Drug intelligence / Profile preview

epalrestat choline

Development stage
Unknown
Lead developer
BioNevia Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Epalrestat choline is a cocrystal formulation combining epalrestat, an aldose reductase inhibitor, with choline. Epalrestat is a noncompetitive and reversible inhibitor of aldose reductase, the key enzyme in the polyol pathway implicated in diabetic complications such as neuropathy. By inhibiting this enzyme, it reduces intracellular sorbitol accumulation and improves nerve function in diabetes mellitus. The addition of choline may enhance stability and handling properties of the drug formulation[4]. Epalrestat is approved for improving symptoms associated with diabetic peripheral neuropathy including abnormal vibration sense and heart rate changes[1][5]. It has also shown potential anti-inflammatory effects via inhibition of NLRP3 inflammasome activation[2].

Other names
epalrestat cholinecholine cocrystal of epalrestat
02

Targets

AR (Adrenergic receptors)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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