Topiroxostat is a selective, non-purine xanthine oxidoreductase (XOR) inhibitor indicated for the treatment of hyperuricemia and gout. It reduces serum uric acid levels by inhibiting the enzymatic conversion of hypoxanthine and xanthine into uric acid during purine metabolism. Chemically known as 4-5-(4-Pyridinyl)-1H-1,2,4-triazole-3-yl-2-pyridinecarbonitrile, Topiroxostat has a molecular formula of C₁₃H₈N₆ and a molecular weight of 248.24 g/mol. The drug exhibits good solubility in organic solvents, limited aqueous solubility, and a half-life of approximately 5 hours. Pharmacokinetically, Topiroxostat is rapidly absorbed with peak plasma concentrations reached within 0.67 hours, exhibits high plasma protein binding (>97.5%), undergoes hepatic metabolism primarily via glucuronidation, and is excreted through feces and urine. In addition to gout management, it shows potential benefits in chronic kidney disease, heart failure, and diabetic nephropathy. Several analytical techniques including UV spectrophotometry, HPLC, and RP-HPLC have been developed and validated for its quantitative estimation, demonstrating excellent linearity, precision, accuracy, and sensitivity. This review summarizes the physicochemical properties, mechanism of action, pharmacokinetics, therapeutic uses, adverse effects, and analytical methods of Topiroxostat.
Ahamed* et al. (Sun,) studied this question.