Crossover Study of the Safety and PK Properties of Proellex®

Study Overview
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Brief Summary
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Study to evaluate the PK of 25 mg and 50 mg of Proellex from 2 different suppliers in the fed and fasting states.

Detailed Description
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This study is intended to evaluate the pharmacokinetic properties of two doses (25 mg and 50 mg) of Proellex® formulated with microcrystalline cellulose (MCC) from 2 different suppliers in the fed and fasting states.

Official Title
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A Phase I, Open-Label, Randomized, Single-Center, Unblinded, Single-Dose, Five-Way Crossover Study of the Safety and PK Properties of Proellex®

Conditions
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Pharmacokinetics

Intervention / Treatment
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* Drug: Proellex


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Subject must be able to speak, read, and understand English and be willing and able to provide written informed consent in English on an Institutional Review Board (IRB) Premenopausal women aged 18-34, inclusive, with body mass index between 18 and 35, inclusive Women of child-bearing potential must be willing to use effective non-hormonal, double-barrier method contraception during the study period and for a minimum of 30 days after discontinuation of the study medication. Women who have had a hysterectomy will be allowed into the study Must have a negative urine pregnancy test at screening Able to swallow gelatin capsules Medically normal subjects with no significant abnormal findings at the screening physical examination as evaluated by the Principal Investigator that would interfere with the subject participating this study Must have agreed to not attempt to become pregnant at any time during study participation or for 30 days thereafter Other inclusion criteria may apply Exclusion Criteria: Symptomatic uterine fibroids or endometriosis Past or present history of any significant cardiovascular, renal, or hepatic disease requiring ongoing medical therapy or clinical intervention Past or present history of thrombophlebitis, thromboembolic disorders, or cerebrovascular accident Abnormal screening visit vital signs or clinical laboratory evaluation considered clinically significant by the Principal Investigator Significant organ abnormality or disease (based on the Principal Investigator's judgment) that would in the opinion of the Principal Investigator exclude the subject from participating Other exclusion criteria may apply

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 34 Years

Sexes Eligible for Study
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Female

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Basic Science
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: 25 mg AMCC fed<br>25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fed State | Drug: Proellex<br>* 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<br>* Other names: Telapristone acetate;|
| Experimental: 25 mg AMCC fasting<br>25 mg Proellex capsule formulated with AMCC coarse microcrystalline cellulose Fasting State | Drug: Proellex<br>* 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<br>* Other names: Telapristone acetate;|
| Experimental: 50 mg AMCC fed<br>2, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fed State | Drug: Proellex<br>* 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<br>* Other names: Telapristone acetate;|
| Experimental: 50 mg AMCC fasting<br>2, 25 mg Proellex capsules formulated with AMCC coarse microcrystalline cellulose Fasting State | Drug: Proellex<br>* 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<br>* Other names: Telapristone acetate;|
| Experimental: 50 mg SMCC fasting<br>2, 25 mg Proellex capsules formulated with SMCC microcrystalline cellulose Fasting State | Drug: Proellex<br>* 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<br>* Other names: Telapristone acetate;|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Cmax of Proellex | Maximum observed concentration of Proellex | Up to 72 hours post-dose | 
| AUC0-last of Proellex | Area under the plasma concentration curve from time 0 to the last measurable plasma concentration time point, up to 72 hours. | Up to 72 hours post dose | 
| Tmax of Proellex | Time to maximum plasma occurrence of Cmax | Up to 72 hours post dose | 
| AUC0-infinity of Proellex | 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 | Up to 72 hours post dose | 
| Terminal Elimination Half-life (T1/2) of Proellex | Time to maximum plasma occurrence of T1/2, calculated as ln(2)/Elimination rate constant. | Up to 72 hours post dose | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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PK, Pharmacokinetics