Drug intelligence / Profile preview

mk-0941

Development stage
Phase 2
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK‑0941 is an orally active, selective, allosteric glucokinase activator (GKA) developed for the treatment of type 2 diabetes. It activates glucokinase (hexokinase subtype IV) with high selectivity over other hexokinase isoforms. In clinical studies, MK‑0941 improved glycemic control when added to insulin glargine therapy in patients with type 2 diabetes; however, these effects were not sustained over time. The drug was associated with increased incidence of hypoglycemia and elevations in triglycerides and blood pressure. Chronic toxicity studies in animals revealed cataract formation at exposures above those planned for human use[1][2][4][5][6].

Other names
3-((6-(ethylsulfonyl)-3-pyridinyl)oxy)-5-(2-hydroxy-1-methylethoxy)-N-(1-methyl-1H-pyrazol-3-yl)benzamide1137916-97-2MK0941 mesylateMK-0941 mesylateMK 0941 mesylate83OY2D8970
02

Targets

GCK (Glucokinase)

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