New oncology compound BIBW 2992 demonstrates potential as a next generation
treatment for non-small cell lung cancer and head-and-neck cancer

BURLINGTON, ON, June 3 /CNW/ - Boehringer Ingelheim will present promising new data on non-small cell lung cancer as well as head-and-neck cancer for its leading investigational compound BIBW 2992* at the American Society of Clinical Oncology (ASCO) annual meeting in Chicago, June 4-8, 2010.

New data on BIBW 2992 reaffirms its significant anti-tumour activity in non-small-cell lung cancer (NSCLC) patients with EGFR mutations. The data from the LUX-Lung 2 trial shows that(1):

    
    -   The majority of patients (61 per cent) with common EGFR mutations
        showed tumour shrinkage (measured as partial response) when treated
        with BIBW 2992 as assessed by independent review.
    -   Patients with common mutations taking BIBW 2992 have a long time to
        progression (median of approximately 14 months) and a long survival
        (median of 2 years).
    

"The results seen with BIBW 2992 are promising, and could one day offer patients and doctors a new option to treat non-small cell lung cancer," says Dr. Vera Hirsh, Chair, Lung Cancer Committee, McGill University. "Unlike other treatments in its class, BIBW 2992 works differently by irreversibly binding to EGFR and HER2 receptors and may be effective against tumour growth mechanisms that aren't targeted by first generation, reversible EGFR therapy. BIBW 2992 is part of an exciting new trend in personalized medicine, where treatment is individualized based on each patient's tumour characteristics."

In another study, BIBW 2992 was shown to shrink tumours in 22 per cent of patients with head-and-neck cancer (measured as partial response), compared to 13 per cent of those receiving cetuximab(2).

BIBW 2992 is a next generation small molecule targeting the epidermal growth factor receptor (EGFR/HER1) and human epidermal receptor 2 (HER2) receptor tyrosine kinase.

The LUX-Lung Trial Program

The leading pivotal phase III trial, called LUX-Lung 1, is investigating BIBW 2992 plus best supportive care (BSC) versus placebo plus BSC in NSCLC patients who were previously treated with erlotinib or gefitinib. The results of this trial are expected soon.

LUX-Lung 2 is a Phase II trial evaluating BIBW 2992 in NSCLC patients with EGFR mutations, either treatment naïve or after first line chemotherapy. LUX-Lung 2 is part of the comprehensive LUX-Lung clinical trial program.

In two further ongoing global phase III trials, LUX-Lung 3 and LUX-Lung 6, the efficacy and safety of BIBW 2992 is compared to standard chemotherapy for first-line treatment of NSCLC patients with EGFR mutations in different geographical regions.

Another trial, LUX-Lung 5, is a global phase III trial in patients previously treated with erlotinib or gefitinib. This is the first randomized phase III trial investigating whether patients who initially benefit from treatment with BIBW 2992 alone may further benefit from BIBW 2992 beyond progression when given in combination with chemotherapy.

Currently, this clinical trial programme comprises more than ten trials conducted across the globe.

Additional data being presented at ASCO

Apart from BIBW 2992, Boehringer Ingelheim's late stage oncology portfolio includes BIBF 1120*, also development for the treatment of patients in two different indications, advanced NSCLC and ovarian cancer.

Additional phase I and phase II data will be presented at ASCO for BIBW 2992 in glioma and head and neck cancer and for BIBF 1120 in colorectal cancer. (2),(3),(4)

BIBF 1120 is a novel triple angiokinase inhibitor that acts on three growth factors simultaneously: vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) - all crucially involved in the formation of blood vessels.

Both BIBW 2992 and BIBF 1120 are investigational compounds and are not approved in Canada.

About lung cancer in Canada(5)

According to the Canadian Cancer Society, this year, an estimated 24,200 Canadians will be diagnosed with lung cancer and 20,600 will die of it. On average, 465 Canadians will be diagnosed with lung cancer every week and on average, 395 Canadians will die. Lung cancer remains the leading cause of cancer death for both men and women in Canada.

About Head and Neck Cancer

Head and neck cancer can occur in over 30 different places in any of the tissues or organs in the head and neck(6), including in and around the mouth, and it is the sixth most frequently occurring cancer worldwide(7). Most head and neck cancers are squamous cell carcinomas(8), over 90 per cent of which express EGFR(9), which is critical for tumour growth(10). In Canada, 3,400 people will be diagnosed with oral cancer this year alone and 1,150 will die as a result11. Furthermore, 1,150 Canadians will be diagnosed with cancer of the larynx, and 500 will die of the disease(11).

About Boehringer Ingelheim in Oncology

Building on scientific expertise and excellence in the fields of pulmonary and cardiovascular medicine, metabolic disease, neurology, virology and immunology, Boehringer Ingelheim has embarked on a major research program to develop innovative cancer drugs. Working in close collaboration with the international scientific community and a number of the world's leading cancer centres, Boehringer Ingelheim is committed to discovering and developing novel cancer treatments. This commitment is underpinned by using advances in science to develop a range of targeted therapies in areas of medical need, including various solid tumours and haematological cancers.

The current focus of research includes compounds in three areas: angiogenesis inhibition, signal transduction inhibition and cell-cycle kinase inhibition. BIBW 2992 is currently in phase III clinical development in NSCLC, and was granted Fast Track designation for a third/fourth line treatment indication in NSCLC by the US Food & Drug Administration. In addition, the LUME-Lung phase III clinical trial program, which is investigating BIBF 1120 in combination with standard second-line chemotherapy treatments for patients with advanced NSCLC, is ongoing. In the area of cell-cycle kinase inhibition, Boehringer Ingelheim is developing inhibitors of polo-like kinase 1 (Plk-1), a protein that is involved in the processes of cell division. These molecules are in the earlier stages of clinical development.

About Boehringer Ingelheim (Canada) Ltd.

The Boehringer Ingelheim group is one of the world's 15 leading pharmaceutical companies. Headquartered in Ingelheim, Germany, it operates globally with 142 affiliates in 50 countries and 41,500 employees.

Founded in 1885, the family-owned company is committed to researching and developing 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 one fifth of net sales in its largest business segment Prescription Medicines on research and development.

The Canadian headquarters of Boehringer Ingelheim was established in 1972 and the Research and Development Centre located in Laval, Québec, Canada since 1988. Boehringer Ingelheim (Canada) Ltd. is home to more than 700 employees including 160 scientists across the country.

* BIBW 2992 and BIBF 1120 are investigational compounds; their safety and efficacy have not yet been fully established. Market Authorization has not been obtained in Canada

For more information please visit www.boehringer-ingelheim.ca.

    
    References

    1.   Chih-Hsin Yang et al. A Phase II study of BIBW 2992 in patients with
         adenocarcinoma of the lunch and activating EGFR mutations (LUX-Lung
         2). Poster presentation at The American Society of Clinical Oncology
         (ASCO) annual meeting, Chicago. June 2010.
         MacMillan Cancer Support.
    2.   Tanguy Y. Seiwert et al. BIBW 2992 versus cetuximab in patients with
         metastatic or recurrent head and neck cancer (SCCHN) after failure
         of platinum-containing therapy with a cross-over period for
         progressing patients: Preliminary results of a randomized, open-
         label Phase II study. Oral presentation at The American Society of
         Clinical Oncology (ASCO) annual meeting, Chicago. June 2010.
    3.   Reardon, A. David et al. Phase I/II study of BIBW 2992 with or
         without daily temozolomide in the treatment of patients with
         recurrent malignant glioma. General poster presentation at The
         American Society of Clinical Oncology (ASCIO) annual meeting,
         Chicago. June 2010.
    4.   Prenen, H et al. A phase I dose escalation study of BIBF 1120
         combined with FOLFOX in metastic colorectal cancer (mCRC) patients
         (pts). Accepted for publication.
    5.   Canadian Cancer Society. Lung Cancer Statistics.
http://www.cancer.ca/Ontario/About%20cancer/Cancer%20statistics/Stats%20at%20a%20glance/Lung%20cancer.aspx?sc_lang=en&r=1
(Accessed May 21, 2010)
    6.   MacMillan Cancer Support.
http://www.macmillan.org.uk/Cancerinformation/Cancertypes/Headneck/Aboutheadneckcancers/Headneckcancers.aspx.
Last accessed 7 May 2010
    7.   Hunter KD et al. Profiling early head and neck cancer. Nat Rev
         Cancer. 2005 Feb; 5 (2): 127-35
    8.   Viviana P. Lutzky. Biomarkers for Cancers of the Head and Neck.
         Clinical Medicine: Ear, Nose and Throat 2008:1
    9.   Grandis, J.R. and Tweardy, D.J. Elevated levels of transforming
         growth factor alpha and epidermal growth factor receptor messenger
         RNA are early markers of carcinogenesis in head and neck cancer.
         Cancer Res., 1993. 53:3579-84.
    10.  Normanno N et al. The ErbB receptors and their ligands in cancer: an
         overview. Current Drug Targets.2005. May;6(3):243-47.
    11.  Canadian Cancer Society Steering Committee: Canadian Cancer
         Statistics 2010. Toronto: Canadian Cancer Society, 2010.

    *  BIBW 2992 and BIBF 1120 are investigational compounds; their safety
         and efficacy have not yet been fully established. Market
         Authorization has not been obtained in Canada.
    *  BIBW 2992 is an investigational compound; its safety and efficacy
         has not yet been fully established. Market Authorization has not
         been obtained in Canada.
    

For further information: Jeanelle Frampton, Environics Communications, [phone], [email protected]