Pharmacokinetics and Safety of the Selective Progesterone Receptor Modulator Vilaprisan in Chinese Healthy Postmenopausal Women

This study investigated the pharmacokinetics, safety, and tolerability of vilaprisan in healthy Chinese postmenopausal women. Twelve participants received multiple doses of vilaprisan once daily over 14 days as a 2‐mg tablet. Plasma vilapr isan concentrations were determined using liquid chromatography–tandem mass spectrometry. The main pharmacokinetic parameters of vilaprisan were assessed with noncompartmental analysis, including maximum observed concentration (Cmax), systemic exposure (area under the plasma concentration –time curve), time to reach Cmax and terminal half ‐life. Safety assessments include the documentation of adverse events, measurement of clinical/anthropometric parameters and vital signs, electrocardiogram, and physical and gynecologic examination. The participants had a mean age of 53.3 (± 4.2) years and a body mass index of 23.8 ± 2.8 kg /m2. Median time to reach Cmax was 1.5  hours after both single and multiple vilaprisan administration. Mean Cmax values obtained after multiple dosing (23.3  μg/L [standard deviation (SD) = 6.73]) were 1.92‐fold (SD = 0.554) higher compared to single dosing (12.5 μg/L [SD = 3.04]). Mean area under the plasma concentration–time curve in the dosing interval increased with an accumulation factor of 2.98 (SD = 0.767) between single (91.3 μ g · h/L [SD = 20.4]) and multiple dosing (276 μg · h/L [SD = 109]). The mean terminal half‐life of vilaprisan was 44.5 hours (SD = 10.3...
Source: Clinical Pharmacology in Drug Development - Category: Drugs & Pharmacology Authors: Tags: Original Manuscript Source Type: research