NDLI: Effect of mavoglurant (AFQ056), a selective mGluR5 antagonist, on the pharmacokinetics of a combined oral contraceptive containing ethinyl estradiol and levonorgestrel in healthy women.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Sivasubramanian, Rama Chakraborty, Abhijit Rouzade-Dominguez, Marie-Laure Neelakantham, Srikanth Jakab, Annamaria Mensinga, Tjeert Legangneux, Eric Woessner, Ralph Ufer, Mike
Abstract	OBJECTIVE: To compare the pharmacokinetics (PKs) of a combination oral contraceptive (OC) when given alone or concomitantly with the selective metabotropic glutamate receptor 5 antagonist mavoglurant (AFQ056). METHODS: This open-label, fixed-sequence, two-period study included 30 healthy female subjects aged 18-40 years. In period 1, a single oral dose of an OC containing 30 µg ethinyl estradiol (EE)/150 µg levonorgestrel (LNG) was administered alone. In period 2, the OC was administered with a clinically relevant multiple dose of mavoglurant 100 mg b.i.d. under steady-state conditions. Plasma concentrations of EE and LNG were measured up to 72 hours post administration, and the PK parameters Cmax and AUClast were estimated using noncompartmental methods. RESULTS: The geometric mean ratios of EE Cmax and AUClast obtained with and without mavoglurant were 0.97 (90% confidence interval (CI): 0.90-1.06) and 0.94 (90% CI: 0.86-1.03), respectively. The corresponding Cmax and AUClast for LNG were 0.81 (90% CI: 0.75-0.87) and 0.68 (90% CI: 0.63-0.73), respectively. CONCLUSIONS: In conclusion, EE PK was unchanged, whereas Cmax and AUClast of LNG were 19% and 32% lower, respectively, when given with mavoglurant Further investigation regarding the impact on contraceptive efficacy is warranted.
File Format	HTM / HTML
ISSN	09461965
Issue Number	7
Volume Number	53
Journal	Int. Journal of Clinical Pharmacology and Therapeutics
Language	English
Publisher	Dustri-Verlag
Publisher Date	2015-07-01
Publisher Place	Germany
Access Restriction	Subscribed
Subject Keyword	Discipline Pharmacology Contraceptives, Oral, Combined Pharmacokinetics Contraceptives, Oral, Hormonal Ethinyl Estradiol Excitatory Amino Acid Antagonists Administration & Dosage Indoles Levonorgestrel Receptor, Metabotropic Glutamate 5 Antagonists & Inhibitors Administration, Oral Adolescent Adult Area Under Curve Adverse Effects Blood Drug Interactions Female Healthy Volunteers Humans Metabolic Clearance Rate Models, Biological Young Adult Clinical Trial Journal Article Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Pharmacology Pharmacology (medical)

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