CompletedPhase 2

A Study of Pharmacokinetic/Pharmacodynamic Profile of Orally Administered Leuprolide in Healthy Female Volunteers

Canada35 participantsStarted 2017-08-23

Plain-language summary

This Phase 2a, pharmacokinetic/pharmacodynamic study will determine the safety and provide evaluation of the PK/PD metrics of three different oral doses selected upon the results of the study LOPDT-PH1-01 - 4 mg oral tablets administered over 28 days as QD and BID regimens and 10 mg oral tablets administered over 28 days as a BID regimen. The PK/PD profiles of the study drug will be compared to the leuprolide formulation approved for the treatment of endometriosis (a monthly intramuscular injection, Lupron Depot 3.75 mg). Major PK (e.g., a total exposure to leuprolide) and PD parameters (e.g., rates of the estradiol suppression and cessation of the menstrual period) will also be evaluated against the Lupron Depot historical data.

Who can participate

Age range18 Years – 49 Years

SexFEMALE

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AI-rewrites the medical criteria so a patient or caregiver can understand them. Always confirm with the trial site.

Inclusion criteria

✓. Healthy premenopausal female volunteers, aged 18 to 49 years;
✓. Body mass index (BMI) ≥ 18 and ≤ 32 kg/m2, and weight ≥ 110 lb (approximately 50 kg);
✓. Regular menstrual cycles with a usual length ranging from 21 days to 35 days. If subject had recently used hormonal birth control, historical data prior to use were used to determine qualification and must also meet this criterion;
✓. If of childbearing potential and sexually active with a risk of pregnancy, willing to use one of the following acceptable methods of contraception throughout the study and for at least 30 days after the last drug administration:
✓. intrauterine contraceptive device (IUD) without hormone release system placed at least 4 weeks prior to the first study drug administration with simultaneous use of condom for the male partner;
✓. simultaneous use of diaphragm with intravaginally applied spermicide and condom for the male partner starting at least 14 days prior to drug administration;
✓. sterile male partner (vasectomized for at least 6 months); Note: Surgically sterile subjects who have had a tubal ligation were considered of non-childbearing potential and were not required to use contraception;
✓. Willing to refrain from excessive use of alcohol during the entire study and willing to refrain from use of alcohol 24 hours prior to any PK blood draw taken during the study;

What they're measuring

Number of Participants With Adequacy of Suppression of Estradiol (E2) as Assessed by Estradiol Level Below 40 pg/mL

Timeframe: Dosing Period: Day 8 to 28, Post-dosing: Day 1 to day 28 of post dosing period; Day 29 is the post dosing day 1

Ovulation Rate - Measured by Number of Subjects With Progesterone Levels Not Less Than 3000 pg/mL

Timeframe: Dosing period: Day 1 to Day 28 and 28 day Post-Dosing Period; 29 day is post dosing day 1

Number of Subjects Who Experienced Treatment Emergent Adverse Events (TEAE) Excluding Menstrual Disorders

Timeframe: Dosing Period: Day 1 to day 28

Number of Subjects Who Experienced Treatment-Emergent Adverse Events (TEAEs), Excluding Menstrual Disorders

Timeframe: Post dosing period (starting day 1 to day 28 post dosing period)

Steady State Concentration Level, (Css) of Leuprolide

Timeframe: Treatment Day 28 for oral groups; Treatment Days 22-29 for Lupron Depot group

Trial details

NCT IDNCT02807363

SponsorEnteris BioPharma Inc.

Sponsor typeINDUSTRY

Study typeINTERVENTIONAL

Primary completion2018-06-27

Results submitted2021-10-27

View on ClinicalTrials.gov More Endometriosis trials

Plain-language summary

Who can participate

Age range18 Years – 49 Years

SexFEMALE

See this in plain English?

AI-rewrites the medical criteria so a patient or caregiver can understand them. Always confirm with the trial site.

Inclusion criteria

✓. Healthy premenopausal female volunteers, aged 18 to 49 years;
✓. Body mass index (BMI) ≥ 18 and ≤ 32 kg/m2, and weight ≥ 110 lb (approximately 50 kg);
✓. Regular menstrual cycles with a usual length ranging from 21 days to 35 days. If subject had recently used hormonal birth control, historical data prior to use were used to determine qualification and must also meet this criterion;
✓. If of childbearing potential and sexually active with a risk of pregnancy, willing to use one of the following acceptable methods of contraception throughout the study and for at least 30 days after the last drug administration:
✓. intrauterine contraceptive device (IUD) without hormone release system placed at least 4 weeks prior to the first study drug administration with simultaneous use of condom for the male partner;
✓. simultaneous use of diaphragm with intravaginally applied spermicide and condom for the male partner starting at least 14 days prior to drug administration;
✓. sterile male partner (vasectomized for at least 6 months); Note: Surgically sterile subjects who have had a tubal ligation were considered of non-childbearing potential and were not required to use contraception;
✓. Willing to refrain from excessive use of alcohol during the entire study and willing to refrain from use of alcohol 24 hours prior to any PK blood draw taken during the study;

What they're measuring

Number of Participants With Adequacy of Suppression of Estradiol (E2) as Assessed by Estradiol Level Below 40 pg/mL

Timeframe: Dosing Period: Day 8 to 28, Post-dosing: Day 1 to day 28 of post dosing period; Day 29 is the post dosing day 1

Ovulation Rate - Measured by Number of Subjects With Progesterone Levels Not Less Than 3000 pg/mL

Timeframe: Dosing period: Day 1 to Day 28 and 28 day Post-Dosing Period; 29 day is post dosing day 1

Number of Subjects Who Experienced Treatment Emergent Adverse Events (TEAE) Excluding Menstrual Disorders

Timeframe: Dosing Period: Day 1 to day 28

Number of Subjects Who Experienced Treatment-Emergent Adverse Events (TEAEs), Excluding Menstrual Disorders

Timeframe: Post dosing period (starting day 1 to day 28 post dosing period)

Steady State Concentration Level, (Css) of Leuprolide

Timeframe: Treatment Day 28 for oral groups; Treatment Days 22-29 for Lupron Depot group

A Study of Pharmacokinetic/Pharmacodynamic Profile of Orally Administered Leuprolide in Healthy Female Volunteers

Plain-language summary

Who can participate

Inclusion criteria

What they're measuring

Trial details

A Study of Pharmacokinetic/Pharmacodynamic Profile of Orally Administered Leuprolide in Healthy Female Volunteers

Plain-language summary

Who can participate

Inclusion criteria

What they're measuring

Trial details

Exclusion criteria