90-week data suggest sustained glucose reduction and weight loss with investigational SGLT-2 inhibitor, empagliflozin

RIDGEFIELD, Conn. and INDIANAPOLIS, June 9, 2012 /PRNewswire/-- Boehringer Ingelheim Pharmaceuticals, Inc. and Eli Lilly and Company (NYSE: LLY) presented results that showed empagliflozin (BI 10773), alone or as an add-on to metformin, reduced hemoglobin A1c (HbA1c or A1C) levels, fasting plasma glucose (FPG) levels and body weight when given to adults with type 2 diabetes for up to 90 weeks.[1] A1C is measured in people with diabetes to provide an index of blood glucose control for the previous two to three months. The new data, from a phase 2b open-label extension study, were presented during a late-breaking session at the American Diabetes Association's (ADA's) 72nd Scientific Sessions®.

Empagliflozin inhibits SGLT-2, which blocks glucose reuptake in the kidney, thereby removing excess glucose through the urine.

"These new findings provide additional information about the use of empagliflozin in type 2 diabetes, and support the phase 3 trials that are underway to confirm the drug's efficacy and safety profile," said John Smith, M.D., Ph.D., senior vice president for clinical development and medical affairs, Boehringer Ingelheim Pharmaceuticals, Inc.

In the open-label study, adults with type 2 diabetes (n=659) who participated in one of two 12-week, blinded, dose-finding empagliflozin trials, were treated for an additional 78 weeks with open-label empagliflozin 10 mg or 25 mg (monotherapy or add-on to metformin), metformin alone, or sitagliptin as add-on to metformin.

At week 90, decreases in average A1C levels (percent), FPG levels (mg/dL), and body weight (kg, weight) were observed with empagliflozin 10 mg alone (-0.34; -30.4; -2.24, respectively) and 25 mg alone (-0.47; -27.8; -2.61, respectively), versus metformin (-0.56; -26.0; -1.28, respectively).[1] When used as an add-on to metformin, empagliflozin showed reductions versus sitagliptin on A1C levels (-0.34 EMPA 10 mg; -0.63 EMPA 25 mg; and -0.40 sitagliptin); FPG levels (-21.3 EMPA 10 mg; -31.8 EMPA 25 mg; and -15.6 sitagliptin); and body weight (-3.14 EMPA 10 mg; -4.03 EMPA 25 mg; and -0.41 sitagliptin).[1]

"The alliance is leveraging the collective scientific expertise of two leading research-driven pharmaceutical companies to address patient needs arising from the growing global diabetes epidemic," said Professor Klaus Dugi, Corporate Senior Vice President Medicine, Boehringer Ingelheim GmbH. "We are committed to developing medications to help patients with diabetes throughout the course of their condition."

The study showed empagliflozin (10 mg or 25 mg) was generally well-tolerated.  When given for a treatment duration of at least 78 weeks and for up to 90 weeks, adverse events (AEs) were reported in 63.2 to 74.1 percent of patients on empagliflozin and in 69.6 percent of patients on metformin alone or sitagliptin plus metformin.[1] More than 90 percent of these AEs were of mild or moderate severity. Between 0.9 and 3.6 percent of patients on empagliflozin reported hypoglycemic events, versus 7.1 percent on metformin only and 5.4 percent on sitagliptin. AEs related to urinary tract infections were reported in 3.8 to 12.7 percent of patients on empagliflozin, 3.6 percent of patients on metformin only, and 12.5 percent of patients on sitagliptin. AEs related to genital infections were reported in 3.0 to 5.5 percent of patients on empagliflozin, 1.8 percent of patients on metformin only, and none of the patients on sitagliptin.[1]

Empagliflozin is currently in phase 3 clinical development with over 14,500 patients planned to be enrolled. [6]

Safety and Efficacy of Empagliflozin as Monotherapy or Add-On to Metformin in a 78-Week Open-Label Extension Study in Patients With Type 2 Diabetes

In this extension study, patients treated with 10 mg or 25 mg of empagliflozin (monotherapy or add-on to metformin), metformin alone, or sitagliptin as add-on to metformin in one of two 12-week trials continued on the same treatment for an additional 78 weeks. Patients in the 12-week trial who had received 1, 5 or 50 mg of empagliflozin or placebo were randomized to 78 weeks of treatment with either 10 mg or 25 mg of empagliflozin (monotherapy [106 on 10 mg; 109 on 25 mg] or add-on to metformin [166 on 10 mg and 166 on 25 mg]), metformin only (56) or sitagliptin (56). Results for empagliflozin monotherapy were compared with those of patients treated with metformin alone, while data among patients on empagliflozin plus metformin were compared with those of patients on sitagliptin plus metformin.  

About Diabetes

Approximately 25.8 million Americans[3] and an estimated 366 million people worldwide[4] have type 1 or type 2 diabetes. Type 2 diabetes is the most common type, accounting for an estimated 90 to 95 percent of all diabetes cases.[3] Diabetes is a chronic disease that occurs when the body either does not properly produce, or use, the hormone insulin.[5]

Boehringer Ingelheim and Eli Lilly and Company

In January 2011, Boehringer Ingelheim and Eli Lilly and Company announced an alliance in the field of diabetes that centers on four pipeline compounds representing several of the largest treatment classes. This alliance leverages the companies' strengths as two of the world's leading pharmaceutical companies, combining Boehringer Ingelheim's solid track record of research-driven innovation and Lilly's innovative research, experience, and pioneering history in diabetes. By joining forces, the companies demonstrate commitment in the care of patients with diabetes and stand together to focus on patient needs. Find out more about the alliance at www.boehringer-ingelheim.com or www.lilly.com.

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 145 affiliates and more than 44,000 employees. Since it was founded in 1885, the family-owned company has been committed to researching, developing, manufacturing and marketing novel medications of high therapeutic value for human and veterinary medicine.

As a central element of its culture, Boehringer Ingelheim pledges to act socially responsible. Involvement in social projects, caring for employees and their families, and providing equal opportunities for all employees form the foundation of the global operations. Mutual cooperation and respect, as well as environmental protection and sustainability are intrinsic factors in all of Boehringer Ingelheim's endeavors.

In 2011, Boehringer Ingelheim achieved net sales of about $17.1 billion (13.2 billion euro). R&D expenditure in the business area Prescription Medicines corresponds to 23.5% of its net sales.

For more information, please visit http://us.boehringer-ingelheim.com and follow us on Twitter at http://twitter.com/boehringerus.

About Eli Lilly and Company

Lilly, a leading innovation-driven corporation, is developing a growing portfolio of pharmaceutical products by applying the latest research from its own worldwide laboratories and from collaborations with eminent scientific organizations. Headquartered in Indianapolis, IN, Lilly provides answers – through medicines and information – for some of the world's most urgent medical needs. Additional information about Lilly is available at www.lilly.com.

About Lilly Diabetes

Lilly has been a global leader in diabetes care since 1923, when we introduced the world's first commercial insulin. Today we work to meet the diverse needs of people with diabetes through research and collaboration, a broad and growing product portfolio and a continued commitment to providing real solutions–-from medicines to support programs and more–-to make lives better.

For more information, visit www.lillydiabetes.com.

This press release contains forward-looking statements about empagliflozin for the treatment of type 2 diabetes. It reflects Lilly's current beliefs; however, as with any such undertaking, there are substantial risks and uncertainties in the process of drug development and commercialization. There is no guarantee that future study results and patient experience will be consistent with study findings to date or that empagliflozin will be commercially successful. For further discussion of these and other risks and uncertainties, please see Lilly's latest Forms 10-Q and 10-K filed with the U.S. Securities and Exchange Commission. Lilly undertakes no duty to update forward-looking statements.

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[1] Woerle HJ, Ferrannini E, Berk A, et al. Safety and Efficacy of Empagliflozin as Monotherapy or Add-On to Metformin in a 78-Week Open-Label Extension Study in Patients With Type 2 Diabetes. Abstract #49-LB. Presented at the American Diabetes Association's (ADA's) 72^nd Scientific Sessions^®. June 8-12, Philadelphia, PA.

[2] Rolf G, et al. In Vitro Properties and In Vivo Effect on Urinary Glucose Excretion of BI 10773, a Novel Selective SGLT2 Inhibitor. Abstract #521-P. Presented at the American Diabetes Association's (ADA's) 69^th Scientific Sessions^®. June 5-9, New Orleans, LA.

[3] Centers for Disease Control and Prevention. National Diabetes Fact Sheet: National Estimates and General Information on Diabetes and Prediabetes in the United States, 2011. Atlanta, GA: U.S. Department of Health and Human Services, Centers for Disease Control and Prevention, 2011.

[4] International Diabetes Federation. Diabetes Atlas, 5th Edition: Fact Sheet. 2011.

[5] International Diabetes Federation. IDF Diabetes Atlas, 5th Edition: What is Diabetes? http://www.idf.org/diabetesatlas/5e/what-is-diabetes. Accessed on: April 11, 2012.

[6] Data on File.

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SOURCE Eli Lilly and Company; Boehringer Ingelheim Pharmaceuticals, Inc.