Highlights on U.S. FDA-approved halogen-containing drugs in 2024

This comprehensive review offers an update on the FDA-approved halogen-containing drugs in 2024. The agency approved a total of 50 drugs, including small molecules and macromolecules. Excitingly, 16 out of 50 are halogen-containing drugs, indicated to diagnose, mitigate and treat the various human diseases. Among halogens, fluorine and chlorine are highly prevalent in drug discovery and development. Therefore, the properties of fluorine and chlorine and their impact on the drug profile are briefly discussed. In addition, the specific role of halogens in these drugs has been discussed with the help of structure-activity relationships (SARs), co-crystal structures, and closely related literature precedents. This review also provides the additional information for each drug, such as trade name, active ingredients, route of administration, approval date, sponsors, indication, mode of action, major drug metabolizing enzyme(s), and route of elimination. We expect that the present review may garner the attention of drug discovery researchers and inspire them toward the potential applications of halogens to discover novel therapeutics in the future.