Fluorine-containing FDA-approved small-molecule drugs in 2025: significance, synthetic insights, and therapeutic applications
Shweta Mishra, Chetna Jadala, Savio Cardoza, Gal Reddy Potuganti, Ganga Reddy Velma
TL;DR
This paper reviews 14 FDA-approved small-molecule drugs in 2025 that contain fluorine, highlighting their importance in drug design and development.
Contribution
The paper provides an updated summary of fluorine-containing drugs approved in 2025 and their synthetic and therapeutic relevance.
Findings
14 of 29 FDA-approved small-molecule drugs in 2025 contain fluorine.
Fluorine enhances drug properties like metabolic stability and pharmacokinetics.
The review outlines therapeutic uses and synthetic methods for these fluorinated drugs.
Abstract
Fluorine has been widely incorporated into small-molecule drugs as an effective strategy to modulate metabolic stability, lipophilicity, target interactions, and overall pharmacokinetic profile. As a result, fluorine-containing compounds remain well represented among newly approved therapeutics across a broad spectrum of disease areas; notably, in 2025, 14 of the 29 small-molecule drugs approved by the U.S. Food and Drug Administration (FDA) contained at least one fluorine atom, underscoring the continued relevance of fluorine in contemporary drug design. This annual review highlights the role of fluorine in modern medicinal chemistry by summarizing FDA-approved fluorine-containing small-molecule drugs in 2025. The review examines their therapeutic indications, molecular targets, and structural features, and outlines representative synthetic strategies used in their preparation.…
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Taxonomy
TopicsFluorine in Organic Chemistry · Click Chemistry and Applications · Protein Degradation and Inhibitors