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Boehringer Ingelheim Unveils Diabetes Pipeline

- New data presented at ADA demonstrate significant decrease in blood sugar levels with linagliptin added to metformin -

Ridgefield, CT, June 6, 2009 - Boehringer Ingelheim Pharmaceuticals, Inc. today announced its pipeline of oral antidiabetic compounds, establishing itself in the type 2 diabetes therapeutic area.  The Company is investigating compounds in Phase II and Phase III clinical development worldwide.  New Phase II data results for linagliptin (BI 1356), a dipeptidyl peptidase 4 (DPP-4) inhibitor and the Company’s lead diabetes compound, were presented today at the 69th Annual American Diabetes Association (ADA) Scientific Sessions in New Orleans.  

“Type 2 diabetes is a growing public health concern,” said J. Martin Carroll, Boehringer Ingelheim USA Corporation president and CEO. “Our Company will draw from its knowledge and experience to help us deliver on the much needed treatment options for patients who are living with the disease.  Boehringer Ingelheim is inspired to make a difference in diabetes care.” 

Results from the Phase II study presented at ADA show that 1, 5 and 10 mg doses of linagliptin achieved clinically relevant and statistically significant reductions in HbA1c, a measure of blood sugar, when given as add-on therapy to type 2 diabetes patients inadequately controlled on metformin (placebo-corrected changes from baseline; –0.40 percent for the 1 mg dose, –0.73 percent for the 5 mg dose, and –0.67 percent for the 10 mg dose).¹ The most frequently reported adverse events in patients treated with all doses of linagliptin compared to placebo were nasopharyngitis, (7.1 vs. 9.9 percent) diarrhea (2.5 vs. 4.2 percent) and nausea (3.5 vs. 4.2 percent).  No cases of hypoglycemia were reported in patients receiving linagliptin.¹

“Many patients don’t achieve adequate blood sugar control with commonly used diabetes medications like metformin. The significant reduction in HbA1c levels seen in this trial is encouraging as it indicates linagliptin may have a potential role in the management of this prevalent disease," said Dr. Thor Voigt, senior vice president, Medicine and Drug Regulatory Affairs, Boehringer Ingelheim Pharmaceuticals, Inc. “Type 2 diabetes is a progressive chronic condition that frequently requires long-term treatment. A range of treatment options and combination regimens are needed so physicians can tailor therapy to the individual patient needs. We are now awaiting results from additional ongoing studies which will further assess the full potential of linagliptin for the treatment of type 2 diabetes.”

DPP-4 inhibitors are a newer class of oral hypoglycemics that target the incretin hormones GLP-1 and GIP, which are believed to be involved with regulating blood sugar.²

Linagliptin is a compound discovered by Boehringer Ingelheim and is being developed as an oral once-daily tablet for the treatment of type 2 diabetes.  The compound is currently being studied in five pivotal Phase III clinical trials including more than 4,000 patients.  These trials are fully recruited and underway globally and in many states across the U.S. ³

Boehringer Ingelheim is also investigating sodium-dependent glucose co-transporter-2 inhibitors (SGLT-2 inhibitors), which are a new, emerging class of antidiabetic compounds that block tubular reabsorption of glucose in the kidney.⁴ Phase IIb clinical trials for this innovative approach to diabetes treatment are underway.  There are currently no SGLT-2 inhibitors approved by the U.S. Food and Drug Administration (FDA).

About the linagliptin (BI 1356) Phase II study
The aim of the 12-week, international, randomized, double-blind placebo-controlled study was to assess the efficacy and safety profile of linagliptin as add-on therapy in patients with type 2 diabetes who were failing to achieve glycemic control despite being treated with metformin.¹ The primary endpoint was the change in HbA1c from baseline to week 12. ¹ Out of the 333 randomized patients, 268 patients received double-blind treatment with linagliptin (1 mg, n=65; 5 mg, n=66; 10 mg, n=66) or placebo.¹ An open-label arm with 65 patients on glimepiride was added for descriptive control. ¹

Additional results from the study
The addition of linagliptin to metformin treatment for 12 weeks resulted in clinically relevant and statistically significant reductions in HbA1c and fasting blood sugar or fasting plasma glucose (FPG) levels (p-values of less than 0.05%):¹

• Statistically significant reductions in mean HbA1c levels with linagliptin 5 mg and 10 mg compared with metformin alone (both p<0.001) were observed from week four though week 12.¹
• In addition, all linagliptin doses showed significant reductions in FPG levels compared with metformin alone (placebo-corrected mean changes from baseline; –19.2 mg/dL for 1 mg, –34.7 mg/dL for 5 mg, and –29.0 mg/dL for 10 mg).¹
• In the open-label comparator arm, the placebo-corrected mean change from baseline in HbA1c was –0.90 percent.¹
• More than 85% of the patients receiving the 5mg and 10mg doses of linagliptin demonstrated > 80% DPP-4 inhibition at trough at week 12.¹
• HbA1c reductions of at least 0.5 percent were achieved in 44 percent to 53 percent of patients on linagliptin, but only in 13 percent of the patients receiving metformin alone.¹

About type 2 diabetes
There are approximately 23.6⁵ million Americans and 246 million people worldwide⁶ with diabetes.  Type 2 diabetes is the most common type of diabetes accounting for more than 90% of all diabetes cases in the developed world.⁷ Every ten seconds two people develop diabetes and one person dies from diabetes-related causes around the world.⁶ Each year, more than 200,000 people in North America⁶ and more than 3.8 million people worldwide die from diabetes and its complications⁶ - a number which is expected to increase by more than 50 percent over the next decade.⁷ Diabetes is a chronic disease that occurs when the body does not properly produce or use the hormone, insulin.⁶

To address this unmet need, Boehringer Ingelheim is committed to researching and developing new compounds in this therapeutic area.

Boehringer Ingelheim Pharmaceuticals, Inc.
The Boehringer Ingelheim group is one of the world’s 20 leading pharmaceutical companies. Headquartered in Ingelheim, Germany, it operates globally with 138 affiliates in 47 countries and 41,300 employees. Since it was founded in 1885, the independent, family-owned company has been committed to researching, developing, manufacturing and marketing novel products of high therapeutic value for human and veterinary medicine.

In 2008, Boehringer Ingelheim posted net sales of $17 billion (11.6 billion euro) while spending one-fifth of net sales in its largest business segment, Prescription Medicines, on research and development.

For more information, please visit http://us.boehringer-ingelheim.com.

 

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References

1. DPP-4 inhibitor linagliptin improves glycaemic control in type 2 diabetes patients when added to onogoing metformin therapy.  ADA, 05-09 June 2009, New Orleans, U.S.A.
2. Nathan DM et al. Medical Management of Hyperglycemia in Type 2 Diabetes: A Consensus Algorithm for the Initiation and Adjustment of Therapy.  Diabetes Care 21:1-11,  2008.
3. Clinicaltrials.gov. Available at:  http://www.clinicaltrials.gov/ct2/results?term=BI+1356. Accessed on: April 30, 2009.
4. Jabbour SA, et al. Sodium glucose co-transporter 2 inhibitors: blocking renal tubular reabsorption of glucose to improve glycaemic control in patients with diabetes. International Journal of Clinical Practice, July 2008. 62, 8, 1279-1284.
5. American Diabetes Association. 2007 National Diabetes Fact Sheet.
6. International Diabetes Federation. Diabetes Atlas. 3rd edn.  Brussels: International Diabetes Federation, 2006.
7. International Diabetes Federation. Diabetes Atlas. 3rd edn.  Brussels: International Diabetes Federation, 2006.

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