zopolrestat

Zopolrestat is a potent, orally active small molecule inhibitor of aldose reductase (AKR1B1), an enzyme involved in the polyol pathway that catalyzes the reduction of glucose to sorbitol during hyperglycemia. By inhibiting aldose reductase, zopolrestat was developed to prevent or treat diabetic complications such as neuropathy, nephropathy, and cardiomyopathy. The drug normalizes sorbitol and fructose levels in tissues affected by diabetes and has demonstrated efficacy in preclinical models for restoring normal renal plasma flow and correcting metabolic imbalances associated with diabetes. Despite promising pharmacokinetics and mechanism-based rationale, clinical development was discontinued after phase 2 trials for diabetic complications[1][3][4][6][8].

Brand names

XediaAlond

Other names

ZopolrestatumZopolrestatum [INN-Latin]2-[4-oxo-3-[[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl]phthalazin-1-yl]acetic acid3,4-dihydro-4-oxo–3–[[5-(trifluoromethyl)-2-benzothiazolyl]methyl]-1-phthalazineacetic acid