Crossover Study of the Safety and PK Properties of Proellex®

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

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

Study Overview

• Status: Completed
• Conditions: Pharmacokinetics
• Intervention / Treatment: Drug: Proellex

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Actual): 17
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • San Antonio, Texas, United States, 78229
      • Healthcare Discoveries Inc.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 34 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Female

Description

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

Study Plan

How is the study designed?

Design Details

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

Number of Arms

5

Arms and Interventions

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

What is the study measuring?

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

Collaborators and Investigators

• Sponsor: Repros Therapeutics Inc.

Study record dates

Study Major Dates

• Study Start (Actual): August 11, 2008
• Primary Completion (Actual): October 23, 2008
• Study Completion (Actual): October 23, 2008

Study Registration Dates

• First Submitted: September 5, 2008
• First Submitted That Met QC Criteria: September 5, 2008
• First Posted (Estimate): September 9, 2008

Study Record Updates

• Last Update Posted (Actual): April 29, 2019
• Last Update Submitted That Met QC Criteria: January 23, 2019
• Last Verified: January 1, 2019

More Information

Terms related to this study

• Keywords: Pharmacokinetics; PK
• Other Study ID Numbers: ZP-008

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No