The clinical success of antibody-drug conjugates (ADCs) has driven the rapid development of novel conjugate drugs, including radionuclide drug conjugates (RDCs), peptide drug conjugates (PDCs), and small molecule drug conjugates (SMDCs). These drugs offer significant advantages in cancer treatment by integrating targeted delivery with efficient payload release and are progressively expanding into disease diagnosis and therapeutic areas beyond oncology. This article systematically reviewed the current landscape of conjugate drugs, coupling technologies, recent progress, and clinical translation, while exploring future directions in expanding indications, technological advancements, and integrated theranostic applications.