FDA-Approved Fluorine-Containing Molecules in 2024: Significance, Synthesis, and Therapeutic Applications

Abstract: For the past 75 years, the development pipeline of fluorinated drugs has exemplified the strategic use of fluorine to enhance key pharmacological properties, including bioavailability, metabolic stability, and target affinity. Consequently, fluorine incorporation has become a cornerstone in drug design, inspiring continuous research and development efforts across both academic and industrial sectors. Each year, numerous reviews highlight the ongoing importance of fluorinated drugs and aim to keep the field updated on emerging advancements. This review provides a comprehensive evaluation of the structural and functional benefits of fluorine in medicinal chemistry, presenting an extensive analysis of FDA-approved fluorine-containing drugs from 2015 to 2024. Special attention is paid to the latest approvals from 2024, with a focus on their mechanisms of action and detailed synthetic methodologies.