An important step in cancer drug research and development is to generate molecules and agents with better outcomes for inhibition of cancer progression. To date, classic cytotoxic chemotherapy is one of the most frequent methods of treatment. Cytotoxic agents currently used frequently have severe side effects. Thus, clinicians are forced to reduce the recommended dosage, or even avoid the extreme usage of these agents because they are nonselective and are distributed to healthy cells as well as cancer cells. Antibody drug conjugates (ADCs) are a new generation of drugs that consist of three parts: a monoclonal antibody (monoclonal antibodies), a small molecule, and a linker between the two. The use of this structure in research pipelines and recently in clinical practice is likely to achieve more precise and selective distribution and delivery of the cytotoxic agents to cancer cells. This review analyzes the structure of ADCs and the advantages of targeted chemotherapeutics. Possible methods of improvement are also discussed.