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New phase III data demonstrate clinically meaningful improvements in blood glucose control with linagliptin mono- and combination therapy
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Ingelheim/Germany, 26 June 2010 - Linagliptin phase III data were presented for the first time this week at the 70th Scientific Sessions of the American Diabetes Association (ADA), showing that this investigational compound, a dipeptidyl peptidase (DPP)-4 inhibitor, achieved significant, sustained and clinically meaningful reductions in blood glucose as measured by haemoglobin A1c (HbA1c), fasting plasma glucose (FPG), and postprandial glucose (PPG) concentrations.1-6 Linagliptin is being investigated by Boehringer Ingelheim as a once-daily oral treatment in type 2 diabetes.
In the pivotal phase III studies, linagliptin was shown to have a very favourable safety profile, with an overall rate of adverse events similar to placebo. In addition, linagliptin showed an excellent tolerability, was weight neutral, showed no increased risk of drug-drug interactions and, importantly, there was no increased risk of hypoglycaemia attributed to linagliptin use in monotherapy, or combination therapy with metformin or pioglitazone.1-6
Notably, in diabetes patients with mild and moderate renal impairment, linagliptin blood plasma levels were comparable to those seen in diabetes patients with normal renal function,1 suggesting that linagliptin, which has a primarily non-renal route of excretion, may have distinct pharmacological features not yet seen in this novel class of drugs.8 The data suggest that linagliptin would not need dose adjustment in patients with type 2 diabetes regardless of the stage of renal impairment.
In four multi-centre, 24 weeks, randomised, double-blind, controlled trials, statistically significant reductions in blood glucose were observed with linagliptin monotherapy versus placebo1 and when used in combination with other commonly used oral anti-diabetes drugs.2-4 This was accompanied by significant improvements in beta-cell function.1,3 Declining beta-cell function is a key factor driving the progression of type 2 diabetes.7
In a further study, linagliptin monotherapy showed superiority in glucose lowering versus placebo and versus voglibose, the most commonly used alpha glucosidase inhibitor in Japan.5-6
“Many type 2 diabetes patients treated with traditional anti-diabetes agents fail to achieve their glycaemic targets or maintain them over time, which can leave them at a higher likelihood of developing diabetic complications, including renal disease. Although renal impairment is very common in patients with type 2 diabetes, early stage renal dysfunction often goes undiagnosed. It is important to identify those patients as they will require effective and safer drugs with low risk of hypoglycaemia”, commented Julio Rosenstock, M.D., Director of Dallas Diabetes and Endocrine Center at Medical City and also a Clinical Professor of Medicine, University of Texas Southwestern Medical School, Dallas, Texas, USA. “For linagliptin, we see from studies that only approximately five percent of the orally administered drug is excreted via the kidneys. Data to date appear to indicate that linagliptin would not require dose adjustment, which could translate into an important benefit for physicians when choosing a treatment, not only for the type 2 diabetes patient population with diagnosed renal impairment, but also for those patients at risk of developing renal complications”, he added.
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About Diabetes and Type 2 Diabetes
There are approximately 285 million people with diabetes in the adult population worldwide.9 The International Diabetes Federation estimates that the number of people with diabetes will increase to 438 million people worldwide by 2030. Nearly four million people within the 20-79 age group are predicted to die from diabetes and its complications in 2010.9 Approximately 50% of people with diabetes die of cardiovascular disease,9 and more than 8% die of renal causes.10
For more information about type 2 diabetes, please also visit:
Boehringer Ingelheim Diabetes Pipeline
Metabolism is one of Boehringer Ingelheim’s core R&D areas and diabetes one of the indications at the centre of interest within the company’s global research network. Boehringer Ingelheim is committed to researching and developing new diabetes compounds with novel modes of action to improve patients’ health and increase overall quality of life. These include:
Linagliptin phase III pivotal trials description:1-6
Four multi-centre, randomised, placebo-controlled, double-blind, phase III studies were conducted to investigate the efficacy, safety and tolerability of linagliptin (5 mg once daily) versus placebo, administered over 24 weeks in type 2 diabetes mellitus patients with insufficient glycaemic control. The overall HbA1c range for these studies was ≥6.5% and ≤11%, with the following background therapy: linagliptin monotherapy1 (exercise and diet alone), as add-on to metformin2, as add-on to metformin plus a sulfonylurea3, and as initial combination with pioglitazone.4 A multi-centre, 12 and 26 weeks, randomised, double-blind, controlled study comparing the efficacy and safety and tolerability of linagliptin versus placebo and the alpha glucosidase inhibitor voglibose in drug-naïve or previously treated Japanese patients with type 2 diabetes (baseline HbA1c 7 -10% if drug-naïve, 7.0-9.0% if previously treated with an oral hypoglycaemic agent).5-6
Summary of key efficacy results from these trials:
About Boehringer Ingelheim
The Boehringer Ingelheim group is one of the world’s 20 leading pharmaceutical companies. Headquartered in Ingelheim, Germany, it operates globally with 142 affiliates in 50 countries and more than 41,500 employees. Since it was founded in 1885, the family-owned company has been committed to researching, developing, manufacturing and marketing novel products of high therapeutic value for human and veterinary medicine.
In 2009, Boehringer Ingelheim posted net sales of 12.7 billion euro while spending 21% of net sales in its largest business segment Prescription Medicines on research and development.
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1Owens D.R. et al. Linagliptin improves glycemic control in Type 2 diabetes patients inadequately controlled by metformin and sulfonylurea without weight gain and low risk of hypoglycaemia. Poster No 548-P from the 70th American Diabetes Association Scientific Sessions, 25-29 June 2010, Orlando, Florida, U.S.A.
2Taskinen M.R. et al. Efficacy and safety of linagliptin in Type 2 diabetes inadequately controlled on metformin monotherapy. Poster No 579-P from the 70th American Diabetes Association Scientific Sessions, 25-29 June 2010, Orlando, Florida, U.S.A.
3Del Prato S, et al. Linagliptin monotherapy improves glycaemic control and measures of beta-cell function in Type 2 diabetes. Poster No 695-P from the 70th American Diabetes Association Scientific Sessions, 25-29 June 2010, Orlando, Florida, U.S.A.
4Gomis R. et al. Efficacy and safety of initial combination therapy with linagliptin and pioglitazone in patients with inadequately controlled Type 2 diabetes. Poster No 551-P from the 70th American Diabetes Association Scientific Sessions, 25-29 June 2010, Orlando, Florida, U.S.A.
5Kawamori R. et al. Linagliptin Provides Superior Glycemic Control Compared to Voglibose as Monotherapy in Japanese Patients with Type 2 Diabetes. Poster No 632-P from the 70th American Diabetes Association Scientific Sessions, 25-29 June 2010, Orlando, Florida, U.S.A.
6Kawamori R. et al. Linagliptin Monotherapy Improves Glycemic Control in Japanese Patients with T2DM over 12 Weeks. Poster number 696-P from the 70th American Diabetes Association Scientific Sessions, 25-29 June 2010, Orlando, Florida, U.S.A.
7Kahn S. The Importance of ß-Cell Failure in the Development and Progression of Type 2 Diabetes. The Journal of Clinical Endocrinology & Metabolism. 2001;86(9):4047-4058.
8Blech S. et al. The Metabolism and Disposition of the Oral Dipeptidyl Peptidase-4 Inhibitor, Linagliptin, in Humans. Drug Metabolism and Disposition: 2010;38:667–678.
9International Diabetes Federation. Available at www.idf.org accessed on: 1 March 2010.
10Morrish, N.J. et al. Mortality and causes of death in the WHO Multinational Study of Vascular Disease in Diabetes. Diabetologia.2001;44 Suppl 2: S14-S21.