Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women
| Autor: | Ermer James C, Deborah Foss, Ferron Geraldine M, Gayle P. Orczyk, Jody L. Bapst |
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| Rok vydání: | 2006 |
| Předmět: |
Agonist
Adult medicine.medical_specialty medicine.drug_class Pharmacology Placebo Gastroenterology Cohort Studies Pharmacokinetics Double-Blind Method Oral administration Internal medicine Progesterone receptor Medicine Humans Pyrroles Adverse effect Dose-Response Relationship Drug business.industry Obstetrics and Gynecology Benzoxazines Reproductive Medicine Tanaproget Pharmacodynamics Area Under Curve Cervix Mucus Female business Receptors Progesterone Contraceptives Oral Half-Life |
| Zdroj: | Contraception. 74(5) |
| ISSN: | 0010-7824 |
| Popis: | Objective This study aimed to evaluate the pharmacokinetics, pharmacodynamics and safety of the nonsteroidal progesterone receptor agonist, tanaproget. Methods A randomized, double-blind, placebo-controlled, sequential-group study of ascending single doses of tanaproget was conducted in healthy, 25- to 45-year-old women on cycle days 8 to 12. Eight subjects (six active, two placebo) per cohort received a dose of 0.1, 0.3, 1, 3, 7 (��high-fat meal) or 15 mg. Results The maximum concentration ( C max ) of tanaproget occurred approximately 2 to 3 h after administration. The elimination half-life ( t 1/2 ) ranged from 12 to 30 h, and the oral clearance was approximately 70 L/h. The pharmacokinetics of tanaproget was not noticeably altered with a high-fat meal. All doses of tanaproget decreased cervical mucus scores (using a modified Insler method), indicating poor production and poor quality of cervical mucus. The most frequent treatment-emergent adverse events were vaginal bleeding/spotting, abdominal cramping and vomiting; their incidence was not dose related and most events were mild. Conclusions Tanaproget was safe and well tolerated, decreased cervical mucus scores and had a pharmacokinetic profile acceptable for use as a once-daily oral contraceptive. |
| Databáze: | OpenAIRE |
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