Boehringer Ingelheim to Commence Phase III Study Investigating the Role of BIBW 2992 (Tovok(TM)) as First-Line Treatment for Non-Small Cell Lung Cancer (NSCLC) Patients With EGFR Mutations

Ingelheim, Germany (ots/PRNewswire) -

- Data From Phase II Studies Investigating BIBW 2992 (Tovok(TM))
and BIBF 1120 (Vargatef(TM)) in NSCLC Patients Presented at 13th
World Conference on Lung Cancer (WCLC)

INGELHEIM, Germany, August 3 /PRNewswire/ --

Boehringer Ingelheim announced today at the International
Association for the Study of Lung Cancer's 13th World Conference on
Lung Cancer (WCLC), San Francisco, CA, the initiation of a Phase III
clinical study of BIBW 2992 as first-line treatment in non-small cell
lung cancer (NSCLC) patients with epidermal growth factor receptor
(EGFR) mutations. BIBW 2992 (planned brand name Tovok(TM)) is the
first orally-administered, irreversible dual inhibitor of EGFR and
HER2,[1] to reach Phase III development in NSCLC.[2]

This LUX-Lung 3 trial will compare the efficacy and safety of the
single-agent BIBW 2992 to that of standard chemotherapy
(cisplatin/pemetrexed ) as a potential first-line treatment for NSCLC
patients with EGFR mutations.[3] Boehringer Ingelheim's LUX-Lung
trial programme currently includes two Phase III trials assessing the
efficacy and safety of BIBW 2992 in various NSCLC patient populations
across the globe.

"The Boehringer Ingelheim LUX-Lung 3 trial studying BIBW 2992 in
patients with EGFR mutations will be important as we continue to work
towards providing personalized medicine for patients with lung
cancer," said James Yang, MD, PhD, Professor at the Graduate
Institute of Clinical Medicine and the Graduate Institute of Clinical
Pharmacy at the College of Medicine at the National Taiwan University
(NTU). "BIBW 2992 is an irreversible tyrosine kinase inhibitor1 whose
clinical benefit we are hoping to confirm in the first-line setting
for patients with EGFR mutations".

This milestone coincides with the oral presentations of new data
at WCLC suggesting the compound's potential:

- Preliminary data from the Phase II LUX-Lung 2 trial of NSCLC
patients with an EGFR mutation show a response rate of nearly two-
thirds (63%) and a disease control rate of 97% in 38 evaluable first-
line patients.[4] The most commonly (greater than 5%) observed adverse
events were Grade 3 and included diarrhea, skin-related adverse events
and mouth ulcerations.[4] Comparable response rates (66%) and disease
control (97%) rates were observed in the second-line setting.[4]
- Preliminary data from another study showed that BIBW 2992
improved disease symptoms and reduced the size of tumors in three
heavily pre-treated patients with HER2neu mutations.[5] Results from
this trial warrant further investigation of BIBW 2992 as a potential
new treatment option for NSCLC patients who have HER2neu mutations.[5]

On May 29, Boehringer Ingelheim announced that it entered into an
agreement with the Manchester, UK-based company DxS to provide a
companion diagnostic test kit for BIBW 2992 to identify mutations of
the EGFR in patients with non- small cell lung cancer. Under the
terms of the agreement, DxS and Boehringer Ingelheim will work
jointly to make a suitable companion diagnostic test kit globally
available.

Data for BIBF 1120 (Vargatef(TM)) in NSCLC

Also presented at the conference were results from a
pharmacokinetic analysis of another Boehringer Ingelheim compound,
BIBF 1120 (planned brand name Vargatef(TM)), an angiogenesis
inhibitor that simultaneously inhibits vascular endothelial growth
factor receptors (VEGFR), platelet-derived growth factor receptors
(PDGFR) and fibroblast growth factor receptors (FGFR). The data
presented at the conference come from a Phase II study investigating
the efficacy and safety of the compound in patients with relapsed
advanced NSCLC.6 This double-blind multicenter trial included
patients with an Eastern Cooperative Oncology Group (ECOG)
performance status of 0-2 with relapsed NSCLC after failure of first-
or second-line chemotherapy.[6]

The analysis shows that the pharmacokinetics of BIBF 1120 are
independent from patient characteristics (e.g., age, weight, height,
gender, smoking status, etc.).[6]

Updated efficacy and safety data from this study demonstrate that
patients with an ECOG performance status of 0-1 had a median overall
survival of 264 days (n=56).[6] These data suggest that BIBF 1120 has
single-agent activity in patients suffering from recurrent NSCLC.6
Preliminary data from this study were presented in April 2008 at the
1st European Lung Cancer Conference in Switzerland.

The data presented at WCLC, and the ongoing Phase III development
of its two most advanced compounds, mark significant progress for
Boehringer Ingelheim's evolving oncology pipeline. In addition to
BIBW 2992 and BIBF 1120, Boehringer Ingelheim has several oncology
compounds in earlier clinical and pre-clinical development.

Boehringer Ingelheim believes in evidence-based, scientific
progress; its extensive oncology clinical trial programme involves
more than 800 study centers in 47 countries. Boehringer Ingelheim has
a dedicated cancer research center in Vienna where scientists are
focused on the discovery and development of new treatments to combat
or alleviate the symptoms of cancer.

Clinical trial information

Additional information on the LUX-Lung 3 trial will be available
on http://www.clinicaltrials.gov.

The global LUME-Lung Phase III clinical trial programme is
investigating BIBF 1120 in combination with standard second-line
chemotherapy in patients with advanced NSCLC. The studies are ongoing
and with a recruitment target of 2,600 patients worldwide. This is
one of the largest Phase III study programs in an advanced NSCLC
patient population to date.[7,8]

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. In the United States, an estimated
161,840 deaths, accounting for 29 percent of all cancer deaths,
occurred in 2008, according to the American Cancer Society (ACS).

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 centers, 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 tumors and hematological cancers.

The current focus of research includes compounds in three areas:
angiogenesis inhibition, signal transduction inhibition and
cell-cycle kinase inhibition. BIBW 2992 entered Phase IIb/III
clinical development in NSCLC earlier in 2008 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 (Plk1), a protein that is involved
in the processes of cell division. These molecules are in the early
stages of clinical development.

Boehringer Ingelheim

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 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://www.boehringer-ingelheim.com

REFERENCES

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

2. BIBW 2992 and BSC Versus Placebo and BSC in Non-Small Cell
Lung Cancer Patients Failing Erlotinib or Gefitinib (LUX-LUNG 1). 23
April 2009. Available at: http://clinicaltrials.gov/ct2/show/NCT00656
136?term=BIBW+2992+and+Phase+III&rank=1 . Accessed on 5 May 2009.

(Due to the length of this URL, it may be necessary to copy and
paste this hyperlink into your Internet browser's URL address field.
Remove the space if one exists.)

3. Boehringer Ingelheim. Clinical Trial Protocol. BIBW 2992:
Trial No. 1200.32. Doc. No.:U09-1380-01. 14 May 2009.

4. Yang, Chih-Hsin et al., "BIBW 2992, a novel irreversible
EGFR/HER2 tyrosine kinase inhibitor, in chemonaïve patients with
adenocarcinoma of the lung and activating EGFR mutations (LUX-Lung
2)." 2009 WCLC, Oral Presentation#1200.22.

5. De Greve, J. et al., "Clinical activity of BIBW2992, an
irreversible inhibitor of EGFR and HER2 in adenocarcinoma of the lung
with mutations in the kinase domain of HER2neu." 2009 WCLC, Oral
presentation # 1200.41.

6. Reck, Martin et al., "A Phase II double-blind study to
investigate efficacy and safety of the triple angiokinase inhibitor
BIBF 1120 in patients with relapsed advanced non-small cell lung
cancer." 2009 WCLC, Poster Discussion Presentation #1199.10.

7. LUME-Lung 1: BIBF 1120 Plus Docetaxel as Compared to Placebo
Plus Docetaxel in 2nd Line NSCLC. Available at:
http://clinicaltrials.gov/ct2/show/NCT00805194?term=LUME+Lung&rank=1.
Accessed on 25 March 2009.

8. LUME Lung 2: BIBF 1120 Plus Pemetrexed Compared to Placebo
Plus Pemetrexed in 2nd Line Nonsquamous NSCLC. Available at:
http://clinicaltrials.gov/ct2/show/NCT00806819?term=LUME+Lung&rank=2.
Accessed on 25 March 2009.

ots Originaltext: Boehringer Ingelheim
Im Internet recherchierbar: http://www.presseportal.de

Contact:
Corporate / Global Media Contact, Julia Meyer-Kleinmann, Head Science
& Technology, Communications, Boehringer Ingelheim GmbH, Tel:
+49-6132-77-8271, Mobile: +49-178-2908178, Email:
press@boehringer-ingelheim.com