Abstract
4/2010
vol. 5
Review paperNew direction in diabetes treatment – incretinomimetics and DPP-4 inhibitors
Przegląd Kardiodiabetologiczny 2010; 5 (3, 4): 171–181
Online publish date: 2011/01/13
Incretin hormones are produced and released from intestine during food digesting. There are two incretin hormones: glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). Both of them stimulate pancreatic cells to release insulin. Only 20% of GLP-1 released from intestine reach cells, mainly due to the dipeptidyl peptidase-4 enzyme (DPP-4) actions. DPP-4 inactivates GLP-1 in 4-5 min. In healthy persons incretin hormones are responsible for up to 70% of insulin release after a meal. In type 2 diabetes (DM2) incretin effect is disturbed. Exogenous administration of GLP-1 and GIP restore early phase of insulin release in DM2 patients. Late phase of insulin release is re-established only after GLP-1 administration. That is why only GLP-1 is used in therapy of DM2. There are two strategies of DM2 treatment, which involve intervention in incretin axis. First of them is administration of GLP-1 receptor agonist – exenatide or GLP-1 analog – liraglutide. Second of them is based on inhibition of DPP-4 enzyme – sitagliptin, vildagliptin or saksagliptin. All of those strategies regulate glucose level in blood, but only GLP-1 receptor agonist and GLP-1 analog may also cause body mass reduction. This work describes mechanism of action of incretin based drugs and also summarizes results of third phase of clinical studies.
Keywords
diabetes, incretinomimetics, DPP-IV inhibitors