brequinar sodium

Brequinar sodium is a potent, selective, and non-competitive inhibitor of the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which catalyzes the fourth step in the de novo pyrimidine biosynthetic pathway. By depleting intracellular pools of uridine and cytidine, brequinar exerts potent antiproliferative effects on rapidly dividing cells, such as cancer cells and activated lymphocytes. Originally developed in the 1980s by DuPont Pharmaceuticals for the treatment of solid tumors and as an immunosuppressant for organ transplantation, its clinical development was initially hampered by a narrow therapeutic window. Recently, interest in brequinar has been revitalized, with investigations focusing on its potential in treating acute myeloid leukemia (AML) by inducing differentiation, as well as its broad-spectrum antiviral activity against RNA viruses, including SARS-CoV-2, by limiting the availability of nucleotides required for viral replication.

Brand names

Brequinar

Other names

brequinar sodium salt6-fluoro-2-(2'-fluoro-1,1'-biphenyl-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium salt