A comprehensive review of new small molecule drugs approved by the FDA in 2022: Advance and prospect.

In 2022, the U.S. Food and Drug Administration approved a total of 16 marketing applications for small molecule drugs, which not only provided dominant scaffolds but also introduced novel mechanisms of action and clinical indications. The successful cases provide valuable information for optimizing efficacy and enhancing pharmacokinetic properties through strategies like macrocyclization, bioequivalent group utilization, prodrug synthesis, and conformation restriction. Therefore, gaining an in-depth understanding of the design principles and strategies underlying these drugs will greatly facilitate the development of new therapeutic agents. This review focuses on the research and development process of these newly approved small molecule drugs including drug design, structural modification, and improvement of pharmacokinetic properties to inspire future research in this field. [Display omitted] • The clinical applications and mechanisms of action of newly approved drugs were summarized. • The development processes and design concepts of new drugs were reviewed. • The X-ray crystal structures and molecular binding models of new drugs were exhibited. • The practical structure-activity relationship of each new drugs was summarized. [ABSTRACT FROM AUTHOR]