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"E4/DRSP Endocrine Function, Metabolic Control and Hemostasis Study"

Phase 1
Completed
Conditions
Liver Metabolism
Contraception
Hemostasis Parameter
Interventions
Drug: 15 mg E4/3 mg DRSP
Drug: 30 mcg EE/150 mcg LNG
Drug: 20 mcg EE/3 mg DRSP
Registration Number
NCT02957630
Lead Sponsor
Estetra
Brief Summary

The proposed study will provide an assessment of the effect of this combination on endocrine function, metabolic control and hemostasis during 6 treatment cycles. This will be compared to the effects of two reference COCs.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Female
Target Recruitment
101
Inclusion Criteria
  • Healthy adult woman
  • Negative pregnancy test at subject screening and randomization
  • Aged 18-50 years (inclusive) at the time of signing the ICF
  • Good physical and mental health on the basis of medical, surgical and gynecological history, physical examination, gynecological examination, clinical laboratory, ECG, echocardiography and vital signs
  • BMI from 18.0 to 30.0 kg/m², inclusive, at time of screening visit
  • Able to fulfil the requirements of the protocol and have indicated a willingness to participate in the study by providing written informed consent
Exclusion Criteria
  • Known hypersensitivity to any of the investigational product ingredients
  • Smoking if > 35 years old
  • Dyslipoproteinemia or use of antilipidemic agent
  • Known diabetes mellitus
  • Current use of antidiabetic drugs, including insulin
  • Arterial hypertension
  • Any condition associated with an increased risk of venous thromboembolism and/or arterial thromboembolism.
  • Any condition associated with abnormal uterine/vaginal bleeding.
  • Presence of an undiagnosed breast mass
  • Current symptomatic gallbladder disease
  • History of pregnancy- or COC-related cholestasis
  • Presence or history of severe hepatic disease
  • Presence or history of pancreatitis if associated with hypertriglyceridemia
  • Porphyria
  • Presence or history of benign liver tumors (focal nodular hyperplasia and hepatocellular adenoma)
  • Presence of renal impairment (glomerular filtration rate [GFR] <60 mL/min/1.73m²)
  • Hyperkalemia or presence of conditions that predispose to hyperkalemia
  • Presence or history of hormone-related malignancy
  • History of non-hormone-related malignancy within 5 years before screening; subjects with a non-melanoma skin cancer are allowed in the study
  • Use of drugs potentially triggering interactions with COCs
  • History of alcohol or drug abuse within 12 months prior to screening
  • Presence or history of thyroid disorders
  • Participation in another investigational drug clinical study within 1 month (30 days) or have received an investigational drug within the last 3 months (90 days) prior to randomization. Subjects who participated in an oral contraceptive clinical study using Food and Drug Administration (FDA)/European Union (EU) approved active ingredients, may be randomized 2 months (60 days) after completing the preceding study
  • Sponsor, contract research organization (CRO) or Principal Investigator's (PI's) site personnel directly affiliated with this study
  • Is judged by the PI to be unsuitable for any reason

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
15 mg E4/3 mg DRSP15 mg E4/3 mg DRSP15 mg estetrol/3 mg drospirenone combined oral contraceptive
30 mcg EE/150 mcg LNG30 mcg EE/150 mcg LNG30 mcg ethinylestradiol/150 mcg levonorgestrel combined oral contraceptive
20 mcg EE/3 mg DRSP20 mcg EE/3 mg DRSP20 mcg ethinylestradiol/3 mg drospirenone combined oral contraceptive
Primary Outcome Measures
NameTimeMethod
Serum concentration of C-peptideAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of glycated hemoglobin (HbA1c)At screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Oral glucose tolerance test (OGTT)At 0 (pre-glucose challenge), 30, 60, 90, 120 and 180 minutes after glucose challenge during pretreatment Cycle; at 0 (pre-glucose challenge), 30, 60, 90, 120 and 180 minutes after glucose challenge during Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of follicle-stimulating hormone (FSH)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of free thyroxine (fT3)/free triiodothyronine (fT4)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of thyroxin binding globulin (TBG)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of factor IIBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of E-selectinBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of fibrinogenBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of glucoseAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of thyroïd stimulating hormone (TSH)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of triglyceridesAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of lipoprotein (a)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of factor VIIBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of factor VIIIBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of von Willebrand factorBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of antithrombinBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of free and total Protein SBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of plasminogen activator inhibitor type-1 (PAI-1)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of tissue type plasminogen activator (t-PA)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of plasminogenBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of insulinAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for Cycles 3 and 6 (1 cycle = 28 days).
Homeostasis Model Assessment - Insulin Resistance (HOMA-IR)At screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of D-dimerBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of protein CBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of total cortisolBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of aldosteroneBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of prothrombin fragment 1+2Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of APC resistance (ETP-based, APTT-based)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Plasma concentration of free tissue factor pathway inhibitor (TPFI)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of prolactinBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of luteinizing hormone (LH)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of estradiol (E2)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of progesterone (P)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of dihydroepiandrostenedione (DHEAS)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of androstenedioneBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of apoliporotein A1Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of dihydrotestosterone (DHT)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of high density lipoprotein (HDL)-cholesterolAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of C-reactive proteinBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of corticosteroid binding globulin (CBG)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of total testosterone (T)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of low density lipoprotein (LDL)-cholesterolAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of total cholesterolAt screening, between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of apoliporotein BBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of sex hormone binding globulin (SHBG)Between Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Serum concentration of angiotensinogenBetween Days 18 and 21 for the pretreatment Cycle, and between Days 18 and 21 for the Cycles 3 and 6 (1 cycle = 28 days).
Secondary Outcome Measures
NameTimeMethod
Serum concentration of lactate dehydrogenase (LDH) 1 and 2Between Days 18 and 21 for the pretreatment Cycle and between Days 18 and 21 for the Cycle 6 (1 cycle = 28 days)
Serum concentration of tropinin T and IBetween Days 18 and 21 for the pretreatment Cycle and between Days 18 and 21 for the Cycle 6 (1 cycle = 28 days)
Number of subjects with adverse events as a measure of safety and tolerabilityFrom up to 28 days before randomization to maximum Day 4 of the Cycle 7 (1 cycle = 28 days).
Electrocardiogram (ECG) parametersAt screening and between Days 18 and 21 for Cycle 6 (1 cycle = 28 days).

The following ECG parameters will be recorded: heart rate, PR-interval, QRS-duration, QT-interval, QTc interval (Fridericias's)

Echocardiographic parametersAt screening and between Days 18 and 21 for Cycle 6 (1 cycle = 28 days).
Change from baseline to end of treatment in the different items of the menstrual distress questionnaires (MDQ) form CAt pretreatment Cycle and between Days 18 and 21 for Cycle 6 (1 cycle = 28 days).

Trial Locations

Locations (1)

Dinox BV

🇳🇱

Groningen, Netherlands

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