Abstract: Recent developments in biomedicinal applications of fluorine-containing compounds are reviewed. Biochemical and mechanistic aspects of this field are discussed first. The development of enzyme inhibitors and other pharmacological tools and medicinal agents is considered from the point of view of how the special properties of fluorine can be exploited in analogue design. In the second part of this review, an array of recent medicinal candidates is described, encompassing drugs that show promise for the treatment of a variety of diseases. In both sections, the emphasis has been on material published within the past five years.