FDA‐approved drugs featuring macrocycles or medium‐sized rings

Youlong, Du and Semghouli, Anas and Wang, Qian and Mei, Haibo and Kiss, Loránd and Baecker, Daniel and Soloshonok, Vadim A. and Han, Jianlin (2025) FDA‐approved drugs featuring macrocycles or medium‐sized rings. Archiv der Pharmazie / Chemistry in Life Sciences, 358 (1). No.-e2400890. ISSN 1521-4184

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Abstract

Macrocyclesormedium‐sizedringsofferdiversefunctionalityandstereochemical complexity inawell‐organizedringstructure, allowingthemtofulfill variousbiochemicalfunctions,resultinginhighaffinityandselectivityforproteintargets,while preserving sufficient bioavailability to reach intracellular compartments. These featureshavemademacrocyclesattractivecandidatesinorganicsynthesisanddrug discovery. Since the 20th century, more than three‐scoremacrocyclic drugs, including radiopharmaceuticals, havebeenapprovedby theUSFoodandDrug Administration (FDA) for treating bacterial and viral infections, cancer, obesity, immunosuppression, inflammatory, andneurological disorders, managing cardiovascular diseases, diabetes, andmore. This reviewpresents 17FDA‐approved macrocyclicdrugsduringthepast5years,highlightingtheir importanceandcritical role inmodern therapeutics, and the innovative synthetic approaches for the constructionofthesemacrocycles.

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