Uric acid (UA) transporters, including urate transporter 1 (URAT1), glucose transporter 9 (GLUT9), and ATP-binding cassette subfamily G member 2 (ABCG2), are involved in hyperuricemia. A novel selective urate reabsorption inhibitor, developed in Japan, reduces serum UA levels by selectively inhibiting URAT1. The Japanese Society of Gout and Nucleic Acid Metabolism published “Guidelines for the Management of Hyperuricemia and Gout (3rd edition, 2022-Supplementary Edition-)” in March 2022. This guideline provides valuable information for decision-making in clinical management of hyperuricemia.
 The balance of UA production and excretion aids in maintaining serum UA levels; imbalances lead to hypouricemia and hyperuricemia. In recent years, additional evidence and more information, including that on the risks of hyperuricemia, have become available. After lifestyle intervention, medication is the next step for treating hyperuricemia. The number of drugs for treating hyperuricemia is currently increasing; these are classified based on their mechanism of action (e.g., xanthine oxidoreductase inhibitors, uricosuric agents, and recombinant urate oxidase). Furthermore, various types of uricosuric agents are used as drugs that can lower UA levels; for example, SGLT2 inhibitors (oral hypoglycemic agents) are recognized to lower serum UA levels. The pharmacological profiles of drugs related with reducing UA levels are described in the above-mentioned guideline. Hence, herein, we introduce and focus on drugs act on UA transporters mentioned in the guideline.