Clinical Study Investigating the Conversion of the Contraceptive Compound Norethisterone Within the Body Towards the Contraceptive Compound Ethinylestradiol

Open Label, One-way Crossover Study to Assess the in Vivo Formation of Ethinylestradiol Following Single Intramuscular Administration of 200 mg Norethisterone Enantate Compared to Ethinylestradiol Pharmacokinetics After Multiple Doses of a Combined Oral Contraceptive Containing Ethinylestradiol and Levonorgestrel in Healthy Premenopausal Women

The clinical phase I study aims at investigating the conversion of the contraceptive compound norethisterone within the body towards the contraceptive compound ethinylestradiol. Therefore concentrations of ethinylestradiol will be measured from blood samples after administration of a single intramuscular dose of norethisterone. In a comparison arm concentrations of ethinylestradiol will be measured from blood samples after administration of a pill containing ethinylestradiol itself.

Study Overview

• Status: Completed
• Conditions: Pharmacokinetics
• Intervention / Treatment: Drug: Microgynon; Drug: Noristerat(BAY86-6308)

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Berlin, Germany, 13353

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 45 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: Female

Description

Inclusion Criteria:

• Healthy female subject
• Age: 18 to 45 years (inclusive) at the first screening examination / visit
• Body mass index (BMI): above or equal 18 and below or equal 30 kg / m²
• At least 3 months since delivery, abortion, or lactation before the first screening examination / visit

Exclusion Criteria:

• - Incompletely cured pre-existing diseases for which it can be assumed that the absorption, distribution, metabolism, elimination and effects of the study drugs will not be normal
• Liver diseases, kidney diseases, metabolic disorders, thyroid disorders and known or suspected malignant or benign tumors
• Presence or a history of venous or arterial thrombotic/thromboembolic events
• Migraine with neurologic symptoms (complicated migraine)
• Clinically significant depression
• Pancreatitis or a history thereof if associated with severe hypertriglyceridemia
• Use of systemic or topical medicines or substances which oppose the study objectives or which might influence them

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Arm 1; Healthy premenopausal subjects will receive multiple oral doses of Microgynon for 21days	Drug: Microgynon; Subjects will receive 21 daily oral doses of Microgynon tablets containing 0.15 mg levonorgestrel und 0.03 mg ethinylestradiol.
Experimental: Arm 2; Healthy premenopausal subjects will receive a single intramuscular dose of Noristerat	Drug: Noristerat(BAY86-6308); Subjects will receive one intramuscular dose of Noristerat (oily solution for intramuscular injection) containing 200 mg norethisterone enantate.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Maximum observed drug concentration of ethinylestradiol at steady state after multiple administrations of Microgynon (Cmax)ss	At different time points on day 21
Area under the concentration-time curve of ethinylestradiol at steady state after multiple administrations of Microgynon {AUC(0-24)}ss	At different time points on day 21
Maximum observed drug concentration of ethinylestradiol after single administration of Noristerat (Cmax)	At different time points upto 8 weeks
Area under the concentration-time curve of ethinylestradiol after single administration of Noristerat (AUC)	At different time points up to 8 weeks
Maximum observed drug concentration of Norethisterone after single administration of Noristerat (Cmax)	At different time points up to 8 weeks
Area under the concentration-time curve of Norethisterone after single administration of Noristerat (AUC)	At different time points up to 8 weeks

Collaborators and Investigators

• Sponsor: Bayer

Study record dates

Study Major Dates

• Study Start: June 1, 2014
• Primary Completion (Actual): December 1, 2014
• Study Completion (Actual): March 1, 2015

Study Registration Dates

• First Submitted: June 20, 2014
• First Submitted That Met QC Criteria: June 20, 2014
• First Posted (Estimate): June 23, 2014

Study Record Updates

• Last Update Posted (Estimate): February 18, 2016
• Last Update Submitted That Met QC Criteria: February 17, 2016
• Last Verified: February 1, 2016

More Information

Terms related to this study

• Keywords: Drug Kinetics
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Contraceptive Agents, Hormonal; Contraceptive Agents; Reproductive Control Agents; Contraceptives, Oral, Combined; Contraceptives, Oral; Contraceptive Agents, Female; Contraceptives, Oral, Synthetic; Contraceptives, Oral, Hormonal; Contraceptives, Postcoital, Synthetic; Contraceptives, Postcoital; Contraceptives, Postcoital, Hormonal; Ethinyl estradiol, levonorgestrel drug combination; Ethinyl Estradiol-Norgestrel Combination
• Other Study ID Numbers: 17004; 2013-005280-89 (EudraCT Number)