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Estriol and Trimegestone Dose-response Trial With Single Dose Application of Vaginal Rings

Registration Number
NCT03343912
Lead Sponsor
Galeno Desenvolvimento de Pesquisas Clínicas
Brief Summary

This clinical trial is performed as proof of pharmacological action investigation by demonstration of ovulation inhibition (dose-response study) under treatment with three Test vaginal rings releasing varying doses of estriol (E3) and trimegestone (TMG).

Blood samples for determination of estradiol (E2) and progesterone (PG) levels will serve as pharmacodynamic surrogate parameters for characterization of the treatment effect on the endogenous hormones.

Blood samples for determination of E3 and TMG in plasma will be collected in order to characterize pharmacokinetic parameters.

Additionally, local tolerability characterized by gynecological inspection of the vaginal mucosa prior to and after insertion of the Investigational Medicinal Product (IMPs) is planned to be assessed

Detailed Description

The IMPs, releasing either 0.400 mg E3 and 0.06 mg TMG, or 0.300 mg E3 and 0.12 mg TMG, or 0.200 mg E3 and 0.18 mg TMG per 24 h, will be applied intravaginally and remain in the vagina for the subsequent 21 days (single dose, 1 treatment cycle). A total of 36 female subjects, 12 per treatment group, are intended to be randomized.

Blood samples for determination of E2 and PG levels will be collected during treatment and until 20 days after removal of the ring. Blood samples for determination of E3 and TMG in plasma will be collected over the treatment period and until 48 h after removal of the ring.

Bleeding intensity will also be documented during treatment and until 20 days after removal of the vaginal ring in a diary to characterize the effects of the different treatments.

Recruitment & Eligibility

Status
COMPLETED
Sex
Female
Target Recruitment
36
Inclusion Criteria
  • Under treatment with a commercially available combined oral contraceptive containing 30 µg ethinylestradiol (EE) and 150 µg levonorgestrel (LVN) for the last 3 months prior to enrolment
  • Body-mass index (BMI): ≥ 18.5 kg/m² and ≤ 30.0 kg/m²
  • Good state of health
  • Non-smoker, ex-smoker for at least 3 months
  • Regular menstrual cycle with a length between 21 and 35 days
  • Written informed consent, after having been informed about benefits and potential risks of the clinical trial
Exclusion Criteria
  • Existing diseases or pathological findings, which might interfere with the safety or tolerability, and/or pharmacokinetics of the IMPs
  • Subjects with severe allergies or multiple drug allergies
  • Positive anti human immunodeficiency virus (anti-HIV) test, hepatitis B surface antigen (HBs-AG) test or anti hepatitis C virus (anti-HCV) test
  • Presence or history of venous or arterial thrombosis, cerebrovascular accident, or increased risk of thrombosis
  • Diabetes mellitus
  • Unclarified vaginal bleeding or frequent infections of the urogenital tract
  • Severe or chronic constipation
  • Presence or history of migraine
  • Drug or alcohol dependence
  • Blood donation or other blood loss of more than 400 ml within the last 3 months
  • Participation in a clinical trial during the last 6 months
  • Pregnant or lactating women
  • Subjects who do not agree to apply a barrier method for contraception

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Test 1 vaginal ringEstriol 0.400 mg/day and Trimegestone 0.06 mg/daySingle intravaginal application of 1 vaginal ring of Estriol 0.400 mg/day and Trimegestone 0.06 mg/day (Test 1) over 21 days
Test 2 vaginal ringEstriol 0.300 mg/day and Trimegestone 0.12 mg/daySingle intravaginal application of 1 vaginal ring of Estriol 0.300 mg/day and Trimegestone 0.12 mg/day (Test 2) over 21 days
Test 3 vaginal ringEstriol 0.200 mg/day and Trimegestone 0.18 mg/daySingle intravaginal application of 1 vaginal ring of Estriol 0.200 mg/day and Trimegestone 0.18 mg/day (Test 3) over 21 days
Primary Outcome Measures
NameTimeMethod
Measurement of E2 and PG plasma levels0 - 41 days

Blood sampling for the determination of plasma levels of E2 and PG, in participants of each treatment group, as surrogate variables for treatment response.

Measurement of E3 and TMG plasma levels0 - 23 days

Blood sampling for the determination of plasma levels of E3 and TMG, in participants of each treatment group.

Secondary Outcome Measures
NameTimeMethod
Bleeding intensitystart of treatment until 42 days after treatment

Bleeding intensity, graded as "no bleeding", "spotting" or "bleeding" as recorded in diary by the subject on a daily basis

Number of adverse events per participantup to 42 days after treatment

Number of adverse events, in each treatment group, including clinically relevant alterations of vital signs and laboratory tests results

Maximum Plasma Concentration (Cmax) of E3 and TMG0 - 23 days

Determination of Cmax for E3 and for TMG, based on plasma concentrations of samples obtained.

Area Under the Curve (AUC) for E3 and TMG0 - 23 days

Calculation of the AUC for E3 and for TMG, based on plasma concentrations of samples obtained

Trial Locations

Locations (1)

Galeno Desenvolvimento de Pesquisas Clinicas Ltda. - ME

🇧🇷

Campinas, SP, Brazil

Galeno Desenvolvimento de Pesquisas Clinicas Ltda. - ME
🇧🇷Campinas, SP, Brazil
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