Tolrestat is a thioamide-based inhibitor of aldose reductase with an IC50 activity of 35 nM. (1) Along with other similar therapies, Tolrestat has implications in the treatment of diabetic complications, such as diabetic neuropathy, in a manner independent of insulin-related control of blood glucose levels. (2)

In rat diabetes models, Tolrestat reduces sorbitol concentrations in the sciatic nerve and eye lens, as well as prevents diabetic retinopathy, cateracts, thickening of the retinal basement membrane, and nerve dysfunction. Additionally, Tolrestat reduces urinary albumin excretion. (3)