Vildagliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV 
(DPP-4), orally active, that improves glycemic control in patients with type 2 
diabetes (T2DM) primarily by enhancing pancreatic (alpha and beta) islet 
function. Thus vildagliptin has been shown both to improve insulin secretion and 
to suppress the inappropriate glucagon secretion seen in patients with T2DM. 
Vildagliptin reduces HbA(1c) when given as monotherapy, without weight gain and 
with minimal hypoglycemia, or in combination with the most commonly prescribed 
classes of oral hypoglycemic drugs: metformin, a sulfonylurea, a 
thiazolidinedione, or insulin. Metformin, with a different mode of action not 
addressing beta-cell dysfunction, has been used for about 50 years and still 
represents the universal first line therapy of all guidelines. However, given 
the multiple pathophysiological abnormalities in T2DM and the progressive nature 
of the disease, intensification of therapy with combinations is typically 
required over time. Recent guidelines imply that patients will require 
pharmacologic combinations much earlier to attain and sustain the increasingly 
stringent glycemic targets, with careful drug selection to avoid unwanted 
adverse events, especially hypoglycemia. The combination of metformin and 
vildagliptin offers advantages when compared to currently used combinations with 
additive efficacy and complimentary mechanisms of action, since it does not 
increase the risk of hypoglycemia and does not promote weight gain. Therefore, 
by specifically combining these agents in a single tablet, there is considerable 
potential to achieve better blood glucose control and to improve compliance to 
therapy.