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首页> 外文期刊>International journal of clinical pharmacology and therapeutics >Bioequivalence of different dose-strength tablets of selexipag, a selective prostacyclin receptor agonist, in a multiple-dose up-titration study
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Bioequivalence of different dose-strength tablets of selexipag, a selective prostacyclin receptor agonist, in a multiple-dose up-titration study

机译：选择性剂量前列环素受体激动剂selexipag的不同剂量强度片剂的生物等效性在多剂量滴定研究中

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Objective: Selexipag is a novel, oral, selective prostacyclin (PGI(2)) receptor agonist in clinical development for the treatment of pulmonary arterial hypertension. Film-coated tablets with strength between 200 and 1,600 mu g were used. Bioequivalence between 8 x 200 mu g and a new 1,600 mu g tablet was evaluated at steady state in healthy male subjects. Materials and methods: This was an open-label, 2-treatment, 2-period, crossover, up-titration, phase 1 study. The treatments were selexipag at 1,600 mu g b.i.d. for 4.5 days either as 8 x 200 mu g tablets (reference: A) or 1 x 1,600 mu g tablet (test: B), both preceded by an up-titration phase starting from 400 mu g b.i.d. doses, in 200-mu g steps every 4th day. Subjects were randomized 1 : 1 to the A-B or B-A sequence. The pharmacokinetics and tolerability of selexipag and its active metabolite, ACT-333679, were investigated. Results: 80 subjects were enrolled in the study: 65 subjects completed the study according to protocol, and 15 subjects withdrew from the study. The most frequent adverse events (AEs) were headache (86%), myalgia (73%), and jaw pain (73%). There was no difference in nature and overall frequency of AEs between the two treatments. Steady state was attained within 3 days of the selexipag 1,600 gig bid. treatments. The 90% confidence intervals (CIs) of the geometric mean ratio (B/A) at steady state for AUC(tau) and C-max,C-ss were within (0.80, 1.25) bioequivalence interval: (0.92, 1.06) and (0.95, 1.14), respectively, for selexipag and (0.95, 1.06) and (0.94, 1.07), respectively, for the active metabolite, ACT-333679. Conclusions: Bioequivalence was demonstrated between 8 x 200 jig and 1 x 1,600 jag selexipag at steady state.
机译：目的：Selexipag是一种新型的口服选择性前列环素（PGI（2））受体激动剂，正在临床开发中用于治疗肺动脉高压。使用强度在200至1600微克之间的薄膜包衣片剂。在健康男性受试者中，在稳态下评估了8 x 200μg和新的1600μg片剂之间的生物等效性。材料和方法：这是一项开放标签，2处理，2周期，交叉，高滴定度的1期研究。处理方法是selexipag，每天1600微克。以8 x 200μg片剂（参考：A）或1 x 1600μg片剂（测试：B）持续4.5天，两者都在从400μg b.i.d开始的滴定阶段之前。剂量，每4天200克/步。将受试者1：1按照A-B或B-A序列随机分配。研究了selexipag及其活性代谢物ACT-333679的药代动力学和耐受性。结果：80名受试者参加了该研究：65名受试者根据方案完成了研究，而15名受试者退出了研究。最常见的不良事件（AEs）为头痛（86％），肌痛（73％）和下颚疼痛（73％）。两种疗法之间，AEs的性质和总频率没有差异。在selexipag 1600演出后的3天内达到了稳态。治疗。稳态时AUC（tau）的几何平均比（B / A）的90％置信区间（CIs）在（0.80，1.25）生物等效区间内：（0.92，1.06）和活性代谢产物ACT-333679分别为selexipag（0.95，1.14）和（0.95，1.06）和（0.94，1.07）。结论：在稳态下，在8 x 200夹具和1 x 1600尖头塞克西帕格之间表现出生物等效性。

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