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Drugs Fut 2008, 33(6): 473
ISSN 0377-8282
Copyright 2008 Clarivate Analytics
CCC: 0377-8282
DOI: 10.1358/dof.2008.033.06.1215244
Wang, Y., Serradell, N., Rosa, E., Castaner, R.
BI-1356 is a dipeptidyl-peptidase IV (DPP IV, or CD26) inhibitor developed at Boehringer Ingelheim for the treatment of type 2 diabetes. BI-1356 demonstrated long-lasting DPP IV inhibition both in vitro and in vivo. In vitro, BI-1356 was at least 10,000-fold more selective for DPP IV than for DPP-8 and DPP-9. High potency and long-lasting inhibitory effects were also observed in vivo in mice and rats, the inhibition induced by BI-1356 being longer lasting than that induced by any other DPP IV inhibitor tested. BI-1356 exhibited nonlinear pharmacokinetics in healthy volunteers and patients with type 2 diabetes. Oral BI-1356 administered once daily proved to be well tolerated in healthy volunteers and patients with type 2 diabetes. Treatment with BI-1356 increased concentrations of GLP-1 and reduced concentrations of glucose in patients with type 2 diabetes, and it also significantly reduced Hb1Ac in diabetic patients. Phase III clinical trials are under way.

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