Fluorine-containing drugs approved by the FDA in 2025

Wang, Qian and Bian, Yeping and Abouchabaka, Elias and Baecker, Daniel and Dhawan, Gagan and Semghouli, Anas and Kiss, Loránd and Zhang, Wei and Soloshonok, Vadim A. and Jianlin, Han (2026) Fluorine-containing drugs approved by the FDA in 2025. CHINESE CHEMICAL LETTERS, 37 (9). ISSN 1001-8417

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Abstract

Fluorine substitution has emerged as a cornerstone of modern drug design, profoundly influencing the pharmacological properties of therapeutic agents. Owing to its high electronegativity and small atomic radius, fluorine imparts unique electronic and steric effects that enhance lipophilicity, metabolic stability, binding affinity, and pKa, thereby improving efficacy, bioavailability, and pharmacokinetics. Often referred to as an “enchanted atom”, fluorine can decisively alter the trajectory of drug candidates, reducing attrition and increasing clinical success. Within synthetic organic chemistry, the pursuit of novel biologically active compounds is closely tied to monitoring advances in approved pharmaceuticals, with fluorinecontaining drugs representing one of the most dynamic areas of innovation. In this review, we profile fourteen new pharmaceuticals approved by the U.S. Food and Drug Administration (FDA) in 2025, including datopotamab deruxtecan, suzetrigine, mirdametinib, avutometinib/defactinib, taletrectinib, sunvozertinib, sebetralstat, rilzabrutinib, imlunestrant, paltusotine, remibrutinib, elinzanetant, ziftomenib, and zoliflodacin. For each compound, we examine the medicinal chemistry discovery, therapeutic application, and FDA approval timeline, with particular emphasis on synthetic strategies and the role of fluorine incorporation. This review aims to provide a timely resource and inspiration for researchers in academia and the pharmaceutical industry, as well as for students engaged in drug design, fluorine chemistry, and medicinal chemistry.

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