=8 Participants Proellex 50 mg in impaired females Proellex: Proellex 50 mg capsule, single dose
Area Under the Curve (AUC0-t) for Proellex	5147.2 ng x min/L Standard Deviation 2647.3	3603.1 ng x min/L Standard Deviation 1777.2	9062.4 ng x min/L Standard Deviation 4616.1	6988.6 ng x min/L Standard Deviation 3289.1

Adverse Events

Proellex Healthy

Serious events: 0 serious events

Other events: 4 other events

Deaths: 0 deaths

Proellex Impaired

Serious events: 0 serious events

Other events: 3 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure	Proellex Healthy n=8 participants at risk Proellex 25 mg and 50 mg in healthy females Proellex: Proellex 25 mg and 50 mg capsule, single dose each	Proellex Impaired n=8 participants at risk Proellex 25 mg and 50 mg in hepatically impaired females Proellex: Proellex 25 mg and 50 mg capsule, single dose each
Eye disorders Eye pruritis	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Eye disorders Eye swelling	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Eye disorders Vision blurred	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Gastrointestinal disorders Abdominal distension	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Gastrointestinal disorders Abdominal pain lower	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Gastrointestinal disorders Diarrhoea	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Gastrointestinal disorders Nausea	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Musculoskeletal and connective tissue disorders Arthralgia	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Nervous system disorders Dizziness	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Nervous system disorders Headache	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Psychiatric disorders Anxiety	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Reproductive system and breast disorders Breast tenderness	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Reproductive system and breast disorders Metrorrhagia	37.5% 3/8 • Number of events 3 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex
Skin and subcutaneous tissue disorders Acne	0.00% 0/8 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex	12.5% 1/8 • Number of events 1 Adverse events are reported together in each group for exposure to both 25mg Proellex and 50 mg Proellex

Additional Information

Jennifer Wike

Repros Therapeutics

Phone: 2817193402

Email: [email protected]

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
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