Sitagliptin does not undergo extensive metabolism. In the liver sitagliptin partially metabolized by oxidation in a limited rate by the enzyme CYP3A4.Nevertheless, most of the drug is excreted in the intact form in the urine (more than 80%). Sitagliptin is filtered in renal glomerulus but also is actively excreted by active tubular secretion[24].
Six metabolites are detected in amounts of