Clinical Pharmacology and Bioanalytics, Pfizer Research and Development, 445 Eastern Point Road, Groton, Connecticut, 06340, USA.
Clinical Pharmacology and Bioanalytics, Pfizer Research and Development, New York, New York, USA.
AAPS J. 2023 Sep 2;25(5):85. doi: 10.1208/s12248-023-00846-x.
Historically, the biopharmaceutical industry has used titer to characterize the magnitude of an anti-drug antibody (ADA) response. While reporting levels of antibodies in terms of titer is generally understood and accepted by regulatory and medical communities, titer values are inherently variable given the multiple serial dilutions and reporting a value either directly before or interpolated at the assay cut point on the lower plateau of the assay curve range. Using S/N is an appealing alternative approach to titer as it simplifies analysis with less dilutions, significantly reducing testing, time, and resources and provides a more precise value potentially differentiating low-level ADA responses. Current bridging electrochemiluminescence (ECL) ADA assays using Meso Scale Discovery (MSD) platform are also significantly more sensitive and drug tolerant with wider assay ranges compared to historic ELISA platforms; therefore, ADA response based on S/N may help differentiate and identify those ADA samples that are more likely to be clinically relevant. Bococizumab is a humanized monoclonal antibody targeting proprotein convertase subtilisin-kexin type 9 (PCSK9), which reduces plasma levels of low-density lipoprotein (LDL) cholesterol. Bococizumab was discontinued during Phase 3 clinical development based in part on the high rate of ADA and wide variation in LDL cholesterol responses among patients. The impact of anti-bococizumab antibodies on pharmacokinetic (PK) and pharmacodynamic (PD) endpoints was originally assessed using titer. Retrospective analysis of anti-bococizumab ADA responses using S/N ratios illustrates that S/N is an acceptable alternative to titer for characterizing the magnitude of ADA response and interpretation of clinically relevant ADA.
从历史上看,生物制药行业一直使用滴度来描述抗药物抗体 (ADA) 反应的强度。虽然以滴度报告抗体水平在监管和医疗界通常被理解和接受,但由于多次连续稀释以及在低于分析曲线平台下限的检测点之前直接报告值或内插值,滴度值本质上是可变的。与滴度相比,使用 S/N 是一种有吸引力的替代方法,因为它通过减少稀释来简化分析,显著减少测试、时间和资源,并提供更精确的值,可能区分低水平 ADA 反应。与历史 ELISA 平台相比,目前使用 Meso Scale Discovery (MSD) 平台的桥接电化学发光 (ECL) ADA 检测也显著更灵敏且对药物更耐受,具有更宽的检测范围;因此,基于 S/N 的 ADA 反应可能有助于区分和识别那些更可能具有临床相关性的 ADA 样本。Bococizumab 是一种针对前蛋白转化酶枯草溶菌素 9 (PCSK9) 的人源化单克隆抗体,可降低血浆中低密度脂蛋白 (LDL) 胆固醇水平。在 3 期临床开发期间,Bococizumab 因部分患者 ADA 发生率高且 LDL 胆固醇反应差异大而被停用。最初使用滴度评估抗 Bococizumab 抗体对药代动力学 (PK) 和药效学 (PD) 终点的影响。使用 S/N 比值对 Bococizumab ADA 反应的回顾性分析表明,S/N 是替代滴度来描述 ADA 反应强度和解释临床相关 ADA 的可接受方法。