Antidiabetic agent - BI-1356
As DPP4 inactivates GLP-1 in vivo, another strategy that has promise in the treatment of Type 2 diabetes is inhibiting the action of this enzyme. Two compounds in this class - sitagliptin and vildagliptin - have already been approved, and several others are under development. These include one compound which, as a xanthine derivative, is structurally different from the gliptins - Boehringer Ingelheim's BI-1356.1
As DPP4 inactivates GLP-1 in vivo, another strategy that has promise in the treatment of Type 2 diabetes is inhibiting the action of this enzyme. Two compounds in this class - sitagliptin and vildagliptin - have already been approved, and several others are under development. These include one compound which, as a xanthine derivative, is structurally different from the gliptins - Boehringer Ingelheim's BI-1356.1
In a Phase I study in healthy volunteers, subjects were given single or multiple oral doses of the drug ranging from 2.5mg to 600mg or placebo. No hypoglycaemia or serious side-effects were seen, and the activity of DPP4 was inhibited by more than 80% in those subjects given doses of at least 5mg. The effect was seen within three hours of dosing, and was still evident after 24 hours with doses of at least 25mg.2
Another trial looked at its effect in patients with Type 2 diabetes. A total of 47 patients were given 1, 2.5, 5 or 10mg orally once a day or placebo for 12 days. Doses of 2.5mg and above gave a dose-dependent inhibition of DPP4 by about 80% 24 hours after the last dose. Levels of GLP-1 were more than doubled.3 Phase III trials are now under way.