Trial Outcomes & Findings for Crossover Study of the Safety and PK Properties of Proellex® (NCT NCT00749879)

NCT ID: NCT00749879

Last Updated: 2019-04-29

Results Overview

Maximum observed concentration of Proellex

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

17 participants

Primary outcome timeframe

Up to 72 hours post-dose

Results posted on

2019-04-29

Participant Flow

Of the 17 participants, 4 did not meet inclusion/exclusion criteria, and 1 participant enrolled as a spare was not needed, resulting in their involvement in the study being terminated. The remaining 12 participants completed all five study treatments of Proellex.

Each of the 12 participants were randomly assigned a unique sequence of the following 5 following open-label treatments of Proellex * 25 mg formulated with AMCC (fed state) * 25 mg formulated with AMCC (fasting state) * 50 mg formulated with AMCC (fed state) * 50 mg formulated with AMCC (fasting state) * 50 mg formulated with SMCC (fasting state)

Participant milestones

Participant milestones
Measure	Proellex in randomly assigned sequences, all study participants received 5 open-label treatments of Proellex: 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fed State Proellex; 25 mg capsule administered once orally after subjects have been fed; 25 mg capsule administered once orally while subjects are fasting; 2, 25 mg capsules administered once orally after subjects have been fed; 2, 25 mg capsules administered once orally while subjects are fasting; and 2, 25 mg capsules administered once orally while subjects are fasting
Overall Study STARTED	12
Overall Study COMPLETED	12
Overall Study NOT COMPLETED	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

Crossover Study of the Safety and PK Properties of Proellex®

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure	All Subjects n=12 Participants All subjects enrolled
Age, Categorical <=18 years	0 Participants n=99 Participants
Age, Categorical Between 18 and 65 years	12 Participants n=99 Participants
Age, Categorical >=65 years	0 Participants n=99 Participants
Sex: Female, Male Female	12 Participants n=99 Participants
Sex: Female, Male Male	0 Participants n=99 Participants
Region of Enrollment United States	12 Participants n=99 Participants

PRIMARY outcome

Timeframe: Up to 72 hours post-dose

Population: 12 subjects received all 5 treatments

Maximum observed concentration of Proellex

Outcome measures

Outcome measures
Measure	25 mg AMCC Fed n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fed State	25 mg AMCC Fasting n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg AMCC Fed n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fed State	50 mg AMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg SMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with SMCC microcrystalline cellulose Fasting State
Cmax of Proellex	485.6 ng/mL Standard Deviation 151.3	876.7 ng/mL Standard Deviation 201.9	912.9 ng/mL Standard Deviation 157.6	1322.5 ng/mL Standard Deviation 154.5	1346.7 ng/mL Standard Deviation 148.5

PRIMARY outcome

Timeframe: Up to 72 hours post dose

Population: All 12 subjects received each treatment

Area under the plasma concentration curve from time 0 to the last measurable plasma concentration time point, up to 72 hours.

Outcome measures

Outcome measures
Measure	25 mg AMCC Fed n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fed State	25 mg AMCC Fasting n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg AMCC Fed n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fed State	50 mg AMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg SMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with SMCC microcrystalline cellulose Fasting State
AUC0-last of Proellex	6142.1 ng/mL*hour Standard Deviation 2845.9	5765.7 ng/mL*hour Standard Deviation 3036.6	11094.2 ng/mL*hour Standard Deviation 4209.0	9252.0 ng/mL*hour Standard Deviation 4217.5	9576.2 ng/mL*hour Standard Deviation 4328.3

PRIMARY outcome

Timeframe: Up to 72 hours post dose

Population: All 12 subjects received each treatment

Time to maximum plasma occurrence of Cmax

Outcome measures

Outcome measures
Measure	25 mg AMCC Fed n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fed State	25 mg AMCC Fasting n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg AMCC Fed n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fed State	50 mg AMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg SMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with SMCC microcrystalline cellulose Fasting State
Tmax of Proellex	2.6 Hours Standard Deviation 0.6	0.8 Hours Standard Deviation 0.2	2.6 Hours Standard Deviation 1.0	0.9 Hours Standard Deviation 0.4	0.7 Hours Standard Deviation 0.2

PRIMARY outcome

Timeframe: Up to 72 hours post dose

Population: All 12 subjects received each treatment

Area under the plasma concentration curve from time 0 to extrapolated to infinity, calculated by summing the area under the curve from time zero to the time of the last quantifiable concentration

Outcome measures

Outcome measures
Measure	25 mg AMCC Fed n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fed State	25 mg AMCC Fasting n=12 Participants 25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg AMCC Fed n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fed State	50 mg AMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fasting State	50 mg SMCC Fasting n=12 Participants Two, 25 mg Proellex capsules formulated with SMCC microcrystalline cellulose Fasting State
AUC0-infinity of Proellex	7039.8 ng/mL*hour Standard Deviation 3715.6	6897.0 ng/mL*hour Standard Deviation 4440.7	13014.9 ng/mL*hour Standard Deviation 6753.2	11271.6 ng/mL*hour Standard Deviation 6726.6	11804.8 ng/mL*hour Standard Deviation 7186.9

PRIMARY outcome

Timeframe: Up to 72 hours post dose

Population: All 12 subjects received each treatment

Time to maximum plasma occurrence of T1/2, calculated as ln(2)/Elimination rate constant.