In recent years, therapeutic conjugates have attracted considerable attention as a new class of drug due to their unique pharmacological properties, especially from the pharmaceutical community. Their molecular structure tunability, improved targeting specificity, and therapeutic efficacy have been demonstrated in a wide range of research and clinical applications. In this topical review, we summarize selected recent advances in bioconjugation strategies for the development of therapeutic conjugates, their emerging application in clinical settings, as well as perspectives on the direction of future research.