Gemigliptin, a potent, selective and long-acting DPP 4 inhibitor was developed by LG Life Sciences and approved for use in patients with type 2 diabetes mellitus by the Korean Food and Drug Administration in June 2012 under the trade name Zemiglo®. Clinical pharmacokinetic and pharmacodynamic data suggest the efficacy and once daily dosing of gemigliptin. In clinical phase III studies, gemigliptin was efficacious as either monotherapy or combination therapy (add-on to metformin) and well tolerated in patients with type 2 diabetes. Further development of combination therapy is on-going.
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Cefalu, W.T., and S. Urquhart. 2007. Clinical management strategies for type 2 diabetes. Journal of the American Academy of Physician Assistants Suppl: 9–14.
Drucker, D.J. 2007. Dipeptidyl peptidase-4 inhibition and the treatment of type 2 diabetes: preclinical biology and mechanisms of action. Diabetes Care 30: 1335–1343.
Hwang, D.M., S.H. Kim, M.K. Yoon, O.H. Kwon, K.D. Koo, C.H. Min, S.H. Lee, J.I. Lee, C.S. Lee, H.J. Yim. 2008. LC15-0444 is a novel, potent, selective, and orally active dipeptidyl peptidase IV inhibitor. Poster presented at the annual meeting of American Diabetes Association. San Francisco: CA.
Kim, S.E., S. Yi, K.H. Shin, T.E. Kim, M.J. Kim, Y.H. Kim, S.H. Yoon, J.Y. Cho, S.G. Shin, I.J. Jang, and K.S. Yu. 2012. Evaluation of the pharmacokinetic interaction between the dipeptidyl peptidase IV inhibitor LC15-0444 and pioglitazone in healthy volunteers. International Journal of Clinical Pharmacology and Therapeutics 50: 17–23.
Lankas, G.R., B. Leiting, R.S. Roy, G.J. Eiermann, M.G. Beconi, T. Biftu, C.C. Chan, S. Edmondson, W.P. Feeney, H. He, D.E. Ippolito, D. Kim, S.K.A. Lyon, H.O. Ok, R.A. Patel, A.N. Petrov, K.A. Pryor, X. Qian, L. Reigle, A. Woods, J.K. Wu, D. Zaller, X. Zhang, L. Zhu, A.E. Weber, and N.A. Thornberry. 2005. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: Potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes 54: 2988–2994.
Lim, K.S., J.Y. Cho, B.H. Kim, J.R. Kim, H.S. Kim, D.K. Kim, S.H. Kim, H.J. Yim, S.H. Lee, S.G. Shin, I.J. Jang, and K.S. Yu. 2009. Pharmacokinetics and pharmacodynamics of LC15-0444, a novel dipeptidyl peptidase IV inhibitor, after multiple dosing in healthy volunteers. British Journal of Clinical Pharmacology 68: 883–890.
Lim, K.S., J.R. Kim, Y.J. Choi, K.H. Shin, K.P. Kim, J.H. Hong, J.Y. Cho, H.S. Shin, K.S. Yu, S.G. Shin, O.H. Kwon, D.M. Hwang, J.A. Kim, and I.J. Jang. 2008. Pharmacokinetics, pharmacodynamics, and tolerability of the dipeptidyl peptidase IV inhibitor LC15-0444 in healthy Korean men: A dose-block-randomized, double-blind, placebo-controlled, ascending single-dose. Phase I study. Clinical Therapeutics 30: 1817–1830.
Noh, Y.H., H.S. Lim, S.J. Jin, M.J. Kim, Y.H. Kim, H.R. Sung, H.Y. Choi, and K.S. Bae. 2012. Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: A crossover drug–drug interaction study in healthy male Korean volunteers. Clinical Therapeutics 34: 1182–1194.
Ohnuma, K., N.H. Dang, and C. Morimoto. 2008. Revisiting an old acquaintance: CD26 and its molecular mechanisms in T cell function. Trends in Immunology 29: 295–301.
Rhee, E.J., W.Y. Lee, K.H. Yoon, S.J. Yoo, I.K. Lee, S.H. Baik, Y.K. Kim, M.K. Lee, K.S. Park, J.Y. Park, B.S. Cha, H.W. Lee, K.W. Min, H.Y. Bae, M.J. Kim, J.A. Kim, D.K. Kim, and S.W. Kim. 2010. A multicenter, randomized, placebo-controlled, double-blind phase II trial evaluating the optimal dose, efficacy and safety of LC 15–0444 in patients with type 2 diabetes. Diabetes Obesity and Metabolism 12: 1113–1119.
Rhee, E.J., W.Y. Lee, K.W. Min, V.K. Shivane, A.R. Sosale, H.C. Jang, C.H. Chung, I.S. Nam-Goong, J.A. Kim, S.W. Kim. Gemigliptin Study 006 Group. 2013. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor gemigliptin compared with sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Obesity and Metabolism 15: 523–530.
Yang, S.J., K.W. Min, S.K. Gupta, J.Y. Park, V.K. Shivane, S.U. Pitale, P.K. Agarwal, A. Sosale, P. Gandhi, M. Dharmalingam, V. Mohan, U. Mahesh, D.M. Kim, Y.S. Kim, J.A. Kim, P.K. Kim, S.H. Baik. 2012. A multicentre, multinational, randomized, placebo-controlled, double-blind, phase 3 trial to evaluate the efficacy and safety of gemigliptin (LC15-0444) in patients with type II diabetes. Diabetes Obesity and Metabolism 15: 410–416.
This study was partially supported by a grant from the Ministry of Knowledge Economy (Bio-Star, 10024075).
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Kim, S., Lee, S. & Yim, H. Gemigliptin, a novel dipeptidyl peptidase 4 inhibitor: first new anti-diabetic drug in the history of Korean pharmaceutical industry. Arch. Pharm. Res. 36, 1185–1188 (2013). https://doi.org/10.1007/s12272-013-0171-x