INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes.
INCB-13739, being developed by Incyte Corp, is a novel, first-in-class 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor for the potential treatment of metabolic disorders, including type 2 diabetes mellitus (T2DM) and obesity. INCB-13739 has high selectivity for 11beta-HSD1 over other dehydrogenases and glucocorticoid and mineralocorticoid receptors, with prolonged pharmacodynamic activity and good pharmacokinetic/pharmacodynamic properties. INCB-13739 demonstrated improved hepatic and peripheral insulin sensitivity with a satisfactory reduction in fasting plasma glucose and cholesterol after 28 days of treatment in patients with T2DM, with a dose-dependent weight loss, decrease in triglyceride levels and an improvement in blood pressure. Clinical data demonstrated that INCB-13739 had a better efficacy to tolerability ratio compared with potential competitors. The unique differentiation of INCB-13739 is its effects on both glucose and lipid parameters coupled with its effects on body weight and hypertension. The results from phase III clinical trials will be pivotal; however, the available data suggest that INCB-13739 has potential for success in the market.
Tiwari
Atul
A
Jubilant Biosys Ltd, Drug Discovery Unit 96, 2nd Stage, Industrial Suburb, Bangalore, India. atul_tiwari@jubilantbiosys.com
D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000818:Animals; D002986:Clinical Trials as Topic; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D004791:Enzyme Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D007004:Hypoglycemic Agents
D004791:Enzyme Inhibitors; D007004:Hypoglycemic Agents; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1