By the year 2030, diabetes mellitus will globally become the seventh leading cause of death. Currently, 382 million individuals worldwide have diabetes mellitus, with 80% residing in low- and middle-income countries. At present, Type 2 diabetes mellitus (T2DM) accounts for 85-95% of the diabetes burden in high-income countries. Alarmingly, this figure may be higher in the low- and middle-income nations. In an effort to combat this silent but deadly disease, pharmaceutical manufacturers have developed a host of different agents, each targeting a specific biochemical pathway. Among the most recent additions to this armament is linagliptin/metformin HCl, a fixed combination therapy compound manufactured by Boehringer Ingelheim. This novel formulation combines metformin, an insulin sensitizer, with linagliptin, a dipeptidyl peptidase-4 enzyme inhibitor. This review will discuss the pharmacokinetic properties of this molecule, assess clinical efficacy and gauge its place in the treatment algorithm for T2DM.