tolrestat

Tolrestat is a small molecule aldose reductase inhibitor that was developed for the control of certain diabetic complications, particularly those related to chronic hyperglycemia such as diabetic neuropathy. Its mechanism of action involves inhibition of the enzyme aldose reductase, which catalyzes the conversion of glucose to sorbitol in the polyol pathway. By blocking this enzyme, tolrestat reduces intracellular accumulation of sorbitol and fructose, which are implicated in diabetic tissue damage. Tolrestat was approved and marketed in several countries under brand names such as Alredase and Lorestat but failed Phase III trials in the United States due to toxicity concerns—specifically severe liver toxicity—and never received FDA approval. The drug was discontinued by Wyeth in 1997 because of these safety issues[1][2][3][5].

Brand names

AlredaseLorestat

Other names

tolrestatin82964-04-3