Fluorine in the Pharmaceutical Industry: FDA-Approved Fluorine-Containing Drugs in 2024

Youlong Du¹, Yeping Bian², Daniel Baecker³, Gagan Dhawan^{4

5}, Anas Semghouli⁶, Loránd Kiss⁶, Wei Zhang⁷, Alexander E Sorochinsky⁸, Vadim A Soloshonok^{9

10}, Jianlin Han¹

Affiliations

¹ Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, International Innovation Center for Forest Chemicals and Materials, College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, China.
² Department of Intensive Care Unit, Geriatric Hospital of Nanjing Medical University, No.30 Luojia Road, Nanjing, 210024, China.
³ Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Straße 2+4, 14195, Berlin, Germany.
⁴ School of Allied Medical Sciences, Delhi Skill and Entrepreneurship University, Dwarka, New Delhi, 110077, India.
⁵ Department of Biomedical Science, Acharya Narendra Dev College, University of Delhi, Kalkaji, New Delhi, 110019, India.
⁶ Institute of Organic Chemistry, Stereochemistry Research Group, HUN-REN Research Centre for Natural Sciences, Magyar tudósok krt. 2, Budapest, H-1117, Hungary.
⁷ Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Boulevard, Boston, MA, USA, 02125.
⁸ V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry, The National Academy of Sciences of Ukraine, 1 Murmanska str., Kyiv, 02094, Ukraine.
⁹ Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, San Sebastián, 20018, Spain.
¹⁰ IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, Bilbao, 48013, Spain.

PMID: 40119787
DOI: 10.1002/chem.202500662

Review

Fluorine in the Pharmaceutical Industry: FDA-Approved Fluorine-Containing Drugs in 2024

Youlong Du et al. Chemistry. 2025 May.

. 2025 May;31(25):e202500662.

doi: 10.1002/chem.202500662. Epub 2025 Apr 21.

Authors

Youlong Du¹, Yeping Bian², Daniel Baecker³, Gagan Dhawan^{4

5}, Anas Semghouli⁶, Loránd Kiss⁶, Wei Zhang⁷, Alexander E Sorochinsky⁸, Vadim A Soloshonok^{9

10}, Jianlin Han¹

Affiliations

¹ Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, International Innovation Center for Forest Chemicals and Materials, College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, China.
² Department of Intensive Care Unit, Geriatric Hospital of Nanjing Medical University, No.30 Luojia Road, Nanjing, 210024, China.
³ Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Straße 2+4, 14195, Berlin, Germany.
⁴ School of Allied Medical Sciences, Delhi Skill and Entrepreneurship University, Dwarka, New Delhi, 110077, India.
⁵ Department of Biomedical Science, Acharya Narendra Dev College, University of Delhi, Kalkaji, New Delhi, 110019, India.
⁶ Institute of Organic Chemistry, Stereochemistry Research Group, HUN-REN Research Centre for Natural Sciences, Magyar tudósok krt. 2, Budapest, H-1117, Hungary.
⁷ Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Boulevard, Boston, MA, USA, 02125.
⁸ V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry, The National Academy of Sciences of Ukraine, 1 Murmanska str., Kyiv, 02094, Ukraine.
⁹ Department of Organic Chemistry I, Faculty of Chemistry, University of the Basque Country UPV/EHU, Paseo Manuel Lardizábal 3, San Sebastián, 20018, Spain.
¹⁰ IKERBASQUE, Basque Foundation for Science, María Díaz de Haro 3, Plaza Bizkaia, Bilbao, 48013, Spain.

PMID: 40119787
DOI: 10.1002/chem.202500662

Abstract

Fluorine has become an essential element in the development of modern pharmaceuticals, due to its unique chemical properties that can significantly enhance the biological activity, metabolic stability, and lipophilicity of drug molecules. This review explores recent advancements in the synthesis and application of fluorine-containing drugs approved by the US Food and Drug Administration (FDA) in 2024. These novel drugs demonstrate improved efficacy and safety profiles, addressing a range of therapeutic areas including oncology, infectious diseases, metabolic disorders and genetic disorders that affect the adrenal glands. The incorporation of fluorine atoms into drug candidates has facilitated the development of molecules with optimized pharmacokinetic and pharmacodynamic properties, leading to better patient outcomes. The review further discusses the synthetic methodologies employed, the structural characteristics of these drugs, and their clinical implications, providing insights into the ongoing innovation within the pharmaceutical industry driven by fluorine chemistry.

Keywords: asymmetric synthesis; blockbuster drugs; drug design and development; fluorine‐containing compounds; modern pharmaceuticals.

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References

1. P. Bhutani, G. Joshi, N. Raja, N. Bachhav, P. K. Rajanna, H. Bhutani, A. T. Paul, R. Kumar, J. Med. Chem. 2021, 64, 2339.
1. D. G. Brown, H. J. Wobst, J. Med. Chem. 2021, 64, 2312.
1. P. Das, M. D. Delost, M. H. Qureshi, D. T. Smith, J. T. Njardarson, J. Med. Chem. 2019, 62, 4265.
1. D. Douguet, ACS Med. Chem. Lett. 2018, 9, 204.
1. A. Mullard, Nat. Rev. Drug Discov. 2023, 22, 83.

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Fluorine in the Pharmaceutical Industry: FDA-Approved Fluorine-Containing Drugs in 2024

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Fluorine in the Pharmaceutical Industry: FDA-Approved Fluorine-Containing Drugs in 2024

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