Abstract: Promoting uric acid excretion is an important approach for the treatment of gout and hyperuricemia. There are two main approaches included in the mechanism: one is inhibiting the function of renal tubular uric acid transporter to reduce the absorption of uric acid, and promoting excretion; the other is using uricase to catalyze the oxidation of uric acid to a more water-soluble allantoin that can also increase excretion. The mechanisms and progress of the uricosuric drugs are reviewed in this paper, providing reference for the further research and development.