Description
Epalrestat is the second aldose reductase inhibitor to be introduced worldwide and the
first to be launched in Japan. The compound is indicated for the treatment of diabetic
neuropathy. It is also being investigated for diabetic retinopathy and nephropathy.
Chemical Properties
Red Solid
Uses
An aldose reductase inhibitor. It is used in treatment of diabetic neuropathy.
Uses
Epalrestat has been used as an aldose reductase inhibitor:
- in the dahomey larvae diet fed forDrosophila
- for non-irradiated and X-ray irradiated human aldose reductase
- to test its protective effect in mice with bleomycin-induced pulmonary fibrosis
Uses
Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM
Definition
ChEBI: A monocarboxylic acid that is 1,3-thiazolidine which is substituted on the nitrogen by a carboxymethyl group, at positions 2 and 4 by thioxo and oxo groups, respectively, and at position 5 by a 2-methyl-3-phenylprop-2-en-1-ylidene group. It is an inhibitor
of aldose reductase (which catalyses the conversion of glucose to sorbitol) and is used for the treatment of some diabetic complications, including neuropathy.
Biochem/physiol Actions
Epalrestat inhibits Aldose Reductase (AR) involved in the rate limiting step in the conversion of glucose to sorbitol under hyperglycemic conditions. Aldose reductase has been the target of multiple clinical investigatons to treat diabetic neuropathy and retinopathy. Epalrestat is an approved drug in Japan and India, used for the treatment of diabetic neuropathy.
References
1) Kikkawa?et al. (1983)?Effect of a new aldose reductase inhibitor, (E)-3-carboxymethyl-5-[(2E)-methyl-3-phenylpropenylidene]rhodanine (ONO-2235), on peripheral nerve disorders in streptozotocin diabetic rats; Diabetologica,?24?290
2) Terashima?et al. (1984)?Effects of a new aldose reductase inhibitor on various tissues in vitro; J. Pharmacol. Exp. Ther.,?229?226
3) Ramirez and Borja (2008)?Epalrestat: an aldose reductase inhibitor for the treatment of diabetic neuropathy; Pharmacotherapy,?28?646
