Drug intelligence / Profile preview

acetohexamide

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Acetohexamide is an intermediate‐acting, first-generation oral sulfonylurea used to treat type 2 diabetes mellitus, particularly in patients whose blood glucose cannot be controlled by diet alone. It lowers blood sugar by stimulating pancreatic beta cells to secrete insulin and increasing insulin sensitivity at receptor sites. The drug acts by binding to ATP-sensitive potassium channel (KATP channel) on the pancreatic beta cell membrane, causing depolarization and subsequent opening of voltage-gated calcium channels; this leads to increased intracellular calcium and enhanced insulin secretion. Acetohexamide is metabolized in the liver to its active metabolite, 1-hydrohexamide. It has been discontinued in the US market due to safety concerns with first-generation sulfonylureas[1][2][5].

Brand names
DymelorDimelorGamadiabet
Other names
acetohexamideAcetohexamidacetoesamide3-cyclohexyl-1-(p-acetylphenylsulfonyl)urea1-(4-acetylbenzenesulfonyl)-3-cyclohexylurea4-acetyl-N-(cyclohexylcarbamoyl)benzenesulfonamide
02

Targets

SUR1 (Sulfonylurea receptor 1)

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