新型延长半衰期抗白细胞介素-13单克隆抗体APG777在食蟹猴中的临床前安全性

IF 1 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Daniel Rubio, Eric Zhu, Archie Thurston, Kathleen A Funk, Kristina A York, Carl L Dambkowski, Drew Badger
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引用次数: 0

摘要

白细胞介素-13 (IL-13)是一种参与2型炎症性疾病病理生理的细胞因子,是临床上证实的特应性皮炎靶点。APG777是一种人源化IgG1单克隆抗体,具有优化的药代动力学特征。APG777对IL-13具有高亲和力,在其Fc区包含一个三重氨基酸修饰(“YTE”修饰),旨在延长其半衰期。目前的研究检测了食蟹猴每周一次皮下注射APG777 27周的安全性和潜在毒性,以及2个月恢复期后任何发现的潜在可逆性。测定了APG777的毒动学特征。APG777表现出剂量比例的全身暴露,半衰期约为28天。临床观察、体重、眼科、心电图读数、神经参数、血液学、凝血、临床化学、尿液分析、器官重量或组织病理学均未发现与apg777相关的不良反应。apg777暴露动物未检出抗药物抗体。在研究期间药物积累明显;然而,在分析的所有参数中均未发现与apg777相关的不良反应。未观察到的不良反应水平(NOAEL)为150 mg/kg/周。这些发现为APG777治疗il -13介导疾病的持续临床开发提供了临床前证据。APG777延长的半衰期表明,与现有的il -13靶向治疗相比,它在减少给药频率方面有潜在的好处,可以改善治疗依从性和患者预后。APG777的安全性和有效性目前正在一项针对中重度特应性皮炎患者的2期临床试验(NCT06395948)中进行研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preclinical Safety of APG777, A Novel Extended Half-Life Anti-Interleukin-13 Monoclonal Antibody, in Cynomolgus Monkeys.

Interleukin-13 (IL-13) is a cytokine implicated in the pathophysiology of type 2 inflammatory diseases and is a clinically validated target in atopic dermatitis. APG777 is a humanized IgG1 monoclonal antibody with an optimized pharmacokinetic profile. APG777 has high affinity to IL-13 and includes a triple amino acid modification (the "YTE" modification) in its Fc region that is designed to extend its half-life. The current study examined the safety and potential toxicity of APG777 when given by once-weekly subcutaneous injection for 27 weeks to cynomolgus monkeys, and the potential reversibility of any findings following a 2-month recovery period. Toxicokinetic characteristics of APG777 were also determined. APG777 exhibited dose-proportional systemic exposure, with a half-life of approximately 28 days. No APG777-related adverse effects were noted in clinical observations, body weight, ophthalmology, electrocardiogram readings, neurologic parameters, hematology, coagulation, clinical chemistry, urinalysis, organ weights, or histopathology. Anti-drug antibodies were not detected in any APG777-exposed animals. Drug accumulation was evident over the study duration; however, there were no APG777-related adverse findings in any of the parameters analyzed. The no-observed-adverse-effect level (NOAEL) was 150 mg/kg/week. These findings provide preclinical evidence supporting continued clinical development of APG777 for IL-13-mediated diseases. The extended half-life of APG777 suggests potential benefits in reducing dosing frequency compared with existing IL-13-targeting therapies, which could improve treatment adherence and patient outcomes. The safety and efficacy of APG777 are currently being investigated in a Phase 2 clinical trial (NCT06395948) in patients with moderate-to-severe atopic dermatitis.

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来源期刊
CiteScore
3.40
自引率
4.50%
发文量
53
审稿时长
4.5 months
期刊介绍: The International Journal of Toxicology publishes timely, peer-reviewed papers on current topics important to toxicologists. Six bi-monthly issues cover a wide range of topics, including contemporary issues in toxicology, safety assessments, novel approaches to toxicological testing, mechanisms of toxicity, biomarkers, and risk assessment. The Journal also publishes invited reviews on contemporary topics, and features articles based on symposia. In addition, supplemental issues are routinely published on various special topics, including three supplements devoted to contributions from the Cosmetic Review Expert Panel.
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