Abstract: Antibody drug conjugates(ADCs), which couple monoclonal antibodies(mAb) and cytotoxic drug together by chemical bond, are targeted anticancer drugs. ADCs fully take advantage of the specificity of mAb and the high anticancer activity of cytotoxic drug to achieve the efficiency and low-toxic anticancer effects. Cytotoxic drug, mAb and linker are three significant parts of ADC. In this review, target selection, mAb miniaturization and humanization, potent cytotoxic drug application, characteristics of cleavable and non-cleavable linkers and popular site-specific conjugation were described, which were aim to provide evidence for preclinical studies of ADCs.