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dc.contributor.authorHan, Jianlin
dc.contributor.authorRemete, Attila Márió
dc.contributor.authorDobson, Luca S.
dc.contributor.authorKiss, Lorand
dc.contributor.authorIzawa, Kunisuke
dc.contributor.authorMoriwaki, Hiroki
dc.contributor.authorSoloshonok, Vadim A.
dc.contributor.authorO’Hagan, David
dc.identifier.citationHan , J , Remete , A M , Dobson , L S , Kiss , L , Izawa , K , Moriwaki , H , Soloshonok , V A & O’Hagan , D 2020 , ' Next generation organofluorine containing blockbuster drugs ' , Journal of Fluorine Chemistry , vol. 239 , 109639 .
dc.identifier.otherPURE: 270305750
dc.identifier.otherPURE UUID: 78e46693-87c0-4c93-bb0e-f6ad45b06199
dc.identifier.otherRIS: urn:354B1E9A5114A3BBE5EF3B668EBF6141
dc.identifier.otherScopus: 85091678227
dc.identifier.otherWOS: 000581700400007
dc.descriptionFunding: the National Natural Science Foundation of China (No. 21761132021), the Hungarian Research Foundation (NKFIH No. K 119282), and Ministry of Human Capacities, Hungary grant 20391-3/2018/FEKUSTRAT. The Qinlan Project of Jiangsu Province, and IKERBASQUE, the Basque Foundation for Science are also acknowledged.en
dc.description.abstractThe 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.
dc.relation.ispartofJournal of Fluorine Chemistryen
dc.rightsCopyright © 2020 Elsevier B.V. All rights reserved. This work has been made available online in accordance with publisher policies or with permission. Permission for further reuse of this content should be sought from the publisher or the rights holder. This is the author created accepted manuscript following peer review and may differ slightly from the final published version. The final published version of this work is available at
dc.subjectBlockbuster drugsen
dc.subjectDisease statesen
dc.subjectSynthetic routesen
dc.subjectFluorinated pharmaceuticalsen
dc.subjectQD Chemistryen
dc.titleNext generation organofluorine containing blockbuster drugsen
dc.typeJournal itemen
dc.contributor.institutionUniversity of St Andrews.School of Chemistryen
dc.contributor.institutionUniversity of St Andrews.EaSTCHEMen
dc.contributor.institutionUniversity of St Andrews.Biomedical Sciences Research Complexen
dc.description.statusPeer revieweden

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