Next generation organofluorine containing blockbuster drugs

Jianlin Han, Attila Márió Remete, Luca S. Dobson, Lorand Kiss, Kunisuke Izawa, Hiroki Moriwaki, Vadim A. Soloshonok, David O’Hagan*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

46 Citations (Scopus)
2 Downloads (Pure)

Abstract

The role of organo-fluorine compounds in modern health, food and energy related industries is widely-appreciated. The unique properties that fluorine imparts to organic molecules, stemming from its high electronegativity and stability when bound to carbon, finds it increasing 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 organo-fluorine 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.
Original languageEnglish
Article number109639
JournalJournal of Fluorine Chemistry
Volume239
Early online date20 Sept 2020
DOIs
Publication statusPublished - Nov 2020

Keywords

  • Fluorine
  • Blockbuster drugs
  • Disease states
  • Synthetic routes
  • Fluorinated pharmaceuticals

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