MK-0916

MK-0916 is a small molecule inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), an enzyme that catalyzes the conversion of inactive cortisone to active cortisol. By inhibiting this enzyme, MK-0916 aims to reduce local tissue glucocorticoid levels and thereby improve metabolic parameters. It was developed for the treatment of type 2 diabetes mellitus, metabolic syndrome, obesity-related conditions, and hypertension. Clinical studies showed that MK-0916 was generally well tolerated and produced modest dose-dependent reductions in blood pressure and body weight as well as a small reduction in HbA1c at higher doses; however, it did not significantly improve fasting plasma glucose compared to placebo. The drug also led to mechanism-based activation of the hypothalamic-pituitary-adrenal axis with increases in adrenal androgen levels within normal ranges[2][5][6]. Development has not progressed beyond phase 2.

Other names

3-[trans-1-(4-chlorophenyl)-3-fluorocyclobutyl]-4,5-dicyclopropyl-4H-1,2,4-triazole