关键词: 单克隆抗体类药物, 药代动力学特征, 分析方法, 方法学要求

Abstract: In recent years, monoclonal antibodies (mAbs) have been developing rapidly and widely used in fields of tumor, immunity, blood and other systemic diseases. Global share of mAbs in prescription drug market had reached up to $ 140 billion, 15.3% by 2019. As macromolecule proteins, with special structures and physiological properties, mAbs have great differences in absorption, distribution, metabolism and excretion in vivo compared with small molecule drugs, including characteristics of relatively large molecular mass, high specificity and selectivity in target combination, non-linear pharmacokinetics, time dependence, long half-life and so on. Fully understanding of these special pharmacokinetic characteristics shall effectively guide analysis of mAbs. Meanwhile, the particularity and complexity of disposal mechanism in organisms greatly increase the difficulty of biological detection. As a result, it is necessary to establish exclusive, sensitive, accurate and repeatable quantification methods in biological samples. This article focuses on pharmacokinetic characteristics, main analytical methods, and methodology validation of quantification for mAbs in biological samples, expounding with comparisons of small molecular drugs, so as to prompt development of pharmacokinetic study of this kind of drugs.

Key words: monoclonal antibodies, pharmacokinetics characteristics, analysis method, method validation