NCT02807363

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

A Randomized, Open-label, Parallel-group, Active-control PK/PD Study of Three Doses of Leuprolide Oral Tablets in Comparison to an IM Dose of Leuprolide in Healthy Female Volunteers

• Status: Completed
• Phase: Phase 2
• Study type: Interventional
• Enrollment: 35 (actual)
• Sponsor: Enteris BioPharma Inc. · Industry
• Sex: Female
• Age: 18 Years – 49 Years
• Healthy volunteers: Accepted

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.

Detailed description

Site initiation visit of the study site, InVentiv Health Clinique, Inc. by on-site visit and teleconference was done and the final report signed 21st July 2017. For the demographic and baseline characteristics descriptive statistics consisting of mean, median, standard deviation, minimum, maximum and sample size is reported for continuous variables like age, body mass index, weight and height. categorical variables like ethnicity, gender and race is presented as frequency counts and percentages. For PK analysis, Steady state concentration level of leuprolide calculated for oral tablets (Treatments A and B) at the end of the fourth treatment week (Treatment Days 28) as the 24-hour AUCs divided by the duration of the dosing interval i.e., 24 hours. For PD analysis, subject incidence of estradiol level below 40 pg/mL was assessed. The ovulation rate determined by the extent of progesterone suppression is presented. Only observed data is used in the data analysis except for concentration values below the lower limit of quantitation (BLQ) and samples with no reportable value occurring prior to dosing (on Day 1 only). No attempt is made to impute (i.e., extrapolate or interpolate) estimates for missing data. For safety analysis, incidence of treatment emergent adverse events both during the dosing and post dosing period is presented. The Medical Dictionary for Regulatory Activities (MedDRA®) Version 20.1 is used to classify all medical history findings and incidences of treatment emergent adverse events (TEAE) reported during the study by System Organ Class (SOC) and Preferred Term (PT).

Conditions

• Endometriosis

Interventions

Type	Name	Description
DRUG	Leuprolide Oral Tablet 4-mg QD	4-mg Leuprolide oral tablet once daily for 28 consecutive days.
DRUG	Leuprolide Oral Tablet 4-mg BID	4-mg Leuprolide oral tablet twice daily for 28 consecutive days.
DRUG	Leuprolide Depot	3.75 mg intramuscular depot injection
DRUG	Leuprolide Oral Tablet 10-mg BID	10-mg Leuprolide oral tablet twice daily for 28 consecutive days.

Timeline

• Start date: 2017-08-23
• Primary completion: 2018-06-27
• Completion: 2018-06-27
• First posted: 2016-06-21
• Last updated: 2022-02-11
• Results posted: 2022-02-11

Locations

1 site across 1 country: Canada

Regulatory

• FDA-regulated drug study