Vilaprisan is a novel selective progesterone receptor modulator for the long-term treatment of uterine fibroids and endometriosis. 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 vilaprisan 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 μg · 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) after multiple dosing. Mild to moderate adverse events were observed similar to previous studies. Overall, daily oral administration of the therapeutic dose of 2 mg of vilaprisan over 14 days was safe and well tolerated by all participants.

译文

vilaprison是一种新型的选择性孕激素受体调节剂,可长期治疗子宫肌瘤和子宫内膜异位症。这项研究调查了vilaprison在健康的中国绝经后妇女中的药代动力学,安全性和耐受性。12名参与者在14天内每天接受一次多次剂量的vilaprisan,为2 mg片剂。使用液相色谱-串联质谱法测定血浆vilaprison浓度。通过非房室分析评估vilaprison的主要药代动力学参数,包括最大观察浓度 (Cmax),全身暴露 (血浆浓度-时间曲线下的面积),达到Cmax的时间和终末半衰期。安全性评估包括不良事件的记录,临床/人体测量参数和生命体征的测量,心电图以及体格和妇科检查。参与者的平均年龄为53.3 (± 4.2) 岁,体重指数为23.8 ± 2.8千克/m2。达到Cmax的中位时间为单次和多次维拉普瑞沙给药后1.5小时。与单次给药 (23.3 μ g/L [SD = 6.73]) 相比,多次给药 (12.5 μ g/L [SD = 3.04]) 后获得的平均Cmax值高1.92倍 (SD = 0.554)。在单次给药 (91.3 μ g · h/L [SD = 20.4]) 和多次给药 (276 μ g · h/L [SD = 109]) 之间,给药间隔内血浆浓度-时间曲线下的平均面积随累积因子2.98 (SD = 0.767) 而增加。在多次给药后,vilaprison的平均终末半衰期为44.5小时 (SD = 10.3)。观察到轻度至中度不良事件与先前的研究相似。总体而言,所有参与者在14天内每天口服2 mg vilaprissan的治疗剂量是安全的,并且耐受性良好。

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