Immunosuppressant; DHODH inhibitor. Inhibits Sars-CoV-2 in cells, possibly through UTP depletion. Xiong et al. bioRxiv, Mar 12 2020, https://doi.org/10.1101/2020.03.11.983056.
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- Applications:Approved drug (U.S.); in COVID-19 clinical trials
Biochemicals & reagents
1) Teschner et al. (2010), Leflunomide: a drug with a potential beyond rheumatology; Immunotherapy, 2 637 2) Davis et al. (1996), The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase; Biochemistry, 35 1270 3) Latchoumycandane et al. (2007), Mitochondrial protection by the JNK ninhibitor leflunomide rescues mice from acetaminophen-induced liver injury; Hepatology, 45 412
Leflunomide is a pyrimidine biosynthesis inhibitor DMARD (disease-modifying antirheumatic drug) (1) which also displays immunomodulatory activity inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH) (2), although the molecule directly responsible for DHODH is actually A77 1726, a metabolite of Leflunomide. This compound also rescues mice from acetaminophen-induced liver injury (3).