Sitagliptin: the fixed combination of the first dipeptidyl peptidase 4 inhibitor and metformin

Abstract

Worldwide, there is an increasing incidence of type 2 diabetes mellitus (T2DM). Management of patients with T2DM is complex and often requires multiple pharmacological treatments to achieve adequate control of the disease. The long-term diabetes-specific complications have been ameliorated by interventions that decrease chronic glycemia. Most clinical guidelines recommend metformin as the first-line oral hypoglycemic agent. Metformin can be used for monotherapy and combination therapy for T2DM. Initially, metformin monotherapy is often effective, although the effect of glucose control is limited after all, so a second agent is often required in most patients. Unfortunately, the traditional therapeutic drugs for T2DM could not effectively control hyperglycemia, and frequently occurring side effects remain a big problem (weight gain, hypoglycemia). Dipeptidyl peptidase 4 inhibitors are superior to traditional hypoglycemic drugs in terms of efficacy and tolerability. Sitagliptin became the first representative of dipeptidyl peptidase 4 inhibitors. Sitagliptin has been shown to preserve β-cell function and improve 2-h postprandial glucose, fasting plasma glucose and glycated hemoglobin in individuals with T2DM. A systematic review and meta-analysis conducted in 2021 demonstrated that sitagliptin administration with or without metformin might reduce the body weight and body mass index if these drugs are taken for more than 6 months. Sitagliptin add on to metformin achieving better treating effects on weight loss and glucose control without the development of hypoglycemia. This review discusses sitagliptin and its combination with metformin. Velmetia is a fixed combination of these two hypoglycemic drugs with a complementary and safe action profile.