Onglyza (saxagliptin)
Potential health benefits and research finds
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Barnett A., University of Birmingham, and Ahrén B.Lund University
sum up the potential use of dipeptidyl peptidase 4 (DPP-4) inhibitors on
diabetes. Here are their explanation:

Dr. Barnett
"The dipeptidyl peptidase 4 (DPP-4) inhibitors enhance the body's own ability
to control blood glucose by increasing the active levels of incretin hormones
in the body. Their mechanism of action is distinct from any existing class of
oral glucose-lowering agents. They control elevated blood glucose by
triggering pancreatic insulin secretion, suppressing pancreatic glucagon
secretion, and signalling the liver to reduce glucose production. The leading
DPP-4 inhibitors have shown clinically significant HbA1c reductions up to 1
year of treatment and offer many potential advantages over existing diabetes
therapies including a low risk of hypoglycaemia, no effect on body weight,
and the potential, based on animal and in vitro studies, for the regeneration
and differentiation of pancreatic beta-cells."

Dr. Ahrén B.
Inhibition of dipeptidyl peptidase-4 (DPP-4) prevents the inactivation of
glucagon-like peptide-1 (GLP-1). This increases circulating levels of active
GLP-1, stimulates insulin secretion and inhibits glucagon secretion, resulting
in lowering of glucose levels and improvement of glycemic control in patients
with type 2 diabetes. Several DPP-4 inhibitors are emerging for therapeutic
use. Most experience exists for sitagliptin, vildagliptin, saxagliptin and
alogliptin.

Dipeptidyl peptidase 4 (DPP-4) are efficacious as monotherapy and also in
combination with commonly prescribed antidiabetic agents (metformin,
sulfonylurea and thiazolidinediones) and are suitable for once-daily oral
dosing.  Vildagliptin and alogliptin have also been shown to improve glycemic
control when added to insulin therapy, and sitagliptin improves glycemic
control in triple therapy with metformin plus thiazolidinedione.

DPP-4 inhibition also shows a favorable safety profile, high tolerability, only a
minimal risk of hypoglycemia, and body-weight neutrality.

Consequently, many DPP-4 inhibitors such as vildagliptin (Galvus; LAF-237),
sitagliptin (Januvia; MK-0431), and saxagliptin (BMS-477118) have advanced
into late-stage human clinical trials or been approved by US FDA.


SOURCE

Barnett A.DPP-4 inhibitors and their potential role in the management of type
2 diabetes. Int J Clin Pract. 2006 Nov;60(11):1454-70.

Ahrén B. Emerging dipeptidyl peptidase-4 inhibitors for the treatment of
diabetes. Expert Opin Emerg Drugs. 2008 Dec;13(4):593-607.