药物动力学、药效学和安全性的Etrolizumab儿童中度至严重活动性溃疡性结肠炎和克罗恩病:从第一阶段随机试验的结果。

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张W, Scalori Fuh F,麦克布莱德J,她G, Kierkus J, Korczowksi B,李R, Abouhossein M,让我们,公园KT,唐太

药物动力学、药效学和安全性的Etrolizumab儿童中度至严重活动性溃疡性结肠炎和克罗恩病:从第一阶段随机试验的结果。

Inflamm肠道说。2021年11月29日。pii: 6446094。doi: 10.1093 / ibd / izab275。

PubMed ID

34849918 (在PubMed

]

文摘

背景:Etrolizumab,人性化anti-beta7抗体,尚未在孩子学习。在这里,我们评估药物动力学、药效学和安全性etrolizumab与炎症性肠病的孩子。方法:患者年龄4 - 17年中度至严重活动性溃疡性结肠炎和克罗恩病随机1:1接收1.5毫克/公斤每4周etrolizumab皮下注射(q4w)或3.0毫克/公斤每8周(q8w) 16周在这个开放的第一阶段试验。药物动力学、药效学、安全,疗效评估。结果:24例的治疗,21日完成这项研究。在1.5毫克/公斤q4w组和3.0毫克/公斤q8w,分别是(SD)最大浓度(Cmax)为9.8 (4.86)microg /毫升和18.1 (6.25)microg /毫升;和平均(SD)曲线下的面积内剂量间隔(AUCtau) 167(86.9)和521(306)杯子。天/毫升后最后剂量。Cmax增加剂量比例。AUC超过8周时间在3.0毫克/公斤q8w略高剂量组。给药方案的平均半衰期很相似。 Median numbers of free beta7high gut-homing T and B cell subsets declined below 10% of baseline, confirming beta7 target engagement and complete/near-complete receptor occupancy. Adverse events were consistent with the safety profile in adults. Approximately 60% of patients achieved a clinical response. CONCLUSIONS: Etrolizumab showed a dose-proportional increase in Cmax and a slightly greater than dose-proportional increase in AUCtau. Both regimens achieved complete/near-complete beta7 receptor occupancy, with a similar relationship to concentration as adults. Etrolizumab was well tolerated and demonstrated clinical activity in children.

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药物

Etrolizumab