Fluorine-containing FDA-approved small-molecule drugs in 2025: significance, synthetic insights, and therapeutic applications
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. Overall, this review provides an updated perspective on the continued importance of fluorine chemistry in modern drug discovery and development.
Read the paper
Related studies
- Noninvasive and Point-of-Care Surface-Enhanced Raman Scattering (SERS)-Based Breathalyzer for Mass Screening of Coronavirus Disease 2019 (COVID-19) under 5 min
- De Novo Transcriptome Analysis and Detection of Antimicrobial Peptides of the American Cockroach Periplaneta americana (Linnaeus)
- Molecular Characterization and Expression Profiling of Tomato GRF Transcription Factor Family Genes in Response to Abiotic Stresses and Phytohormones
- Assembly of Tight Junction Strands: Claudin-10b and Claudin-3 Form Homo Tetrameric Building Blocks that Polymerise in a Channel-Independent Manner
- Update of the Pompe variant database for the prediction of clinical phenotypes: Novel disease‐associated variants, common sequence variants, and results from newborn screening
- Machine Learning-Based SERS Chemical Space for Two-Way Prediction of Structures and Spectra of Untrained Molecules
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.