Dipeptidyl peptidase-4 inhibitors

Dipeptidyl peptidase-4 inhibitors

Inhibitors of Dipeptidyl peptidase 4 , also DPP-4 inhibitors, are a new class of oral hypoglycemics which block DPP-4.

Their mechanism of action is thought to result from increased Incretin levels (GLP-1 and GIP), [ McIntosh CH, Demuth HU, Pospisilik JA, Pederson R. Dipeptidyl peptidase IV inhibitors: how do they work as new antidiabetic agents? Regul Pept. 2005 Jun 15;128(2):159-65. PMID:15780435 [http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=15780435&query_hl=1&itool=pubmed_docsum] .] [Behme MT, Dupre J, McDonald TJ. Glucagon-like peptide 1 improved glycemic control in type 1 diabetes. BMC Endocr Disord. 2003 Apr 10;3(1):3. PMID 12697069. [http://www.biomedcentral.com/1472-6823/3/3 Full Free Text] .] [Dupre J, Behme MT, Hramiak IM, McFarlane P, Williamson MP, Zabel P, McDonald TJ. Glucagon-like peptide I reduces postprandial glycemic excursions in IDDM.Diabetes. 1995 Jun;44(6):626-30. PMID 7789625.] which, inhibit glucagon release(which increases the blood glucose) but more importantly increase insulin secretion and decrease gastric emptying.

Drugs belonging to this class are vildagliptin [UTGlucagon|laf237 - Vildagliptin] , sitagliptin [UTGlucagon|mk-0431 - Sitagliptin] , saxagliptin and alogliptin.

Although extensive long-term, pre-clinical studies of the major DPP-4 inhibitors has failed to show any evidence of potential to cause tumors in laboratory animals, there was one in-vitro (i.e., test tube) study that has raised some questions. [ [http://content.nejm.org/cgi/medline/pmid;16908079 Masur K et al. DPPIV inhibitors extend GLP-2 mediated tumour promoting effects on intestinal cancer cells, Regul Pept. ,137 (3) p. 147-55 (2006)] PMID 16908079.]

Sitagliptin entered the Australian drug market in late 2007 for the treatment of difficult to control diabetes mellitus type 2.

References

External links

* [http://www.forbes.com/2004/01/26/cx_mh_rl_diabetestearsheet_5.html The race to get DPP-4 inhibitors to market] - Forbes.com


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