Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM, and used for the treatment of diabetic neuropathy.
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Aldose reductase, a cytosolic oxidoreductase in the polyol pathway that catalyzes the reduction of a variety of aldehydes and carbonyls, including the reduction of glucose to sorbitol, is important for various organs. Epalrestat is a noncompetitive and reversible aldose reductase inhibitor with IC50 of 72 nM. Epalrestat can reduce sorbitol accumulation both in animals and in humans by attenuating high glucose-mediated neutrophil-endothelial cell adhesion and decreasing the levels of carboxymethyl-lysine. 50 mg oral administration of epalrestat could reach a peak plasma concentration of 3.9 µg/ml only in 1 hr in healthy adults with a protein binding rate of 90.1%. In patients with somatic diabetic neuropathy, the treatment group received epalrestat 50 mg 3 times/day had a significant increase from baseline in MNCV and SNCV as well as the significant difference from baseline in the threshold of vibratory sensation and the higher disappearance rate of spontaneous pain in the upper limbs and lower limbs. In another group, 45 non–insulin-dependent diabetes patients also received 50 mg epalrestat 3 times/day, the results reported significant improvement regarding spontaneous pain, not significant upper extremities and significant VPT in right tibial and radial styloid processes. 28 patients with mild or no symptoms of diabetic neuropathy were treated with 150 mg/day epalrestat, the least F wave latencies and tibial motor nerves were not shortened[1]. In mice plasma, the linearity with a correlation coefficient of 0.9994 was obtained when examined by epalrestat with range of 2-5000 ng/ml and the accuracy and precision were significant in a dose-dependent way with average RSD% values less than 12.3%. Epalrestat could be rapidly absorbed and distributed in many tissues at 10 min after oral administration.[2]
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