Brequinar: Difference between revisions
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Revision as of 08:48, 29 November 2020
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| Clinical data | |
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| Trade names | Brequinar |
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| Chemical and physical data | |
| Formula | C23H15F2NO2 |
| Molar mass | 375.4 g·mol−1 |
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Brequinar (DuP-785) is a drug that acts as a potent and selective inhibitor of the enzyme dihydroorotate dehydrogenase. It blocks synthesis of pyrimidine based nucleotides in the body and so inhibits cell growth. It has been investigated as an immunosuppressant for preventing rejection after organ transplant and also as an anti-cancer drug, but was not accepted for medical use in either application largely due to its narrow therapeutic dose range and severe side effects when dosed inappropriately.[1][2] However it continues to be researched both as part of a potential combination therapy for some cancers,[3][4] or alternatively as an antiparasitic,[5] or antiviral drug.[6][7][8]
See also
- Leflunomide - Clinically used DHODH inhibitor
- Methotrexate - the most widely used pyrimidine synthesis inhibitor
References
- ^ Cramer DV (1995). "Brequinar sodium". Pediatric Nephrology. 9 Suppl: S52-5. doi:10.1007/bf00867685. PMID 7492488. S2CID 28974570.
- ^ Peters GJ (2018). "Re-evaluation of Brequinar sodium, a dihydroorotate dehydrogenase inhibitor". Nucleosides, Nucleotides & Nucleic Acids. 37 (12): 666–678. doi:10.1080/15257770.2018.1508692. PMID 30663496.
- ^ Vyas VK, Ghate M (October 2011). "Recent developments in the medicinal chemistry and therapeutic potential of dihydroorotate dehydrogenase (DHODH) inhibitors". Mini Reviews in Medicinal Chemistry. 11 (12): 1039–55. doi:10.2174/138955711797247707. PMID 21861807.
- ^ Madak JT, Bankhead A, Cuthbertson CR, Showalter HD, Neamati N (March 2019). "Revisiting the role of dihydroorotate dehydrogenase as a therapeutic target for cancer". Pharmacology & Therapeutics. 195: 111–131. doi:10.1016/j.pharmthera.2018.10.012. PMID 30347213. S2CID 53036782.
- ^ Boschi D, Pippione AC, Sainas S, Lolli ML (December 2019). "Dihydroorotate dehydrogenase inhibitors in anti-infective drug research". European Journal of Medicinal Chemistry. 183: 111681. doi:10.1016/j.ejmech.2019.111681. PMID 31557612.
- ^ Li SF, Gong MJ, Sun YF, Shao JJ, Zhang YG, Chang HY (August 2019). "Antiviral activity of brequinar against foot-and-mouth disease virus infection in vitro and in vivo". Biomedicine & Pharmacotherapy. 116: 108982. doi:10.1016/j.biopha.2019.108982. PMID 31146110.
- ^ Andersen PI, Krpina K, Ianevski A, Shtaida N, Jo E, Yang J, et al. (October 2019). "Novel Antiviral Activities of Obatoclax, Emetine, Niclosamide, Brequinar, and Homoharringtonine". Viruses. 11 (10): 964. doi:10.3390/v11100964. PMC 6832696. PMID 31635418.
{{cite journal}}: CS1 maint: unflagged free DOI (link) - ^ Park JG, Ávila-Pérez G, Nogales A, Blanco-Lobo P, de la Torre JC, Martínez-Sobrido L (January 2020). "Identification and characterization of novel compounds with broad spectrum antiviral activity against influenza A and B viruses". Journal of Virology. 94 (7). doi:10.1128/JVI.02149-19. PMC 7081893. PMID 31941776.