Traditional medicinal chemistry has long centered on the design and optimization of small molecules. However, the therapeutic landscape is rapidly evolving to include a broader spectrum of modalities that extend beyond this classical paradigm. This session, titled “Medicinal Chemistry: Beyond Small Molecules,” will explore how advances in fields such as protein degraders, macrocycles, and antibody-drug conjugates are redefining the frontiers of drug discovery. Speakers will highlight both the scientific and technological innovations enabling these novel approaches. By examining cutting-edge case studies and emerging trends, the session aims to provide insights into how the expanding medicinal chemistry toolkit can unlock new therapeutic opportunities and address previously intractable biological targets.