Abstract: Antibody-drug conjugates (ADCs) are a new class of therapeutic drugs for the treatment of many different malignant tumors. An ADC consists of a monoclonal antibody, a potent cytotoxic small molecule chemotherapeutic (payload) and a chemical linker. Although ADC has both high target specificity of the antibody and highly potential cytotoxicity of the payload, many failed amid the clinical trials because of the high toxicity or low efficacy. In this case, the analysis of pharmacokinetic properties and predication of ADCs in vivo can provide significant reference for the structural design of ADCs and the determination of dosing regimens. This review summarizes multifaceted factors for the pharmacokinetics of ADCs and the commonly used bioanalytical tools of ADCs pharmacokinetics, and provides theoretical reference for the reasonable predication of pharmacokinetics and pharmacodynamics of ADCs in vivo.