Pharmacokinetic Characterization of KR-67500, a Novel 11β-HSD1 Inhibitor |
Im, So Hee
(College of Pharmacy, Chungnam National University)
Ahn, Jin Hee (Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology) Kim, Ki Young (Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology) Bae, Myung Ae (Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology) Kim, Sang Kyum (College of Pharmacy, Chungnam National University) Ahn, Sung-Hoon (College of Pharmacy, Kangwon National University) |
1 | Morton, N. M. : Obesity and corticosteroids: 11betahydroxysteroid type 1 as a cause and therapeutic target in metabolic disease. Mol. Cell Endocrinol. 316, 154 (2010). DOI |
2 | Walker, B. R. and Andrew, R. : Tissue production of cortisol by 11beta-hydroxysteroid dehydrogenase type 1 and metabolic disease. Ann. N. Y. Acad. Sci. 1083, 165 (2006). DOI |
3 | Wamil, M. and Seckl, J. R. : Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Discov. Today 12, 504 (2007). DOI |
4 | Hollis, G. and Huber, R. : 11-Hydroxysteroid dehydrogenase type 1 inhibition in type 2 diabetes mellitus. Diabetes Obes. Metab. 13, 1 (2011). |
5 | Harno, E., Cottrell, E. C., Yu, A., DeSchoolmeester, J., Gutierrez, P. M., Denn, M., Swales, J. G., Goldberg, F. W., Bohlooly-Y, M., Andersen, H., Wild, M. J., Turnbull, A. V., Leighton, B. and White, A. : 11-Hydroxysteroid dehydrogenase type 1 (11-HSD1) inhibitors still improve metabolic phenotype in male 11-HSD1 knockout mice suggesting off-target mechanisms. Endocrinology 154, 4580 (2013). DOI |
6 | Wamil, M., Battle, J. H., Turban, S., Kipari, T., Seguret, D., de Sousa Peixoto, R., Nelson, Y. B., Nowakowska, D., Ferenbach, D., Ramage, L., Chapman, K. E., Hughes, J., Dunbar, D. R., Seckl, J. R. and Morton, N. M. : Novel fat depot-specific mechanisms underlie resistance to visceral obesity and inflammation in 11-hydroxysteroid dehydrogenase type 1- deficient mice. Diabetes 60, 1158 (2011). DOI |
7 | Park, J. S., Rhee, S. D., Kang, N. S., Jung, W. H., Kim, H. Y., Kim, J. H., Kang, S. K., Cheon, H. G., Ahn, J. H. and Kim, K. Y. : Anti-diabetic and anti-adipogenic effects of a novel selective 11-hydroxysteroid dehydrogenase type 1 inhibitor, 2-(3-benzoyl)-4-hydroxy-1,1-dioxo-2H-1,2-benzothiazine-2-yl- 1-phenylethanone (KR-66344). Biochem. Pharmacol. 81, 1028 (2011). DOI |
8 | Tiwari, A. : INCB-13739, an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for the treatment of type 2 diabetes. IDrugs 13, 266 (2010). |
9 | Veniant, M. M., Hale, C., Hungate, R. W., Gahm, K., Emery, M. G., Jona, J., Joseph, S., Adams, J., Hague, A., Moniz, G., Zhang, J., Bartberger, M. D., Li, V., Syed, R., Jordan, S., Komorowski, R., Chen, M. M., Cupples, R., Kim, K. W., St. Jean, D. J. Jr., Johansson, L., Henriksson, M. A., Williams, M., Vallgarda, J., Fotsch, C. and Wang, M. : Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2- ((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5- methylthiazol-4(5H)-one (AMG 221). J. Med. Chem. 53, 4481 (2010). DOI |
10 | Park, J. S., Bae, S. J., Choi, S. W., Son, Y. H., Park, S. B., Rhee, S. D., Kim, H. Y., Jung, W. H., Kang, S. K., Ahn, J. H., Kim, S. H. and Kim, K. Y. : A novel 11-HSD1 inhibitor improves diabesity and osteoblast differentiation. J. Mol. Endocrinol. 52, 191 (2014). DOI |
11 | Lin, J. H. and Lu, A. Y. : Role of pharmacokinetics and metabolism in drug discovery and development. Pharmacol. Rev. 49, 403 (1997). |
12 | 식품의약품안전청, 식품의약품안전평가원: 생명공학의약품의약동학 시험 가이드라인 (2010). |
13 | Pacifici, G. M. and Viani, A. : Methods of determining plasma and tissue binding of drugs. Pharmacokinetic consequences. Clin. Pharmacokinet. 23, 449 (1992). DOI |