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New data from the linagliptin late stage clinical trial programme were presented this week at the 46th Annual Meeting of the European Association for the Study of Diabetes (EASD). The studies included two phase III trials: one investigating linagliptin monotherapy in type 2 diabetes patients for whom metformin therapy is inappropriate and the other studying linagliptin as add-on therapy to a sulphonylurea in patients with inadequately controlled type 2 diabetes. In addition, a pharmacokinetic study was presented at the congress which investigated linagliptin in a special patient population with different degrees of renal impairment.
Linagliptin belongs to the novel class of DPP-4 inhibitors and is currently in late stage development as a once-daily, single-dose oral tablet. The new data add to the large body of clinical evidence demonstrating that linagliptin cannot only achieve significant and sustainable reductions in blood glucose, but that based on its unique pharmacokinetic profile, linagliptin may not require dose adjustment even in patients with type 2 diabetes with any degree of renal impairment. Boehringer Ingelheim is filing linagliptin for market authorisation in key countries across the globe in 2010 and is looking forward to making this novel treatment available to people with type 2 diabetes as soon as possible.
Linagliptin’s profile goes beyond the established favourable characteristics of this novel class of anti-diabetic treatments
One of the unique characteristics of linagliptin among the DPP-4 inhibitors is its primarily non-renal route of excretion. The pharmacokinetic study3 was performed to support the assumption that linagliptin exposure would not show a clinically relevant increase when administered in patients with any degree of renal impairment. Notably, results from this study confirmed that decreases in renal function had only little effect on the elimination of linagliptin and only minor changes were observed in linagliptin exposure in patients with renal impairment (1.4-fold increase in exposure in type 2 diabetes patients with severe renal impairment compared with type 2 diabetes patients with normal renal function). This, along with the large safety window of linagliptin, supports the assumption that no dose adjustment of linagliptin may be required in type 2 diabetes patients with any degree of renal impairment.
“Treating type 2 diabetes demands a holistic approach if we want to be successful in helping patients not only achieve but also maintain good blood glucose levels. Kidney function is an important consideration when prescribing an anti-diabetes therapy. Many type 2 diabetes patients either have, or are at significant risk of developing kidney impairment,” said Professor Anthony Barnett, Professor of Medicine and Clinical Director of the Department of Diabetes and Endocrinology, Heart of England NHS Foundation Trust, Birmingham, UK. “Currently available DPP-4 inhibitors are mainly eliminated via the kidney and therefore not recommended in patients with advanced renal impairment in many countries. Others either require dose adjustment or are contraindicated for such patients. The clinical data for linagliptin seen to date suggest an advantage in this respect due to its primarily non-renal route of excretion. The convenience of a drug not needing additional monitoring of kidney function or not needing dose adjustment as kidney function declines, could improve patient compliance as well as making life easier for the health professional.”