Important fluorinated drugs in experimental and clinical use

This reviews details selected fluorine-containing drugs that either have potential for, or are already in, clinical use. Fluorine imparts desirable characteristics to drugs by modulating both the pharmacokinetics and pharmacodynamic properties of a drug. Therefore, incorporation of fluorine into a drug increases the lipophilicty enhancing absorption into biological membranes whereby its small covalent radius can facilitate docking with their drug receptor(s). By emphasising those structural features that modulate the absorption and metabolism of these compounds, when possible, structure-function relationships are discussed. Drug types are classified according to their therapeutic indication and utility rather than structural type and include phospodiesterase inhibitors, antiparasitic agents (especially antimalarials), anticancer compounds (such as kinases), antibacterials, and selected probes useful for F-18 positron emission tomography. (C) 2002 Elsevier Science B.V. All rights reserved.