Drug intelligence / Profile preview

glibenclamide

Development stage
Approved
Lead developer
Hoechst
Modality
Small Molecules
Administration
Oral
01

Overview

Glibenclamide (also known as glyburide) is a second-generation sulfonylurea oral antidiabetic drug used primarily for the treatment of type 2 diabetes mellitus. It works by binding to and inhibiting ATP-sensitive potassium channels (KATP) via the sulfonylurea receptor 1 (SUR1) on pancreatic beta cells, leading to cell membrane depolarization, opening of voltage-dependent calcium channels, increased intracellular calcium, and subsequent stimulation of insulin release. Glibenclamide may also inhibit hepatic glucose production by increasing portal vein insulin levels or acting directly on the liver. It is not effective in type 1 diabetes or in patients with severely impaired beta-cell function. The drug is taken orally and has a high protein binding rate (~95%). Common side effects include hypoglycemia, nausea, heartburn, weight gain, and bloating[1][4][5].

Brand names
DiabetaGlycronGlynase PresTabMicronase
Other names
glyburide格列本脲
02

Targets

KCNJ11 (Atp-sensitive inward rectifier potassium channel 11)

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