The DOI matches its Crossref record; 102 of the 102 references it cites were found in a registry or an index.
Next generation organofluorine containing blockbuster drugs
Abstract
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 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 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.
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Cites
Fluorine in medicinal chemistry
Purser, S., Moore, P. R., Swallow, S., & Gouverneur, V. (2008) · Chem. Soc. Rev. · doi:10.1039/b610213c · Cited by 7,570
Wang, J., Sánchez-Roselló, M., Aceña, J. L., del Pozo, C., Sorochinsky, A. E., Fustero, S., Soloshonok, V. A., & Liu, H. (2014) · Chemical Reviews · doi:10.1021/cr4002879 · Cited by 4,847
Self-citationZhou, Y., Wang, J., Gu, Z., Wang, S., Zhu, W., Aceña, J. L., Soloshonok, V. A., Izawa, K., & Liu, H. (2016) · Chemical Reviews · doi:10.1021/acs.chemrev.5b00392 · Cited by 2,808
Self-citationFluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design
Meanwell, N. A. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01788 · Cited by 2,655
Contribution of Organofluorine Compounds to Pharmaceuticals
Inoue, M., Sumii, Y., & Shibata, N. (2020) · ACS Omega · doi:10.1021/acsomega.0c00830 · Cited by 1,944
Current Contributions of Organofluorine Compounds to the Agrochemical Industry
Ogawa, Y., Tokunaga, E., Kobayashi, O., Hirai, K., & Shibata, N. (2020) · iScience · doi:10.1016/j.isci.2020.101467 · Cited by 1,253
Successful fluorine-containing herbicide agrochemicals
Fujiwara, T., & O’Hagan, D. (2014) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2014.06.014 · Cited by 894
Self-citationFluorine in health care: Organofluorine containing blockbuster drugs
O’Hagan, D. (2010) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2010.03.003 · Cited by 856
Self-citationKim, D., Wang, L., Beconi, M., Eiermann, G. J., Fisher, M. H., He, H., Hickey, G. J., Kowalchick, J. E., Leiting, B., Lyons, K., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm0493156 · Cited by 822
Zhu, Y., Han, J., Wang, J., Shibata, N., Sodeoka, M., Soloshonok, V. A., Coelho, J. A. S., & Toste, F. D. (2018) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00778 · Cited by 640
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Cited by
Chemical Aspects of Human and Environmental Overload with Fluorine
Han, J., Kiss, L., Mei, H., Remete, A. M., Ponikvar-Svet, M., Sedgwick, D. M., Roman, R., Fustero, S., Moriwaki, H., & Soloshonok, V. A. (2021) · Chemical Reviews · doi:10.1021/acs.chemrev.0c01263 · Cited by 537
Self-citationFluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity
Yu, Y., Liu, A., Dhawan, G., Mei, H., Zhang, W., Izawa, K., Soloshonok, V. A., & Han, J. (2021) · Chinese Chemical Letters · doi:10.1016/j.cclet.2021.05.042 · Cited by 182
Self-citationKhan, M. F., & Murphy, C. D. (2021) · Applied Microbiology and Biotechnology · doi:10.1007/s00253-021-11675-3 · Cited by 52
Alam, M. K., Qian, B., Davis, G. B., Donn, M., Kumar, A., Trinchi, A., Kyratzis, I. (., Kirby, J. K., Lan, M., Zhao, H., et al. (2026) · Ecotoxicology and Environmental Safety · doi:10.1016/j.ecoenv.2026.120038 · Cited by 7
Metadata
- Authors
- Han, J., Remete, A. M., Dobson, L. S., Kiss, L., Izawa, K., Moriwaki, H., Soloshonok, V. A., & O’Hagan, D.
- Venue
- Journal of Fluorine Chemistry
- Publisher
- Elsevier BV
- Published
- 2020-11
- Volume
- 239
- Pages
- 109639
- ISSN
- 0022-1139 (ISSN-L)
- OpenAlex
- W3087684284
- Cited by
- 313
- References
- 102
- FWCI
- 14.69
- Type
- journal article
- Language
- en
- Open access
- closed
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- Han, 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. https://doi.org/10.1016/j.jfluchem.2020.109639
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