EPALRESTAT IS A CARBOXYLIC ACID DERIVATIVE THAT INHIBITS ALDOSE REDUCTASE, A RATE-LIMITING ENZYME OF THE POLYOL PATHWAYS. IN HYPERGLYCEMIA, EPALRESTAT, AN UNCOMPETITIVE ALDOSE REDUCTASE INHIBITOR, SIGNIFICANTLY REDUCES INTRACELLULAR SORBITOL ACCUMULATION, WHICH HAS BEEN RELATED IN THE PATHOGENESIS OF LATE-ONSET DIABETIC COMPLICATION LIKE NEUROPATHY, RETINOPATHY AND NEPHROPATHY.
IT HAS BEEN CONFIRMED IN DIABETIC ANIMAL EXPERIMENTS THAT EPALRESTAT IMPROVED NERVE-CONDUCTION VELOCITY, AND THIS WAS ACCOMPANIED BY AN IMPROVEMENT OF SORBITOL LEVELS AND NA+/K+- AT PASE ACTIVITY IN THE NERVE. AN IMPROVEMENT IN THE MORPHOLOGICAL ABNORMALITIES OF THE NERVES WAS ALSO OBSERVED IN EPALRESTAT TREATED DIABETICS.