Introduction: Saxagliptin (see drug summary box) is a glucose-lowering agent that belongs to the class of Dipeptidylpeptidase-4 (DDP-4) inhibitors used in the treatment of T2DM. Clinical efficacy of saxagliptin as single agent as well as in combination with other medications used for the treatment of T2DM has been well established in several randomized trials. Treatment with saxagliptin is effective, generally safe and well tolerated, apart from a small increase in the incidence of infections such as nasopharyngitis. Its use is not associated with increase risk of hypoglycemia and it is weight neutral. Saxagliptin can be used safely in renal failure (with dose adjustment) and in hepatic impairment. When saxagliptin is used in combination with a strong inhibitor of CYP3A4/A5, reduction in the daily dosage is recommended.
Areas covered: This paper briefly discusses efficacy and pharmacokinetics of saxagliptin. The paper highlights in detail saxagliptin-associated adverse effects, drug interactions, its use in patients with renal and hepatic disease and long-term safety concerns.
Expert opinion: Saxagliptin has comparable efficacy with other DPP-4 inhibitors. It is generally safe and well tolerated; however, it requires dose adjustment in renal disease as well as when used with drugs that are strong inhibitor or inducer of CYP3A4/A5 isoforms. Future safety questions regarding immune system and development of cancer still remain to be completely answered.