The treatment on patients with T2DM who suffered from defective in
insulin secretion and inability of tissues responding to insulin
properly have been studied for decades. Currently, incretins-based
hypoglycemic agents have become a focus in treating T2DM and this kind
of drugs could be classified as GLP-1 receptor agonists which mimic the
function of GLP-1 and DPP-4 antagonists which avoid GLP-1 being
degraded. Both of them focused on GLP-1 polypeptide. Since
incretins-based hypoglycemic agents are widely used, the physiological
disposition is of great significance in discovering more effective drugs
and providing guidance on clinicals for treating T2DM. In the review, we
summarize the mechanisms of these two kinds of drugs and provide
information of the drugs currently be approved. In addition, the
physiological disposition of each type of GLP-1 receptor agonists and
DPP-4 antagonists are thoroughly reviewed. By this review, based on the
physiological disposition of these drugs, patients with different
situation could choose the drugs based on their physical conditions and
the need of supplementary treatment in avoid of drug interactions. We
also hope some drugs with novel structure with appropriate physiological
disposition could be inspired and invented.