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Abstract
Sitagliptin, a dipeptidyl peptidase 4 inhibitor, was the first in its class to receive approval from the US FDA in 2006 for the treatment of Type 2 diabetes mellitus. It has been evaluated in numerous clinical trials and has several attractive features as an antidiabetic agent, including a low risk for hypoglycemia, a neutral effect on weight, and an ability to be used in chronic kidney disease and more. This article provides an up-to-date discussion of the pharmacokinetics/pharmacodynamics, clinical efficacy, safety and tolerability of sitagliptin.
Financial & competing interests disclosure
The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
Sitagliptin is efficacious in randomized clinical trials in reducing A1c, fasting plasma glucose, and 2 h postprandial glucose and has also demonstrated effectiveness in the real world.
Sitagliptin is weight neutral, low risk for hypoglycemia, and generally well tolerated by patients, including the elderly and those with renal dysfunction or nonalcoholic fatty liver disease
Long-term studies need to be conducted to examine sitagliptin’s effect on diabetes complications.
Current data has not shown a causal link between incretin therapies and pancreatitis or pancreatic cancer.
Sitagliptin is not associated with increased cardiovascular risk in several studies and could possibly have a cardioprotective effect.