There are two reasons for the high level of serum uric acid,which induces hyperuricemia.Excessive uricogenesis is considered to be one of the risk factors.Xanthine oxidase is the main drug therapy target in hyperuricemia,which is one of the key enzymes conducting the metabolism of uric acid.The lack of excretion is another reason for the excessive level of uric acid.Uric acid transport is achieved by various kinds of transporters expressed in the membranes of the renal tubular epithelial cells.Gene mutations or deletions of the transporters are the main reasons for abnormal serum uric acid level.Gene expression regulations of these transporters by relevant drugs are the main method to conduct the excretion of uric acid.In this paper,recent advances in the study of the drug therapy targets have been reviewed in those two aspects.