Benzarone is an active metabolite of the urate anion transporter 1 (URAT1) inhibitor benzbromarone .^1,2It inhibits URAT1 inXenopusoocytes expressing the human enzyme (IC₅₀= 2.8 µM).²Benzarone also inhibits the tyrosine phosphatase activity of eyes absent homolog 3 (EYA3; IC₅₀= 17.5 µM), as well as reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 7.5 µM.³It uncouples oxidative phosphorylation in isolated rat liver mitochondria and induces apoptosis and necrosis in isolated rat hepatocytes.⁴Benzarone (25 µg/g) reduces tumor growth in an A-673 Ewing sarcoma mouse xenograft model.⁵

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