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
Wikimedia Foundation.
2010.
Look at other dictionaries:
Development of dipeptidyl peptidase-4 inhibitors — Dipeptidyl peptidase 4 inhibitors (DPP 4 inhibitors) are enzyme inhibitors that inhibit the enzyme dipeptidyl peptidase 4 (DPP 4) and are a potent treatment for type 2 diabetes. Inhibition of the DPP 4 enzyme prolongs and enhances the activity of … Wikipedia
Dipeptidyl peptidase-4 — Ribbon diagram of human DPP 4. From PDB 1PFQ … Wikipedia
Dipeptidyl peptidase-4 inhibitor — DPP 4 inhibitors and GLP 1 Inhibitors of dipeptidyl peptidase 4, also DPP 4 inhibitors or gliptins, are a class of oral hypoglycemics that block DPP 4. They can be used to treat diabetes mellitus type 2. The first agent of the class sitagliptin… … Wikipedia
Dipeptidyl-Peptidase-4-Inhibitor — Sitagliptin, Leitsubstanz der neuen Antidiabetika Klasse der Dipeptidyl Peptidase 4 Inhibitoren Inhibitoren der Dipeptidylpeptidase 4, auch kurz als DPP4 Inhibitoren oder als Inkretinverstärker bezeichnet, sind Substanzen, welche den Abbau des… … Deutsch Wikipedia
Dipeptidyl-Peptidase-IV-Inhibitor — Sitagliptin, Leitsubstanz der neuen Antidiabetika Klasse der Dipeptidyl Peptidase 4 Inhibitoren Inhibitoren der Dipeptidylpeptidase 4, auch kurz als DPP4 Inhibitoren oder als Inkretinverstärker bezeichnet, sind Substanzen, welche den Abbau des… … Deutsch Wikipedia
Dipeptidyl Peptidase 4 Inhibitor — Sitagliptin, Leitsubstanz der neuen Antidiabetika Klasse der Dipeptidyl Peptidase 4 Inhibitoren Inhibitoren der Dipeptidylpeptidase 4, auch kurz als DPP4 Inhibitoren oder als Inkretinverstärker bezeichnet, sind Substanzen, welche den Abbau des… … Deutsch Wikipedia
Dipeptidyl Peptidase IV Inhibitor — Sitagliptin, Leitsubstanz der neuen Antidiabetika Klasse der Dipeptidyl Peptidase 4 Inhibitoren Inhibitoren der Dipeptidylpeptidase 4, auch kurz als DPP4 Inhibitoren oder als Inkretinverstärker bezeichnet, sind Substanzen, welche den Abbau des… … Deutsch Wikipedia
Discovery and development of small molecule c-Met inhibitors — The c Met (mesenchymal epithelial transition) tyrosine kinase stimulates cell scattering, invasion, protection from apoptosis and angiogenesis.[1] c Met is a receptor tyrosine kinase,[2] which can cause a wide variety of different cancers, such… … Wikipedia
Saxagliptin — Systematic (IUPAC) name (1S,3S,5S) 2 [(2S) 2 amino 2 (3 hydroxy 1 adamantyl) acetyl] 2 azabicyclo[3.1.0]hexane 3 carbonitrile Clinical data … Wikipedia
Chemismus der Dipeptidylpeptidase 4 — Das Enzym Dipeptidylpeptidase 4 (kurz DPP 4, DP IV oder DPP IV) wurde erstmals 1964/66 von Hopsu Havu beschrieben. Erst im Laufe der Zeit wurde erkannt, dass dieses Enzym wesentliche Funktionen im menschlichen und tierischen Organismus ausübt.[1] … Deutsch Wikipedia
