Highlights on U.S. FDA-approved fluorinated drugs over the past five years (2018–2022)

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. [Display omitted] •Small molecule FDA-approved fluorinated drugs in the past five years have been reviewed.•The therapeutic areas of these drugs such as cancers, infections and CNS disorders are classified.•Drug action targets and mechanisms of fluorinated drugs are provided.•The attempts to rationalize the presence of fluorination in approved drugs have been made.•Perspectives for the future of fluorinated drug development are discussed.