Proellex® Pharmacokinetic Bridging Study II

Study Overview
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Brief Summary
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An open-label, randomized, single-center, outpatient, unblinded, single-dose, three-way crossover study of the safety and PK properties of Proellex® in women ages 18 - 34 years.

Detailed Description
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This is an open-label, randomized, single-center, outpatient, unblinded, single-dose, three-way crossover study of the safety and PK properties of Proellex® in women ages 18 - 34 years. Twelve female subjects will each receive a single dose of Proellex®: 25 mg (fed state, formulation A), 25 mg (fed state, formulation B), and 25 mg (fasting state, formulation B); successive dosing will be separated by at least one week intervals from the previous dosing. Blood will be collected prior to taking the dose, and following the dose for 24 hours post-dose. Subjects will be discharged from the study after the last blood sample is obtained after the third dose of Proellex®. Safety will be assessed throughout the study.

Official Title
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Proellex® Pharmacokinetic Bridging Study II

Conditions
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Healthy

Intervention / Treatment
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* Drug: Proellex 25 mg formulation A
* Drug: Proellex 25 mg formulation B


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 on an Institutional Review Board (IRB)-approved form prior to the initiation of any study procedures. Subject must have signed and dated a written Informed Consent Form (ICF) before undergoing any study related activities, including discontinuation of any prohibited medications 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 In general good health Must have agreed to not attempt to become pregnant at any time during study participation or for 30 days thereafter Must not have used tobacco (nicotine products) for at least two years before the study starts Must have normal (or abnormal and clinically insignificant) laboratory values at screening Willing to remain in the clinic for the screening visit and for the treatment visits Available for all treatment and follow-up visits Willing to comply with all study procedures Additional inclusion criteria may apply Exclusion Criteria: Pregnant or lactating females or women who are attempting or expecting to become pregnant at any time during the study Past or present history of experiencing any allergic reaction to the formulations administered in this study, or in the opinion of the Principal Investigator, suggests an increased potential for an adverse hypersensitivity Any medical condition, which, in the judgment of the Principal Investigator, will prevent the subject from starting and/or completing the study Past or present history of any significant cardiovascular, renal, hepatic disease, thrombophlebitis, thromboembolic disorders, or cerebrovascular accident requiring ongoing medical therapy or clinical intervention A QTc interval of >450ms at screening Subject with abnormal screening visit vital signs or clinical laboratory evaluation considered clinically significant by the Principal Investigator Subjects with symptomatic uterine fibroids or endometriosis Use of other oral contraceptives or hormonal treatments within 30 days of first dose of study medication Use of a hormone-releasing intrauterine device Subject with a history of alcohol and/or drug abuse Known active infection of HIV, Hepatitis A, B or C Subject who has participated in a clinical trial with investigational medication within 30 days prior to study medication administration or who plans to take an experimental drug prior to the end of 30 days after participation in this study

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: Treatment
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: Formulation A Fed<br>Single dose of Proellex 25 mg formulation A, fed | Drug: Proellex 25 mg formulation A<br>* One Proellex 25 mg formulation A capsule<br>* Other names: Telapristonee acetate;|
| Experimental: Formulation B Fed<br>Single dose of Proellex 25 mg formulation B, fed | Drug: Proellex 25 mg formulation B<br>* One 25 mg Proellex capsule formulation B administered both fed and fasted<br>* Other names: Telapristone acetate;|
| Experimental: Formulation B Fasted<br>Single dose of Proellex 25 mg formulation B, fasted | Drug: Proellex 25 mg formulation B<br>* One 25 mg Proellex capsule formulation B administered both fed and fasted<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 (Cmax) of a single dose of Proellex® (25 mg) Formulation A using two different formulations of the drug in healthy adult female subjects with or without fasting | 24 hours | 
| AUC0-last of Proellex | Area under the plasma concentration curve from time 0 (AUC0-last) to the last measurable plasma concentration time point, up to 24 hours. | Up to 24 hours | 
| Tmax | Time to maximum plasma occurrence of Cmax | 24 hours | 
| 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 | 24 hours | 
| Terminal Elimination Half-life (T1/2) of Proellex | Time to maximum plasma occurrence of T1/2, calculated as ln(2)/Elimination rate constant. | 24 hours | 

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