European journal of medicinal chemistrySep 1, 2023

Overview of FDA-approved small fluorine-containing drugs from 2015 to 2022

Alzheimers & Treatments Weekly Brief ↗PubMed ↗DOI ↗

Updated Mar 31, 2026

Abstract

Over the last 50 years, numerous fluorinated compounds have been approved for clinical use.

Fluorinated corticosteroids and fluoroquinolones were successfully used in the 1950s and 1980s, respectively.
Fluorinated compounds exhibit diverse biological properties, including antitumor, antimicrobial, and anti-inflammatory activities.
The design of fluorinated pharmaceuticals benefits from enhanced potency and favorable absorption, distribution, metabolism, and excretion characteristics.
A review of approved fluorinated drugs from 2015 to 2022 was conducted.

Simplified

Fluorine-containing small molecules have occupied a special position in drug discovery research. The successful clinical use of fluorinated corticosteroids in the 1950s and fluoroquinolones in the 1980s led to an ever-increasing number of approved fluorinated compounds over the last 50 years. They have shown various biological properties such as antitumor, antimicrobial, and anti-inflammatory activities. Fluoro-pharmaceuticals have been considered a strong and practical tool in the rational drug design approach due to their benefits from potency and ADME (absorption, distribution, metabolism, and excretion) points of view. Herein, approved fluorinated drugs from 2015 to 2022 were reviewed.

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Overview of FDA-approved small fluorine-containing drugs from 2015 to 2022

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