The dipeptidyl peptidase inhibitors (DPP-4) are a class of anti-diabetics approved for the oral treatment of type 2 diabetes mellitus (DM). That act by preventing the degradation of incretin hormones: which play an important role in insulin secretion and blood glucose regulation. The DPP-4 inhibitors have the potential to offer beneficial effects beyond the improvement of glycemic control which lies with the functional ability of the DPP-4 enzyme to cleave a variety of peptides other than incretins that have established renal and cardiovascular effects. Linagliptin (Lina) is distinctive amongst gliptins because it is the only compound that can be eliminated via a non-renal pathway, so a reduction in the glomerular filtration rate doesn't require dose adjustment. In addition, Lina is the only identified DPP-4 inhibitor that has been evaluated in a multicenter randomized clinical trial designed to thoroughly evaluate cardio-renal outcomes in patients with type 2 DM. This review provides a brief overview of the current literature on the renoprotective effects of Lina in experimental models of acute and chronic kidney disease (CKD) and clinical studies and sheds some light on the underlying mechanisms of protection.