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XRF-1021 is an orally active, small-molecule homeodomain-interacting protein kinase 2 (HIPK2) inhibitor and dual URAT1/GLUT9 inhibitor developed by Shenzhen Famayi Pharmaceutical Technology for the treatment of gout with hyperuricemia. It lowers serum uric acid levels by inhibiting the renal uric acid transporters URAT1 and GLUT9 (both GLUT9a and GLUT9b), thereby reducing renal uric acid reabsorption and enhancing excretion. Additionally, through its inhibition of HIPK2, XRF-1021 exhibits anti-inflammatory and anti-fibrotic properties, which may alleviate renal tubular injury and tubulointerstitial fibrosis associated with chronic kidney disease and hyperuricemia.
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