ULODESINE Purine nucleoside phosphorylase inhibitor, Treatment of gout

作者：Gras J^*

来源：Drugs of the Future, 2014, 39(2): 123-128.

DOI：10.1358/dof.2014.39.2.2111643

• Gout
• Arthritis
• Metabolic syndrome
• Ulodesine
• BCX-4208

Gout, considered one of the most painful forms of arthritis and strongly associated with metabolic syndrome, i.e., insulin resistance, obesity, hyperlipidemia and hypertension, is often unrecognized and undertreated. Ulodesine is a new, orally active, highly potent inhibitor of purine nucleoside phosphorylase (PNP) for the treatment of hyperuricemia and gout. In enzymatic assays, ulodesine inhibited human, mouse, rat and monkey PNPs in the low nanomolar range. In vitro studies in human liver microsomes and hepatocytes demonstrated that there is a low risk of drug-drug interactions between ulodesine and coadministered medications. In three phase II trials in patients with gout who failed to reach serum uric acid levels lower than 6 mg/dL on allopurinol alone, ulodesine as add-on therapy showed sustained efficacy in reducing serum uric acid and plasma xanthine and hypoxanthine levels, and the product was safe and well tolerated.

• 出版日期2014-2