Boehringer Ingelheim accesses field of oncology with three compounds in phase II – Company presents promising pipeline

08 November 2006 - Ingelheim/Germany and Vienna/Austria, 8 November 2006 - Oncology is new among Boehringer Ingelheim’s indication areas Respiratory, Cardiovascular Diseases, Virology, Central Nervous System, Immunology and Metabolic Diseases. As presented at the company’s international R&D press conference today, three anti-cancer drug candidates are now in advanced stages of development i.e. in clinical phase II.

“Based on promising data from our studies, we are confident that the innovative features of our molecules, once confirmed in Phase III trials, will allow physicians to offer improved treatments choices to cancer patients”, said Dr. Andreas Barner, Vice Chairman of the Board of Managing Directors and responsible for the Corporate Board Division Pharmaceutical Research, Development and Medicine at Boehringer Ingelheim, “We are one step closer to tomorrow’s cancer therapies”.

* BIBF 1120 limits the supply of oxygen and nutrients to cancer cells by inhibiting the development of blood vessels to the tumor (tumor angiogenesis), which inhibits tumor growth and when administered with other cancer therapies the tumor eventually dies. Moving beyond the first generation of anti-angiogenic agents, the triple angiokinase inhibitor BIBF 1120 targets VEGF, FGF, and PDGF* receptors in several cell types required for establishing and maintaining tumor blood vessels, aiming at more durable clinical benefit combined with good tolerability and safety.1,2,3
* BIBW 2992 is a novel kinase inhibitor which effectively blocks the activity of the Epidermal Growth Factor Receptor (EGFR) and the related Human Epidermal growth factor Receptor (Her 2). Aberrant signalling of this family of receptors (erbB family) is involved in a variety of cancer types. Thus, compared with first generation drugs, the dual inhibitor BIBW 2992 broadens the reach in terms of efficacy and potential indications. Due to its irreversible binding, BIBW 2992 holds promise for activity against receptors resistant to first generation inhibitors.4,5
* BI 2536 is a novel inhibitor of Polo-like kinase 1 (Plk-1), a cell cycle switch essential for cell proliferation. BI 2536 inhibits cell division (mitosis), resulting in cancer cell death by apoptosis. As the first Plk-1 inhibitor being tested in clinical trials, BI 2536 shows efficacy in a broad spectrum of cancers combined with better tolerability than conventional chemotherapeutic agents.6,7,8,9

Current target indications include: Non-Small Cell Lung Cancer, Breast Cancer, Colorectal Cancer, Prostate Cancer, Ovarian Cancer, Leukaemia and Lymphomas.

“While we have made good progress in the treatment of cancer, it remains a significant global health issue” commented Dr. Wolfgang Rettig, Head of Research at Boehringer Ingelheim Austria. “In 2005, over 7.6 million people died of cancer and this figure is projected to continue rising. Boehringer Ingelheim is committed to being at the forefront of this research with the aim to provide high therapeutic value to patients.”

Further compounds under development at Boehringer Ingelheim are most advanced and have now reached clinical phase III:

* Dabigatran etexilate, an oral direct thrombin inhibitor, is the frontrunner of all new oral anticoagulants currently being developed. Dabigatran is investigated in the prevention and treatment of thromboembolic diseases including the long term prevention of thromboembolic events (stroke) in patients with atrial fibrillation and primary prevention of deep vein thrombosis after hip or total knee replacement.10,11
* Flibanserin is being developed as potential treatment for women with decreased sexual desire. This condition - also known as Hypoactive Sexual Desire Disorder (HSDD) - is characterized by diminished feelings of sexual interest or desire, causing personal distress or interpersonal difficulties. Epidemiological studies suggest that up to one in five women suffer from decreased sexual desire.12 Currently, there is no approved pharmacological treatment available.

“We are delighted to see that our investments into R&D have resulted into an increased number of phase I - II projects in the last couple of years and we can expect a growing range of promising pipeline compounds for indications such as Diabetes, COPD, inflammatory/ autoimmune diseases, Cancer, HIV and Hepatitis” added Dr. Manfred Haehl, Corporate Senior Vice President Medicine at Boehringer Ingelheim.

The company’s R&D strategy includes the covering of seven indication areas at four major R&D competence centers in Vienna, Austria (for Oncology), in Biberach, Germany (for Metabolism, CNS, Respiratory), in Ridgefield, Connecticut, USA (for Cardiovascular, Immunology/ Inflammation) and in Laval, Canada (for Virology), supported by two more specialised sites in Italy and Japan.

“We have organised our therapeutic area expertise in focused competence centers where specialists conduct research into small and large molecules. They use a shared drug discovery process and are supported by global technology centers. In the last few years we have significantly enhanced our output of innovative drug candidates, with an emphasis on clear medically differentiated drug profiles” said Dr. Mikael Dolsten, Executive Vice President Pharma Research at Boehringer Ingelheim.

After a substantial increase in headcount in the last five years Boehringer Ingelheim now has about 5,700 employees in Research & Development and Medicine worldwide who ensure a continuous flow of new compounds to come into pre-development and development.

Boehringer Ingelheim’s research strategy also allows to in-license compounds from early as well as from later development phases.

Dr. Haehl explained that across big pharma, from more than one million screened molecules, only one will eventually enter the market as an approved medication. Drug discovery, pre-clinical and clinical development need 10 years of time and including failures an investment of in average 800 million Dollars. Every year, the company invests about a fifth of its net sales in Prescription Medicines into research and development; in 2005 this was about 1,4 billion euro.

Boehringer Ingelheim conducts several clinical “Megatrials” with very large numbers of patients involved. In the last ten years, Boehringer Ingelheim has included 1.2 million patients in 1,400 clinical trials for 140 substances.

The company’s expertise becomes manifest in e.g. the cardiovascular outcome trial ONTARGET/ TRANSCEND with nearly 32,000 patients. ONTARGET investigates multiple aspects of cardiovascular morbidity and mortality focusing on Micardis® (telmisartan), a once daily angiotensin II receptor blocker. PRoFESS with 20,000 patients investigates the potential of Aggrenox®/ Asasantin® to prevent secondary strokes. The UPLIFT study with 6,000 patients investigates the potential of Spiriva® to reduce and slow down the long term decline in lung function which is the most devastating clinical consequence of COPD. With over 27,000 patients REVOLUTION is the largest clinical trial programme in thromboembolic disease investigating dabigatran.

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 143 affiliates in 47 countries and almost 37,500 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 2005, Boehringer Ingelheim posted net sales of 9.5 billion euro while spending almost one fifth of net sales in its largest business segment Prescription Medicines on research and development.

Boehringer Ingelheim ranks high among top employers
A most recent publication in “Science” has ranked Boehringer Ingelheim second among all top employers in the global biotechnology and pharmaceutical industries.13

* VEGF = Vascular endothelial growth factor, FGF= Fibroblast growth factor, PDGF= Platelet derived growth factor

References:
1 Hicklin DJ, Ellis LM.JClin Oncol. 2005;23:1011-1027
2 Presta M, Dell’Era P, Mitola S, et al. Cytokine Growth Factor Rev., 2005; 16: 159-178
3 Yu J, Ustach C, Kim R-HC. J Biochem Mol Biol. 2003; 36:49-59
4 Casalini P, Iorio MV, Galmozzi E, Menard S. J Cell Physiol. 2004 200:343-350
5 Normanno N, Bianco C, Strizzi L, et al. Curr Drug Targets 2005;6: 243-257
6 Barr FA, Sillje HH, Nigg EA Nat Rev Mol Cell Biol. 2004;5:429-440
7 Eckerdt F, Yuan J, Strebhardt K. Oncogene. 2005;24:267-276
8 Liu X, Erikson RL. Proc Natl Acad Sci USA. 2003; 100:5789-5794
9 Takai N, Hamanaka R, Yoshimatsu J, Miyakawa I. Oncogene.2005;24:287-291
10 Kakkar VV, De Lorenzo F. Prevention, diagnosis and management of venous thromboembolic disease. Eds. Pineo GF, Hull RD. Baillière’s Clinical Haematology 1998;11:605-619
11 Blanchard J, Meuwly J-Y, Leyvraz P-F et al. J Bone Joint Surg (Br) 1999; 81-B:654-659
12 Laumann EO et al, J American Med Assoc.1999;281:537-544
13 American Assoc fort he Advancement of Science Sciencecareers.sciencemag.org/career_development/previous_issues/articles/2006/Top Employers Survey

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Julia Meyer-Kleinmann

Boehringer Ingelheim GmbH

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