Kombiglyze Xr (rINN) is an orally active hypoglycemic (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP -4) inhibitor class of drugs. FDA approved on July 31, 2009.
Post-administration of kombiglyze xr, GLP-1 and GIP levels rise up to 2- to 3- fold. Because it is very selective of DPP-4 inhibition, there are fewer systemic side effects. Kombiglyze Xr inhibits DPP-4 enzyme activity for a 24-hour period. It also decreased glucagon concentrations and increased glucose-dependent insulin secretion from pancreatic beta cells. The half maximal inhibitory concentration (IC50) is 0.5 nmol/L. Kombiglyze Xr did not prolong the QTc interval to a clinically significant degree.
Adverse reactions reported in ≥5% of patients treated with kombiglyze xr and more commonly than in patients treated with placebo are: upper respiratory tract infection, urinary tract infection, and headache.