Regeneron Pharmaceuticals, Inc., Tarrytown, New York, USA.
Sanofi, Bridgewater, New Jersey, USA.
Clin Pharmacol Ther. 2021 Nov;110(5):1318-1328. doi: 10.1002/cpt.2366. Epub 2021 Aug 24.
Dupilumab demonstrated efficacy with an acceptable safety profile in two randomized, double-blind, placebo-controlled, parallel-group, phase III trials in adolescents (12-17 years; LIBERTY AD ADOL) and children (6-11 years; LIBERTY AD PEDS) with atopic dermatitis (AD) treated for 16 weeks. Here, we present the pharmacokinetic profiles and exposure-response (E-R) relationships of dupilumab that guided the posology in these populations. A total of 251 adolescent patients with moderate-to-severe AD were randomized to subcutaneous dupilumab monotherapy every 2 weeks (q2w; 200 mg q2w, baseline weight < 60 kg; 300 mg q2w, ≥ 60 kg), dupilumab 300 mg every 4 weeks (q4w; non-weight tiered), or placebo; 367 children with severe AD were randomized to dupilumab q2w (100 mg q2w, baseline weight < 30 kg; 200 mg q2w, ≥ 30 kg), dupilumab 300 mg q4w, or placebo. Children received concomitant topical corticosteroids in addition to dupilumab, and loading doses were administered at the start of therapy. Mean dupilumab trough concentrations at week 16 for weight subcategories in each dosing regimen were compared with adult exposures for the approved dupilumab 300 mg q2w regimen. Positive E-R relationships were demonstrated between dupilumab trough concentrations and AD outcome measures across patient populations and regimens; no relationship was observed with treatment-emergent conjunctivitis. Based on these analyses, a weight-tiered posology was proposed for adolescents (200/300 mg q2w in patients 30-< 60 kg/≥ 60 kg) and children (300 mg q4w in patients 15-< 30 kg, 200 mg q2w in patients 30-< 60 kg) with moderate-to-severe AD.
在两项为期 16 周的随机、双盲、安慰剂对照、平行分组的 III 期临床试验中,dupilumab 在青少年(12-17 岁;LIBERTY AD ADOL)和儿童(6-11 岁;LIBERTY AD PEDS)中患有特应性皮炎(AD)的患者中显示出疗效,且安全性良好。在此,我们介绍了引导这些人群剂量选择的 dupilumab 的药代动力学特征和暴露-反应(E-R)关系。共有 251 名中重度 AD 青少年患者被随机分为皮下 dupilumab 单药治疗,每 2 周(q2w;基线体重<60kg 时为 200mg q2w,≥60kg 时为 300mg q2w)、每 4 周(q4w;非体重分层)dupilumab 300mg 或安慰剂;367 名严重 AD 儿童被随机分为 dupilumab q2w(基线体重<30kg 时为 100mg q2w,≥30kg 时为 200mg q2w)、dupilumab 300mg q4w 或安慰剂。儿童在接受 dupilumab 治疗的同时还接受了局部皮质类固醇治疗,并在开始治疗时给予了负荷剂量。在每个治疗方案中,根据体重亚组,在第 16 周时比较 dupilumab 谷浓度与成人批准的 dupilumab 300mg q2w 方案的暴露情况。在患者人群和治疗方案中,均显示出 dupilumab 谷浓度与 AD 疗效指标之间存在正 E-R 关系;未观察到与治疗诱发的结膜炎有关。基于这些分析,提出了一种用于青少年(体重 30-<60kg/≥60kg 的患者为 200/300mg q2w)和儿童(体重 15-<30kg 的患者为 300mg q4w,体重 30-<60kg 的患者为 200mg q2w)中重度 AD 的体重分层方案。