In the age of precision medicine, new developments and proof-of-concept formats are rapidly enhancing antibody-based treatments. Antibody-drug conjugates (ADCs) have completely changed the way cancer chemotherapy is practiced over the past couple of decades. ADCs use monoclonal antibodies (mAbs) to precisely bind tumor-associated target antigens and release a highly effective cytotoxic agent, in contrast to traditional therapies that cause damage to healthy tissues during dose escalation. An incredibly effective class of anticancer medications with an already sizable and expanding clinical pipeline has been created by the synergistic combination of mAbs conjugated to small-molecule chemotherapeutics via a stable linker.