@article{ec6c77b2c5a44822a43b2f48aa6b5177,
title = "Highlights on U.S. FDA-approved fluorinated drugs over the past five years (2018–2022)",
abstract = "The objective of this review is to provide an update on the fluorine-containing drugs approved by U.S. Food and Drug Administration in the span of past five years (2018–2022). The agency accepted a total of fifty-eight fluorinated entities to diagnose, mitigate and treat a plethora of diseases. Among them, thirty drugs are for therapy of various types of cancers, twelve for infectious diseases, eleven for CNS disorders, and six for some other diseases. These are categorized and briefly discussed based on their therapeutic areas. In addition, this review gives a glimpse about their trade name, date of approval, active ingredients, company developers, indications, and drug mechanisms. We anticipate that this review may inspire the drug discovery and medicinal chemistry community in both industrial and academic settings to explore the fluorinated molecules leading to the discovery of new drugs in the near future.",
keywords = "Cancer, CNS disorders, Diagnosis, Drug development, Drug discovery, FDA-approved drugs, Fluorinated drugs, Fluorine, Infectious diseases, PET imaging, Therapeutics",
author = "Saghir Ali and Jia Zhou",
note = "Funding Information: This work is partly supported by the grant R01 DA038446 from the National Institutes of Health , the John D. Stobo, M.D. Distinguished Chair Endowment Fund (JZ), and Edith & Robert Zinn Chair in Drug Discovery Endowment Fund (JZ). Funding Information: The prevalence of fluorine or groups of fluorine atoms or its isotope in the FDA-approved drugs manifests its significant role in the pharmaceutical research in terms of diagnosis and therapeutics. Judicious deployment of fluorine or groups of fluorine atoms in a molecule under investigation may lead to enhanced pharmacological and pharmacokinetic profiles with improved potency, decrease in pKa, higher permeability, decrease in clearance, and conformational constraint [ 31–34]. Inspired by the outstanding performance, sustainability, and a high pace of approval of fluorinated drugs in the past decade, pharmaceutical companies continued to explore fluorine-containing entities in an expectation to discover new medications to combat deadly diseases. It is noteworthy that FDA granted approval to four fluorine-containing drugs 59–62 within merely three months of 2023 (Fig. 7). FDA approved Rykindo 59 and Jaypirca 60 for the treatment of schizophrenia and mantle cell lymphoma, respectively. Subsequently, Skyclarys 61 received approval for the therapy of Friedrich's Ataxia. In addition, FDA granted approval to Joenja 62 for the treatment of activated phosphoinositide 3-kinase delta syndrome. The approval of these four drugs within such a short period of this year warrants that fluorine or group of fluorine atoms play a pivotal role in the pharmaceutical industry, indicating a great potential in the future trends of drug discovery and development.This work is partly supported by the grant R01 DA038446 from the National Institutes of Health, the John D. Stobo, M.D. Distinguished Chair Endowment Fund (JZ), and Edith & Robert Zinn Chair in Drug Discovery Endowment Fund (JZ). Publisher Copyright: {\textcopyright} 2023 Elsevier Masson SAS",
year = "2023",
month = aug,
day = "5",
doi = "10.1016/j.ejmech.2023.115476",
language = "English (US)",
volume = "256",
journal = "European journal of medicinal chemistry",
issn = "0223-5234",
publisher = "Elsevier Masson SAS",
}