title: [Progress on pharmacokinetic study of antibody-drug conjugates].
abstract: Antibody-drug conjugate (ADC) is a new class of therapeutics composed of a monoclonal antibody and small cytotoxin moieties conjugated through a chemical linker. ADC molecules bind to the target antigens expressed on the tumor cell surfaces guided by the monoclonal antibody component. The binding ADC molecules can be internalized and subsequently the toxin moieties can be released within the tumor cells via chemical and/or enzymatic reactions to kill the target cells. The conjugation combines the merits of both components, i.e., the high target specificity of the monoclonal antibody and the highly potent cell killing activity of the cytotoxin moieties. However, such complexities make the pharmacokinetic and metabolic studies of ADCs highly challenging. The major challenges should include characterization of absorption, distribution, metabolism and excretion, investigation of underlying mechanisms, assessment of pharmacokinetic- pharmacodynamic relationship, and analytical method development of ADC drugs. This review will discuss common pharmacokinetic issues and considerations, as well as tools and strategies that can be utilized to characterize the pharmacokinetic and metabolic properties of ADCs.
authors.forename: Jian-jun
authors.initials: JJ
authors.lastname: Guo
authors.forename: Ran
authors.initials: R
authors.lastname: Gao
authors.forename: Teng-fei
authors.initials: TF
authors.lastname: Quan
authors.forename: Ling-yu
authors.initials: LY
authors.lastname: Zhu
authors.forename: Ben
authors.initials: B
authors.lastname: Shi
authors.forename: Yong-yue
authors.initials: YY
authors.lastname: Zhao
authors.forename: Jing
authors.initials: J
authors.lastname: Zhu
authors.forename: Meng-sha
authors.initials: MS
authors.lastname: Li
authors.forename: Hai-zhi
authors.initials: HZ
authors.lastname: Bu
mesh_terms: D000911:Antibodies, Monoclonal / Q000493:pharmacokinetics*; D003603:Cytotoxins / Q000493:pharmacokinetics; D006801:Humans; D018796:Immunoconjugates / Q000493:pharmacokinetics*; D009369:Neoplasms / Q000188:drug therapy
chemical_list: D000911:Antibodies, Monoclonal; D003603:Cytotoxins; D018796:Immunoconjugates