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Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.
Zhang C, Xu M, He C, Zhuo J, Burns DM, Qian DQ, Lin Q, Li YL, Chen L, Shi E, Agrios C, Weng L, Sharief V, Jalluri R, Li Y, Scherle P, Diamond S, Hunter D, Covington M, Marando C, Wynn R, Katiyar K, Contel N, Vaddi K, Yeleswaram S, Hollis G, Huber R, Friedman S, Metcalf B, Yao W. Zhang C, et al. Bioorg Med Chem Lett. 2022 Aug 1;69:128782. doi: 10.1016/j.bmcl.2022.128782. Epub 2022 May 7. Bioorg Med Chem Lett. 2022. PMID: 35537608
Reiterative optimization provided valuable insight into the bioactive conformation of our novel scaffold and led to the discovery of INCB13739. Clinical evaluation of INCB13739 confirmed for the first time that tissue-specific inhibition of 11beta-HSD1 in patients w …
Reiterative optimization provided valuable insight into the bioactive conformation of our novel scaffold and led to the discovery of INCB …
11beta-Hydroxysteroid dehydrogenase type 1 inhibitors: novel agents for the treatment of metabolic syndrome and obesity-related disorders?
Anagnostis P, Katsiki N, Adamidou F, Athyros VG, Karagiannis A, Kita M, Mikhailidis DP. Anagnostis P, et al. Metabolism. 2013 Jan;62(1):21-33. doi: 10.1016/j.metabol.2012.05.002. Epub 2012 May 30. Metabolism. 2013. PMID: 22652056 Review.
In view of this concept, novel compounds, such as adamantyltriazoles, arylsulfonamidothiazoles, anilinothiazolones, BVT2733, INCB-13739, MK-0916 and MK-0736, are currently under investigation and the preliminary findings from both experimental and human studies show …
In view of this concept, novel compounds, such as adamantyltriazoles, arylsulfonamidothiazoles, anilinothiazolones, BVT2733, INCB- …
11β-Hydroxysteroid dehydrogenase type 1 inhibition in type 2 diabetes mellitus.
Hollis G, Huber R. Hollis G, et al. Diabetes Obes Metab. 2011 Jan;13(1):1-6. doi: 10.1111/j.1463-1326.2010.01305.x. Diabetes Obes Metab. 2011. PMID: 21114597 Review.
In patients with T2DM failing metformin monotherapy, INCB13739 treatment achieves significant reductions in haemoglobin A1c (HbA1c) and fasting plasma glucose (FPG), and when present improves hyperlipidaemia and hypertriglyceridaemia. ...This review summarizes the therapeu …
In patients with T2DM failing metformin monotherapy, INCB13739 treatment achieves significant reductions in haemoglobin A1c (HbA1c) a …
The 11-beta-hydroxysteroid dehydrogenase type 1 inhibitor INCB13739 improves hyperglycemia in patients with type 2 diabetes inadequately controlled by metformin monotherapy.
Rosenstock J, Banarer S, Fonseca VA, Inzucchi SE, Sun W, Yao W, Hollis G, Flores R, Levy R, Williams WV, Seckl JR, Huber R; INCB13739-202 Principal Investigators. Rosenstock J, et al. Diabetes Care. 2010 Jul;33(7):1516-22. doi: 10.2337/dc09-2315. Epub 2010 Apr 22. Diabetes Care. 2010. PMID: 20413513 Free PMC article. Clinical Trial.
Basal cortisol homeostasis, testosterone in men, and free androgen index in women were unchanged by INCB13739. Adverse events were similar across all treatment groups. CONCLUSIONS: INCB13739 added to ongoing metformin therapy was efficacious and well tolerated in pa …
Basal cortisol homeostasis, testosterone in men, and free androgen index in women were unchanged by INCB13739. Adverse events were si …
INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes.
Tiwari A. Tiwari A. IDrugs. 2010 Apr;13(4):266-75. IDrugs. 2010. PMID: 20373256 Review.
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 we …
Clinical data demonstrated that INCB-13739 had a better efficacy to tolerability ratio compared with potential competitors. Th …
11beta-hydroxysteroid dehydrogenase type 1 inhibitors as promising therapeutic drugs for diabetes: status and development.
Ge R, Huang Y, Liang G, Li X. Ge R, et al. Curr Med Chem. 2010;17(5):412-22. doi: 10.2174/092986710790226147. Curr Med Chem. 2010. PMID: 20015040 Review.
Lowering intracellular glucocorticoid concentrations through administration of small molecule 11beta-HSD1 selective inhibitors, significantly attenuates the signs and symptoms of disease in preclinical animal models and clinical trials of diabetes and metabolic syndrome. Among pu …
Lowering intracellular glucocorticoid concentrations through administration of small molecule 11beta-HSD1 selective inhibitors, significantl …