Tradjenta is a DPP -4 inhibitor developed by Boehringer Ingelheim for the treatment of type II diabetes . Two pharmacological characteristics that sets tradjenta apart from other DPP -4 inhibitors is that it has a non-linear pharmacokinetic profile and is not primarily eliminated by the renal system. FDA approved on May 2, 2011.
Tradjenta is a more potent inhibitor of DPP-4 than other drugs that belong to the same class with an IC50 of 1 nM. In comparison, sitagliptin, saxagliptin, and vildagliptin have an IC50 of 19, 50, and 62 nM respectively. A dose of 2.5 and 5 mg reduces the activity of DPP-4 by 72.7% and 86.1% from baseline respectively in healthy male subjects. In diabetes patients, a dose of 5 and 10 mg inhibits >90% of DPP-4. Tradjenta is also selectively inhibits DPP-4 as indicated by the lack of DPP-8 or DPP-9 inhibition at therapeutic exposures in vitro.