Li Haiyan, Liu Juanfang, Wang Xiaohong, Zhao Weilong, Zhang Lili, Niu Xiaoye, Liu Jingyao, Dong Zhongqi
Peking University Third Hospital, Beijing, China.
Johnson & Johnson, Shanghai, China.
Neurol Ther. 2025 May 19. doi: 10.1007/s40120-025-00763-5.
Nipocalimab is a high-affinity, fully human, immunoglobulin G (IgG) 1 monoclonal antibody that inhibits the neonatal Fc receptor. Nipocalimab is under development for the treatment of various IgG autoantibody- and alloantibody-mediated diseases. This study assessed the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of a single dose of nipocalimab in healthy Chinese volunteers.
In this phase I, open-label study, healthy volunteers received single doses of intravenous (IV) nipocalimab at 15, 30, or 45 mg/kg. The primary objective was to assess the PK following a single administration of nipocalimab. Secondary objectives included the PD effects of nipocalimab on change from baseline in total serum IgG levels, safety, and tolerability.
A total of 30 healthy Chinese volunteers (mean age 31.0 years, 93.3% men) received single doses of IV nipocalimab. Following a single infusion of nipocalimab, mean exposure increased as the dose of nipocalimab increased. Maximum serum nipocalimab concentrations increased proportionally with doses, whereas the area under the concentration-time curve increased by greater than a dose-proportional manner. Nipocalimab led to dose-dependent reductions in serum IgG levels from baseline; this decrease was sustained over a longer period of time with higher dose levels. Nipocalimab was generally well tolerated, with an acceptable safety profile, across all three doses; most of the treatment-emergent adverse events (TEAEs) were mild. Higher doses of nipocalimab were not associated with increased frequency of TEAEs.
Our findings add to the evidence on the safety, tolerability, and PD of nipocalimab in the Chinese population, and support for the treatment of pathogenic IgG-mediated diseases in this population.
ClinicalTrials.gov NCT05151692.
尼泊卡利单抗是一种高亲和力、全人源免疫球蛋白G（IgG）1单克隆抗体，可抑制新生儿Fc受体。尼泊卡利单抗正在开发用于治疗各种IgG自身抗体和同种抗体介导的疾病。本研究评估了单剂量尼泊卡利单抗在健康中国志愿者中的安全性、药代动力学（PK）和药效学（PD）。
在这项I期开放标签研究中，健康志愿者接受了15、30或45mg/kg的单剂量静脉注射（IV）尼泊卡利单抗。主要目的是评估单次给药尼泊卡利单抗后的药代动力学。次要目的包括尼泊卡利单抗对总血清IgG水平相对于基线变化的药效学作用、安全性和耐受性。
共有30名健康中国志愿者（平均年龄31.0岁，93.3%为男性）接受了单剂量静脉注射尼泊卡利单抗。单次输注尼泊卡利单抗后，平均暴露量随尼泊卡利单抗剂量的增加而增加。血清尼泊卡利单抗最大浓度与剂量成比例增加，而浓度-时间曲线下面积的增加幅度大于剂量成比例的方式。尼泊卡利单抗导致血清IgG水平相对于基线呈剂量依赖性降低；在较高剂量水平下，这种降低在更长时间内持续存在。在所有三个剂量组中，尼泊卡利单抗总体耐受性良好，安全性可接受；大多数治疗中出现的不良事件（TEAE）为轻度。较高剂量的尼泊卡利单抗与TEAE频率增加无关。
我们的研究结果补充了尼泊卡利单抗在中国人群中的安全性、耐受性和药效学证据，并支持在该人群中治疗致病性IgG介导的疾病。
ClinicalTrials.gov NCT05151692。
