Cancer is still the disease that ranks first in human mortality in the twenty-first century. In the last 20 years, the concept of molecular targeted therapy has come to the fore with the use of small molecule agents or signal transduction inhibitors that show anticancer effects for certain types of cancer. Monoclonal antibodies, which have a therapeutic effect, especially by providing signal transduction inhibition, are used clinically as first-line treatment in various types of cancer. Molecular targeted therapies are critical for eliminating the adverse effects and drug resistance problems that occur in traditional cancer treatments. This review summarizes current information on various targeted therapeutic agents, including the structure and classification of monoclonal antibodies, their production methods and mechanisms of action, the monoclonal antibodies used in clinical trials, the complement system mechanism and cancer relationship, and the relationship between complement-dependent cytotoxicity and monoclonal antibodies.