Proellex Pharmacokinetics Bridging Study

Healthy female subjects received a single dose of four different types of Proellex, the original 25 mg dose and three new formulations

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: 25 mg Proellex; Drug: 25 mg Proellex; Drug: 25 mg Proellex; Drug: 50 mg Proellex

Detailed Description

Healthy female subjects received a single dose of four different types of Proellex, the original 25 mg dose and three new formulations (24 and 50 mg dose). Blood was collected pre-dose, at specified intervals and 24 hours post dose. Each dose was separated by at least one week interval from the previous dose.

• Study Type: Interventional
• Enrollment (Actual): 21
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • San Antonio,, Texas, United States, 78209
      • Healthcare Discoveries, Inc

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 40 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Female

Description

Inclusion Criteria:

• Medically normal subjects with no significant abnormal findings at the screening physical examination as evaluated by the clinical Investigator
• Subject was willing to remain in the clinic for the screening visit; and for the treatment visits (day -1, day of treatment and day 1; approximately 36 hrs per treatment visit)

Exclusion Criteria:

• Post-menopausal women,
• Subject with documented endometriosis
• Subject with known uterine fibroids or vaginal polyps

Study Plan

How is the study designed?

Design Details

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

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Proellex Formulation 1; 25 mg Proellex Gelucire and PEG (original formulation)	Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (252 mg of Gelucire and 88 mg of PEG400, original formulation) [Original], single dose; Other Names: Telapristone acetate; CDB-4124; Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (coated with microcrystalline cellulose, new formulation) (coated), single dose; Other Names: CDB-4124; Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (blended with microcrystalline cellulose, new formulation) [Blended], single dose; Other Names: CDB-4124
Experimental: 25 mg Proellex Formulation 2; 25 mg Proellex coated with MCC	Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (252 mg of Gelucire and 88 mg of PEG400, original formulation) [Original], single dose; Other Names: Telapristone acetate; CDB-4124; Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (coated with microcrystalline cellulose, new formulation) (coated), single dose; Other Names: CDB-4124; Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (blended with microcrystalline cellulose, new formulation) [Blended], single dose; Other Names: CDB-4124
Experimental: 25 mg Proellex Formulation 3; 25 mg Proellex blended with MCC	Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (252 mg of Gelucire and 88 mg of PEG400, original formulation) [Original], single dose; Other Names: Telapristone acetate; CDB-4124; Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (coated with microcrystalline cellulose, new formulation) (coated), single dose; Other Names: CDB-4124; Drug: 25 mg Proellex; 25 mg - given as one 25 mg capsule (blended with microcrystalline cellulose, new formulation) [Blended], single dose; Other Names: CDB-4124
Experimental: 50 mg Proellex Formulation 3; 50 mg Proellex blended with MCC	Drug: 50 mg Proellex; 50 mg - given as two 25 mg capsules (blended with microcrystalline cellulose, new formulation) [Blended], single dose; Other Names: CDB-4124

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Proellex peak plasma concentration (Cmax)	24 hours
Proellex time to peak plasma concentration (tmax).	24 hours

Secondary Outcome Measures

Outcome Measure	Time Frame
The area under the plasma concentration over time curve from zero to the last measurable Proellex plasma concentration (AUC0-24) was calculated.	24 hours
The area under the plasma concentration over time curve from zero to infinity (AUC 0-infinity).	24 hours
Terminal elimination half-life (t1/2).	24 hours
Vital signs evaluated at screening, treatment days 0 and 1. Clinical laboratory values obtained at screening, treatment days 0 and 1. Adverse events assessed at treatment visits and followed until resolution.	24 hours

Collaborators and Investigators

• Sponsor: Repros Therapeutics Inc.
• Investigators: Study Director: Andre van As, PhD, MD, Repros Therapeutics Inc.

Study record dates

Study Major Dates

• Study Start: June 1, 2007
• Primary Completion (Actual): July 1, 2007
• Study Completion (Actual): July 1, 2007

Study Registration Dates

• First Submitted: February 10, 2010
• First Submitted That Met QC Criteria: February 10, 2010
• First Posted (Estimate): February 12, 2010

Study Record Updates

• Last Update Posted (Estimate): July 8, 2014
• Last Update Submitted That Met QC Criteria: July 3, 2014
• Last Verified: July 1, 2014

More Information

Terms related to this study

• Keywords: Pharmacokinetics
• Other Study ID Numbers: ZP-001