PMID- 20373256 OWN - NLM STAT- MEDLINE DCOM- 20100914 LR - 20100407 IS - 2040-3410 (Electronic) IS - 1369-7056 (Linking) VI - 13 IP - 4 DP - 2010 Apr TI - INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes. PG - 266-75 AB - 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. FAU - Tiwari, Atul AU - Tiwari A AD - Jubilant Biosys Ltd, Drug Discovery Unit 96, 2nd Stage, Industrial Suburb, Bangalore, India. atul_tiwari@jubilantbiosys.com LA - eng PT - Journal Article PT - Review PL - England TA - IDrugs JT - IDrugs : the investigational drugs journal JID - 100883655 RN - 0 (Enzyme Inhibitors) RN - 0 (Hypoglycemic Agents) RN - EC 1.1.1.146 (11-beta-Hydroxysteroid Dehydrogenase Type 1) SB - IM MH - 11-beta-Hydroxysteroid Dehydrogenase Type 1/*antagonists & inhibitors MH - Animals MH - Clinical Trials as Topic MH - Diabetes Mellitus, Type 2/*drug therapy MH - Enzyme Inhibitors/adverse effects/chemistry/pharmacokinetics/*therapeutic use MH - Humans MH - Hypoglycemic Agents RF - 103 EDAT- 2010/04/08 06:00 MHDA- 2010/09/15 06:00 CRDT- 2010/04/08 06:00 PHST- 2010/04/08 06:00 [entrez] PHST- 2010/04/08 06:00 [pubmed] PHST- 2010/09/15 06:00 [medline] PST - ppublish SO - IDrugs. 2010 Apr;13(4):266-75.