| Summary: | Linagliptin, one of the five dipeptidyl peptidase-4 inhibitors available, has recently entered the market both in US and in most European countries for the treatment of type 2 diabetes mellitus. It presents a xanthine-based structure, and is characterized by unique pharmacokinetics, with non-linear profile, long terminal half-life allowing prolonged exposure to the drug. It is eliminated predominately through the intestinal tract and only minimally into urine, so that it can be administered, without any dose adjustment, in conditions of renal impairment. Linagliptin is effective in modifying all parameters of hyperglycemia either in monotherapy, or as add-on therapy, together with metformin or a sulphonylurea. It exhibits also a good tolerability profile with the appearance of few side effects, absence (when used in monotherapy) or low risk (when in combination with a sulphonylurea) of hypoglycemia. More importantly it has a neutral weight gain effect. A comprehensive report of the literature on linagliptin is provided, paying attention in particular to pre-clinical studies, interactions with other drugs, safety and tolerability and results obtained in animal models that highlight properties of linagliptin suggestive of potential additional uses. Particularly promising appear in fact data demonstrating a positive effect of linagliptin on metabolic dysfunction and renal and/or cardiovascular damage together with the more recently reported effects of linagliptin on tissue repair and neuroprotection.
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