A comprehensive review of small molecule drugs approved by the FDA in 2025: advance and prospect

In 2025, the FDA approved 46 drug marketing applications, 31 of which were small molecule drugs. Despite the advancements in biotechnologies such as antibody drugs, RNA-based treatments, and antibody-drug conjugates, small molecule drugs remain dominant in new drug discovery. With progress in computer-aided drug design and scaffold-based drug design etc, modern drug discovery has stepped into a phase of rapid development. The marketed drugs in the same field often share similar structures and biological activities, while development of me-too drugs can notably enhance potency and streamline the development process. Comprehending the development process of newly launched drugs helps to identify mainstream technologies and provides structural scaffolds and inspirations for future research. This review comprehensively summarises the development progress of new drugs approved in 2025, including molecular design, structural modification, structure-activity relationship, and enhancement of drug-like properties to offer valuable insights to pharmaceutical chemists and bring inspiration for future research.