Dipeptidyl peptidase IV inhibitor

If a patient has inadequate control on two drugs, adding a third class can be considered (e.g., a glitazone, exenatide, a dipeptidyl peptidase-IV inhibitor, or basal insulin). Therapy should be guided by the A 1C, FPG, cost, additional benefits (e.g., weight loss), and avoidance of side effects). 

Case History JANUVIA (Sitagliptin), a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes... 

A similar but simpler 4-imino-hexahydropyrrolo[l,2-tf]pyrazin-l(277)-one 311 was prepared starting from the product obtained by nucleophilic substitution of a primary amine to the bromoacetamide of the L-prolylnitrile 310 (Scheme 40). The cyclization occurred directly in basic medium by refluxing for 96 h in EtOAc. This compound showed a potent activity as an orally bioavailable dipeptidyl peptidase IV inhibitor with anti-hyperglycemic properties <2003JME2774>. 

Dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes... 

For recent reviews see Weber, A.E. (2004) Dipeptidyl peptidase IV inhibitors for the treatment of diabetes. Journal of Medicinal Chemistry, 47, 4135-4141 (b)... 

C., Piteau, S., Demuth, H.-U., McIntosh, C.H.S. and Pederson, R. (2003) Dipeptidyl peptidase IV inhibitor treatment stimulates P-cell survival and islet neogenesis in streptozotodn-induced diabetic rats. Diabetes, 52, 741-750. 

H., Lyons, K.A., Thornberry, N.A. and Weber, A.E. (2004) Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors. Bioorganic e[ Medicinal Chemistry Letters, 14, 1265-1268. 

Mastracchio, A., Parmee, E.R., Leiting, B., Marsilio, F., Patel, R., Thornberry, N. A. and Edmondson, S.D. (2004) Heterocycle fused cyclohexylglycine derivatives as novel dipeptidyl peptidase-IV inhibitors. Heterocycles, 62, 203-206. 

A.E. (2006) (2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-l-yl)-N,N-dimethyl-4-oxo-2-(4-[l,2,4]triazolo[l,5-a]pyridin-6-ylphenyl)butanamide a selective a-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Journal of Medicinal Chemistry, 49, 3614-3627. 

P. Van der Veken, I. Kertesz, K. Senten, A. Haemers, K. Augustyns, Synthesis of ( )- and (Z)-fluoro-olefin analogs of potent dipeptidyl peptidase IV inhibitors. Tetrahedron Lett. 44 (2003) 6231-6234. 

P.E. Wiedeman, J.M. Trevillyan, Dipeptidyl peptidase IV inhibitors for the treatment of impaired glucose tolerance and type 2 diabetes, Curr. Opin. Investig. Drugs (Thomson Curr. Drugs) 4 (2003) 412-420. 

Miller S, St Onge EL. Sitagliptin a dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Ann Pharmacother 2006 40(7-8) 1336 l3. 

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