Chen Naihan, Sano Yamato, Wang Xiaohong, Hu Shuiyi, Tabira Junichi, Luo Xin, Yoshimatsu Hiroki, Prybylski John, Chu Myron, Li Haiyan, Takazawa Kenji
Development China - Oncology & Rare Disease Development, Clinical Pharmacology, Pfizer Inc, Beijing, China.
Clinical Pharmacology and Bioanalytics, Pfizer R&D Japan, Tokyo, Japan.
Clin Pharmacol Drug Dev. 2025 Aug;14(8):572-582. doi: 10.1002/cpdd.1522. Epub 2025 May 22.
Dazukibart is a humanized monoclonal antibody selectively targeting interferon-β. The pharmacokinetics (PK), safety, tolerability, and immunogenicity of dazukibart were evaluated in 2 double-blind, randomized, placebo-controlled, single-dose, Phase 1 studies in healthy adults in China (Study 1: N = 18; dazukibart 900 mg = 15; placebo = 3) and Japan (Study 2: N = 12; Cohort 1: dazukibart 300 mg = 5, placebo = 1; and Cohort 2: dazukibart 900 mg = 5, placebo = 1). PK parameters were assessed after dosing in Study 1 and Study 2, and no significant differences were observed between PK findings among participants in both studies. A biphasic decline in dazukibart serum concentrations was observed in both studies. Exposures increased dose proportionally in Study 2. Body weight, but not race, was identified as an independent covariate of exposure using population PK modeling (including data from a Phase 1 US study [NCT02766621]). No deaths/discontinuations or serious/severe adverse events were observed, mostly mild adverse events were reported. No participants in Study 1 were antidrug antibody positive; 20.0% in Study 2 were positive for treatment-induced antidrug antibodies and neutralizing antibodies. PK parameters and immunogenicity rates were consistent with the US study, and no new safety signals were identified.
达祖基巴特是一种选择性靶向干扰素-β的人源化单克隆抗体。在中国健康成年人中开展了2项双盲、随机、安慰剂对照、单剂量1期研究(研究1:N = 18;达祖基巴特900 mg = 15例;安慰剂 = 3例)以及在日本开展了研究(研究2:N = 12;队列1:达祖基巴特300 mg = 5例,安慰剂 = 1例;队列2:达祖基巴特900 mg = 5例,安慰剂 = 1例),对达祖基巴特的药代动力学(PK)、安全性、耐受性和免疫原性进行了评估。在研究1和研究2给药后评估了PK参数,两项研究参与者的PK结果之间未观察到显著差异。两项研究均观察到达祖基巴特血清浓度呈双相下降。在研究2中,暴露量随剂量成比例增加。使用群体PK模型(包括来自一项美国1期研究[NCT02766621]的数据)确定体重而非种族是暴露的独立协变量。未观察到死亡/停药或严重/重度不良事件,报告的大多为轻度不良事件。研究1中没有参与者抗药抗体呈阳性;研究2中有20.0%的参与者治疗诱导的抗药抗体和中和抗体呈阳性。PK参数和免疫原性率与美国研究一致,未发现新的安全信号。