Healthy
Conditions
Keywords
Pharmacokinetics
Brief summary
Dose escalating study of 7 daily doses of Proellex at 100 mg, 150 mg and 200 mg
Detailed description
This is an open-label, single-center, outpatient, unblinded, multi-dose study of the safety and pharmacokinetic properties of Proellex®. Six female subjects will each receive seven daily doses of Proellex® in separate, rising doses. Dosing must be accomplished between menstrual periods. The first six women will complete the 100 mg visit schedule before the next six women will begin the 150 mg visit schedule. Blood will be collected at pre-dose, and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 5, 8, 12, 24 and 36 (Day 7 only) hrs post-dose on Day 1 and Day 7. Subjects will be allowed to leave the clinic between the 12 and 24 hr and the 24 and 36 hr PK blood draws. Subjects will be discharged from the study after a one month follow-up visit. Safety will be assessed throughout the study.
Interventions
DRUGProellex
Proellex 25 mg capsules 100 mg, 150 mg or 200mg daily for 7 days
Sponsors
Repros Therapeutics Inc.
Study design
Allocation
NON_RANDOMIZED
Intervention model
SINGLE_GROUP
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
FEMALE
Age
18 Years to 34 Years
Healthy volunteers
Yes
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
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| AUC Post Final Dose | 7 days | — |
| Cmax Post Final Dose | 7 days | To determine the safety and PK properties of 100 mg, 150 mg and 200 mg of Proellex® taken for seven days by healthy adult female subjects. |
Countries
United States
Participant flow
Participants by arm
| Arm | Count |
|---|---|
| Proellex 100 mg Proellex 100 mg daily for 7 days
Proellex: Proellex 25 mg capsules 100 mg, 150 mg or 200mg daily for 7 days | 7 |
| Proellex 150 mg Proellex 150 mg daily for 7 days
Proellex: Proellex 25 mg capsules 100 mg, 150 mg or 200mg daily for 7 days | 8 |
| Proellex 200 mg Proellex 200 mg daily for 7 days
Proellex: Proellex 25 mg capsules 100 mg, 150 mg or 200mg daily for 7 days | 10 |
| Total | 25 |
Withdrawals & dropouts
| Period | Reason | FG000 | FG001 | FG002 |
|---|---|---|---|---|
| Overall Study | Adverse Event | 0 | 0 | 3 |
| Overall Study | Other | 1 | 2 | 1 |
Baseline characteristics
| Characteristic | Total | Proellex 100 mg | Proellex 150 mg | Proellex 200 mg |
|---|---|---|---|---|
| Age, Categorical <=18 years | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Age, Categorical >=65 years | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
| Age, Categorical Between 18 and 65 years | 25 Participants | 7 Participants | 8 Participants | 10 Participants |
| Region of Enrollment United States | 25 participants | 7 participants | 8 participants | 10 participants |
| Sex: Female, Male Female | 25 Participants | 7 Participants | 8 Participants | 10 Participants |
| Sex: Female, Male Male | 0 Participants | 0 Participants | 0 Participants | 0 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk |
|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — |
| other Total, other adverse events | 6 / 7 | 6 / 8 | 6 / 10 |
| serious Total, serious adverse events | 0 / 7 | 0 / 8 | 0 / 10 |
Outcome results
Primary
AUC Post Final Dose
Time frame: 7 days
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Proellex 100 mg | AUC Post Final Dose | 57591 hour*ng/mL | Standard Deviation 70514 |
| Proellex 150 mg | AUC Post Final Dose | 137634 hour*ng/mL | Standard Deviation 146024 |
| Proellex 200 mg Caps | AUC Post Final Dose | 230731 hour*ng/mL | Standard Deviation 371463 |
| Proellex 200 mg Vials | AUC Post Final Dose | 190324 hour*ng/mL | Standard Deviation 95387 |
Primary
Cmax Post Final Dose
To determine the safety and PK properties of 100 mg, 150 mg and 200 mg of Proellex® taken for seven days by healthy adult female subjects.
Time frame: 7 days
| Arm | Measure | Value (MEAN) | Dispersion |
|---|---|---|---|
| Proellex 100 mg | Cmax Post Final Dose | 1944 ng/mL | Standard Deviation 625 |
| Proellex 150 mg | Cmax Post Final Dose | 3807 ng/mL | Standard Deviation 1670 |
| Proellex 200 mg Caps | Cmax Post Final Dose | 2293 ng/mL | Standard Deviation 1319 |
| Proellex 200 mg Vials | Cmax Post Final Dose | 2777 ng/mL | Standard Deviation 954 |