First Pivotal Trials Begin for Boehringer Ingelheim's Novel Triple Angiokinase Inhibitor Vargatef(TM) (BIBF 1120)

Ingelheim, Germany, November 17 (ots/PRNewswire) -

- Progress Continues Across Expanding Oncology Pipeline With
Two Compounds now in Phase III Clinical Development and a Potential
First-in-Class Polo-Like Kinase 1 Inhibitor Soon to Enter Phase II

- For non-US Healthcare Media

Boehringer Ingelheim has marked a new milestone within its
rapidly expanding oncology portfolio with the announcement today that
the company has progressed another of its oncology compounds into
pivotal phase III clinical development. The two studies, known as
LUME-Lung 1 and LUME-Lung 2, for Vargatef(TM) (BIBF 1120), a triple
angiokinase inhibitor(1), will evaluate the molecule as a second-line
therapy in combination with standard chemotherapy agents in patients
with advanced non-small-cell lung cancer (NSCLC), a patient
population with limited treatment choices. This significant advance
represents encouraging progress for the company across a portfolio
that spans three key areas of focus: angiokinase inhibition, signal
transduction inhibition and cell cycle kinase inhibition and further
confirms its continued commitment to the field of oncology.

In addition, Boehringer Ingelheim's most advanced compound
Tovok(TM) (BIBW 2992) will soon enter its second pivotal trial,
LUX-Lung 3 in first-line NSCLC. Furthermore, a new compound and
potentially first-in class-molecule, polo-like kinase 1 (Plk1)
inhibitor, BI 6727, has demonstrated such positive phase I results
that it will be progressed to phase II.

According to Dr Nasser Hanna, Associate Professor of Medicine in
the Division of Oncology at Indiana University and principal
investigator of one of the LUME-Lung studies, the commencement of
these trials heralds another stepping stone in the quest to combat
the world's most common fatal malignancy.

"While our battle to conquer cancer continues, lung cancer
remains the leading cause of worldwide cancer deaths despite the
availability of numerous therapeutic options. The need to develop
newer, smarter therapies has never been so urgent," said Dr Hanna.

"The fact remains that one in two non-small cell lung cancer
patients who receive treatment fail their initial therapies and
remain well enough to receive additional options. The LUME-Lung
studies will look at whether the addition of Vargatef(TM) (BIBF 1120)
to standard second-line treatment regimes will improve the outcome
for these patients, and with 2,600 patients, is one of the largest
clinical trial programmes in this indication. There remains a great
need for new treatments for cancer patients to prevent suffering and
prolong life," he added.

Vargatef(TM) (BIBF 1120), works by simultaneously inhibiting
vascular endothelial growth factor receptors (VEGFRs),
platelet-derived growth factor receptors (PDGFRs) and fibroblast
growth factor receptors (FGFRs)1 - all crucially involved in the
formation of blood vessels and is administered as a capsule taken
twice daily. As angiogenesis plays a pivotal role in the growth of
all solid tumours, Vargatef(TM) (BIBF 1120) is currently being
investigated in a number of indications including advanced NSCLC,
prostate cancer, ovarian cancer and colorectal cancer.

The decision to progress this molecule into phase III trials in
NSCLC was based on phase I and II results which showed the agent to
be both efficacious and well tolerated when administered as both
monotherapy and in combination.

In a phase II Vargatef(TM) (BIBF 1120) study(2), which included
74 patients with relapsed, advanced NSCLC, notable results were
reported for patients with good performance status (ECOG* 0 or 1)
(n=57): these patients experienced longer overall survival (OS)
(median OS was 9.5 months), longer Progression Free Survival (PFS)
(median PFS was 2.9 months) and a higher rate of disease control
(59%) compared to the overall study population. Stable disease rate
was 48%. The majority of adverse events reported in the study were
mild to moderate in nature.

In phase I studies, Vargatef(TM) (BIBF 1120) was observed to be
well tolerated at a dose of 200mg twice daily when given in
combination with pemetrexed(3) or paclitaxel/carboplatin(4) in NSCLC
patients and when given in combination with docetaxel in hormone
refractory prostate cancer patients. In addition, initial signs of
clinical efficacy were observed.(5)

According to Dr Manfred Haehl, Corporate Senior Vice President
Medicine, Boehringer Ingelheim, the latest developments across the
company's oncology portfolio are testament to its continued
commitment to research and development in oncology and indicative of
the continual progress being made.

"The commencement of our second pivotal phase III trial programme
within the oncology portfolio, a potential first-in-class within our
cell cycle kinase family and an additional phase III trial planned
for Tovok(TM) (BIBW 2992) reinforce the fact that our pipeline
continues to move closer to our goal - to develop innovative
treatment options that we hope will ultimately offer patients with
cancer better treatment options," said Dr Haehl.

About ECOG
Grade Eastern Cooperative Oncology Group (ECOG) performance status
0 Fully active, able to carry on all pre-disease
performance without restriction
1 Restricted in physically strenuous activity but
ambulatory and able to carry out work of a light or
sedentary nature, e.g., light house work, office work
2 Ambulatory and capable of all self-care but unable to
carry out any work activities. Up and about more than
50% of waking hours
3 Capable of only limited self-care, confined to bed or
chair more than 50% of waking hours
4 Completely disabled. Cannot carry on any self-care.
Totally confined to bed or chair
5 Dead

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 that have the potential to provide significant
clinical and quality of life benefits for patients. 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. Tovok(TM) (BIBW 2992), a novel
representative of the new generation of tyrosine kinase inhibitors,
entered phase IIb/III clinical development in NSCLC earlier in 2008
and was granted Fast Track designation by the FDA. Its second pivotal
trial LUX-Lung 3, will commence soon.

In the area of cell-cycle kinase inhibition, Boehringer Ingelheim
is developing novel, potent and highly selective 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.

The clinical trial programme for Boehringer Ingelheim's oncology
portfolio is themed around the concept of light, and the notion that
the company is committed to illuminating research and development
within the field of oncology. All trials are named accordingly, as
variations on this overall theme.

Boehringer Ingelheim

The Boehringer Ingelheim group is one of the world's 20 leading
pharmaceutical companies. Headquartered in Ingelheim, Germany, it
operates globally with 135 affiliates in 47 countries and 39,800
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 2007, Boehringer Ingelheim posted net sales of 10.9 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

Please be advised

This release is from Boehringer Ingelheim Corporate Headquarters
in Germany. Please be aware that there may be national differences
between countries regarding specific medical information, including
licensed uses. Please take account of this when referring to the
information provided in this document. This press release is not
intended for distribution within the USA.

References

---------------------------------

* ECOG Definition: The Eastern Cooperative Oncology Group
performance status are scales and criteria used by doctors and
researchers to assess how a patient's disease is progressing, assess
how the disease affects the daily living activities of the patient,
and determine appropriate treatment and prognosis.

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(1) Hilberg, F et al. Cancer Res 2008;68(12):4774-82.

(2) von Pawel J et al. J Thorac Oncol. 2008; 3(Suppl 1): Abstract
163O (oral presentation).

(3) Hanna N et al. 12th World Conference on Lung Cancer, Seoul,
South Korea, 2-6 September, 2007.

(4) Camidge R et al. J Clin Oncol 26: 2008 (May 20 suppl; abstr
3567).

(5) Data on file. Boehringer Ingelheim.

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

Contact:
Contact: Julia Meyer-Kleinmann, Science & Technology Communications,
Boehringer Ingelheim GmbH, Tel.: +49-6132-77-8271, Email:
press@boehringer-ingelheim.com