Efficacy and safety of Jentadueto® (linagliptin plus metformin)

Abstract

Introduction: Metformin is the first-choice drug in the management of type 2 diabetes. However, most patients require a combined therapy to reach and/or maintain targets of glucose control. Dipeptidyl peptidase-4 (DPP-4) inhibitors offer new options for combined therapy with metformin. Linagliptin shares a similar pharmacodynamic (PD) profile with other gliptins, but has a unique pharmacokinetic (PK) profile characterized by negligible renal excretion.

Areas covered: An extensive literature search was performed to analyze the potential PK/PD interactions between linagliptin and metformin. They are not prone to PK drug–drug interactions. The two compounds may be administered together, either separately or using a fixed-dose combination (FDC) as shown by bioequivalence studies. The addition of linagliptin in patients not well controlled with metformin alone has proven its efficacy in improving glucose levels with a good safety profile. Initial co-administration of linagliptin plus metformin improves glucose control more potently than either compound separately, without hypoglycemia, weight gain or increased metformin-related gastrointestinal side effects.

Expert opinion: The linagliptin plus metformin combination may offer some advantages over the classical sulfonylurea–metformin combination. Even if linagliptin is safe in patients with renal impairment, the use of metformin (and thus of the linagliptin plus metformin FDC) is still controversial in this population.

Keywords::

• DPP-4 inhibitor
• fixed-dose combination
• linagliptin
• metformin
• pharmacokinetics
• type 2 diabetes mellitus