Dipeptidyl peptidase IV is a key regulator of insulin- stimulating hormones, glucagon-like peptide
and glucose dependent insulinotrophic polypeptide. Thus it is a promising target for treatment of
type 2 Diabetes mellitus. Inhibition of plasma Dipeptidyl peptidase IV enzyme lead to enhanced
endogenous glucagon like peptide-1, GIP activity which ultimately results in the potentiating of
insulin secretion by pancreatic cell and subsequent lowering blood glucose level, HbA [1c],
glucose secretion, liver glucose production. One of the principal goals of diabetes management is
to attain haemoglobin HbA [1c] treatment goals and prevent the onset or decrease the rate of
occurrence of Microvascular conditions.2, 6 numerous treatment options are available for
management of Type 2 Diabetes mellitus, various class of DPP IV inhibitor being explored such as
Sitagliptin and Vildagliptin successfully launched. Several other novel DPP IV inhibitors are in
pipeline, Unless there are clear contraindications, metformin monotherapy is prescribed, and if
HbA [1c] targets are not attained after 3 months, 1 of several classes of agents could be added,
such as sulfonylurea’s, Thiazolidinediones, dipeptidyl peptidase-4 inhibitors, - glucagon like
peptide-1 receptor agonists, or basal insulin.2,6 Despite the broad range of therapeutic options, the
attainment of HbA [1c] goals among patients with diabetes remains challenging, with just slightly
more than half (52%) of diabetes patients attaining the common HbA [1c] goal of < 7.0%. The
present review summarizes latest preclinical and clinical trial data of different DPP IV inhibitors
with a special emphasis on their DPP8/9 fold selectivity and therapeutic advantages over GLP-1
based approach.
Keywords: Diabetes 2, Dipeptidyl Peptidase-4, glucose-dependent insulinot