Next generation organofluorine containing blockbuster drugs

Jianlin, Han and Remete, Attila Márió and Dobson, Luca S. and Kiss, Loránd and Izawa, Kunisuke and Moriwaki, Hiroki and Soloshonok, Vadim A. and O'Hagan, David (2020) Next generation organofluorine containing blockbuster drugs. JOURNAL OF FLUORINE CHEMISTRY, 239. p. 109639. ISSN 0022-1139

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Abstract

The role of organo-fluorine compounds in modern health, food and energy related industries is widelyappreciated. The unique properties that fluorine imparts to organic molecules, stemming from its high electronegativity and stability when bound to carbon, finds it increasingly being used in the development of new bioactivities. Around 25 % of the current blockbuster drugs contain fluorine and this number is increasing to well above 30 % for recent FDA approvals. In this Review we highlight a selection of the most successful organofluorine drugs, that have achieved blockbuster status, namely, sitagliptin (diabetes), sofosbuvir (hepatitis C), emtricitabine (HIV), glecaprevir/pibrentasvir (hepatitis C), elvitegravir (HIV), dolutegravir (HIV), bictegravir (HIV), efavirenz (HIV), enzalutamide (prostate cancer), aubagio (immunomodulatory) and paliperidone palmitate (schizophrenia). For each compound we discuss their discovery, their relevant disease state and how they are made, emphasizing the source of fluorine-containing moieties, and where known, their mode of action.

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