13/10 Boehringer Ingelheim's lead investigational oncology compound BIBW 2992 demonstrates potential as a next generation treatment for non-small cell lung cancer and head-and-neck cancer

21 mai 2010

Further new data on BIBW 2992* suggests it is at least as effective as cetuximab in head-and-neck cancer, and reaffirms activity in non-small-cell lung cancer with EGFR mutations)

Boehringer Ingelheim will present promising new data at the American Society of Clinical Oncology (ASCO) annual meeting in Chicago, 4-8 June 2010, for its leading investigational compound BIBW 2992. New data from a recent study that was accepted by ASCO for presentation showed that BIBW 2992 shrank tumours in 22% of patients with head and neck cancer (measured as partial response), compared to 13% of those receiving cetuximab 1.

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 compound works distinctively by irreversibly binding to the receptor 2 - unlike available treatments in this class.

"The results for BIBW-2992 are potentially quite meaningful for patients diagnosed with Head and Neck Cancer since the data support that this novel, irreversible EGFR/erbB2 compound appears to be at least as effective as cetuximab with a comparable safety profile." says Tanguy Y. Seiwert, MD, lead investigator of the trial, University of Chicago Medical Center "Recurrent Head and Neck Cancer carries a very poor prognosis, and this is truly the first time that an oral EGFR targeting agent has shown this level of activity in Head and Neck Cancer. At this advanced stage patients with Head and Neck Cancer have few treatment options, and BIBW 2992 could potentially provide a much needed alternative treatment option."

Furthermore, new data on BIBW 2992 that will be presented at ASCO 2010 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 3:

• The majority of patients (61%) with common EGFR mutations (deletion 19 and L858R) have significant 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).

Professor James CH Yang, National Taiwan University Hospital and investigator of the LUX-Lung 2 clinical trial comments: "These results are exciting, as they affirm BIBW 2992's marked and durable anti-tumour activity in NSCLC patients with EGFR mutations."

LUX-Lung 2 is part of the comprehensive LUX-Lung clinical trial programme.
Currently, this clinical trial programme comprises more than ten trials conducted across the globe.

The LUX-Lung Trial Programme

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.

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 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.

Additionally Boehringer Ingelheim has recently commenced a phase III clinical trial evaluating BIBW 2992 in advanced breast cancer (LUX-breast 1).

BIBW 2992 & BIBF 1120*: the two front-runner molecules within Boehringer Ingelheim's investigational oncology portfolio

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

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.

Notes to editors

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 4 and is the sixth most frequently occurring cancer worldwide. 5 Most head and neck cancers are squamous cell carcinomas 6 over 90% of which express EGFR 7 which is critical for tumor growth. 8

About lung cancer
Lung cancer is the world's most common cancer and kills more people than any other cancer. In 2008, approximately 1.52 million new cases of lung cancer were diagnosed worldwide, with 1.31 million people dying from the disease. 9

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 programme 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.

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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.

References

1. 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.

2. Li D et al. "BIBW2992, an irreversible EGFR/HER2 inhibitor highlyeffective in preclinical lung cancer models." Oncogene 2008;27:4702-4711

3. 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.

4. MacMillan Cancer Support. http://www.macmillan.org.uk/Cancerinformation/Cancertypes/Headneck/Aboutheadneckcancers/Headneckcancers.aspx. Last accessed 7 May 2010 

5. Hunter KD et al. Profiling early head and neck cancer. Nat Rev Cancer. 2005 Feb; 5 (2): 127-35

6. Viviana P. Lutzky. Biomarkers for Cancers of the Head and Neck. Clinical Medicine: Ear, Nose and Throat 2008:1

7. 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.

8. Normanno N et al. The ErbB receptors and their ligands in cancer: an overview. Current Drug Targets.2005.  May;6(3):243-47.

9. Cancer Research UK. CancerStats Key Facts on Lung Cancer and Smoking. Available at http://info.cancerresearchuk.org/cancerstats/types/lung/. [Accessed 11 May 2010.]

*BIBF 1120 is an investigational compound, its safety and efficacy has not yet been fully established.

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