Drug intelligence / Profile preview

Alrestatin

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Alrestatin is a small molecule inhibitor of aldose reductase (AKR1B1), an enzyme involved in the polyol pathway that catalyzes the reduction of glucose to sorbitol during hyperglycemia. This mechanism is implicated in the pathogenesis of diabetic complications such as diabetic neuropathy. Alrestatin was first synthesized in 1969 and became the first orally bioavailable aldose reductase inhibitor to enter clinical trials for diabetes-related complications. However, its development was discontinued due to a high incidence of adverse effects, particularly hepatotoxicity, and lack of significant clinical efficacy. It was never approved or marketed for clinical use[1][3][5][7].

Other names
alrestatin sodium阿司他丁
02

Targets

AR (Adrenergic receptors)

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