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Boehringer Ingelheim

Boehringer Ingelheim Broadens Oncology Pipeline With Promising New Data for Potentially First in Class Plk1 Inhibitor

Ingelheim, Germany (ots/PRNewswire)

  • BI 6727, a Highly Potent and Selective Plk1 inhibitor, Represents Latest Advance in Company's Plk1 Programme
  • For non-US Healthcare Media
Boehringer Ingelheim's most promising new cell cycle kinase
inhibitor and potentially first-in-class compound, BI 6727, has shown
encouraging results in a phase I clinical trial in patients with
advanced tumours who have failed to respond to other treatments.(1)
The data, presented today at a prestigious plenary session and
included in the official press conference of the 20th EORTC-NCI-AACR
Symposium in Geneva, Switzerland, is testament to the company's
ongoing commitment to research and development of innovative cancer
treatments in areas of significant unmet medical need. Boehringer
Ingelheim's research efforts are focused on three main areas:
angiokinase inhibition, signal transduction inhibition and cell cycle
kinase inhibition, under which BI 6727 falls.
Unlike established anti-cancer agents, BI 6727 works by
selectively blocking a part of the cell's make-up that is crucial for
cell division. BI 6727 is one in a series of compounds being
developed by Boehringer Ingelheim in this field. By inhibiting the
activity of Polo-like kinase 1 (Plk1), which is highly expressed in
proliferating cells and most tumours, BI 6727 effectively disrupts
the cell division and induces cell death, thereby inhibiting cancer
growth. Due to its unique mode of action, typical side effects
induced by established anti-mitotic agents such as neuropathy have
not occurred.
According to Professor Patrick Schöffski, Head of the Department
of Medical Oncology at the University Hospitals Leuven, Belgium,
Chairman of the scientific committee for the congress, secretary
general of the EORTC and lead investigator in the trial, the results
indicate an exciting scientific advance.
"Compelling new science in fields such as cell cycle kinase
inhibition brings us a step closer to better understanding the
multiple pathways involved in the growth and spread of tumours and
will hopefully provide us with better treatments to add to the
armoury against this deadly disease," said Professor Schöffski.
"Results to date for BI 6727 have indicated that the drug can be
safely administered to patients with advanced solid tumours and that
it has potential anti-tumour activity. This agent certainly warrants
further investigation," he added.
In the study, which assessed the maximum tolerated dose, overall
safety, pharmacokinetics and preliminary efficacy of BI 6727, a total
of 50 patients were treated at doses of 12 to 450 mg. Results were
encouraging; 32% of patients had stable disease and two patients with
advanced bladder and ovarian cancers showed confirmed responses, both
of whom had previously failed other standard and experimental
treatments. The clear anti-tumour activity demonstrated, not
typically seen in a phase I trial, illustrates the significance of
these findings. Furthermore, BI 6727 was shown to be well-tolerated
with no serious side effects detected.
Preclinical data(2) were also presented at the meeting which
showed  highly selective target inhibition, cellular activity at very
low levels and long-lasting tumour exposure for BI 6727. This,
combined with the phase I data presented suggests a promising future
for BI 6727, supporting Plk1 as a therapeutic target and warranting
further investigation.
The new results presented today complement Boehringer Ingelheim's
additional progress in the fields of signal transduction inhibition
and angiokinase inhibition. Boehringer Ingelheim recently announced
the commencement of pivotal phase III trials for its most advanced
compound, signal transduction inhibitor Tovok(TM) (BIBW 2992) and its
novel triple angiokinase inhibitor(3) Vargatef(TM) (BIBF 1120) is
planned to enter phase  III in the near future.
Commenting on the growth of the Boehringer Ingelheim oncology
portfolio, Dr Manfred Haehl, Corporate Senior Vice President Medicine
at Boehringer Ingelheim said, "The latest data for our Plk1 inhibitor
BI 6727, including initial safety and efficacy results, further
reinforce our continued growth in oncology research and are evidence
of our sustained leadership in Plk1 inhibition. As a company, we are
really excited by the potential these impressive first results hold
and look forward to ongoing growth within our oncology pipeline."
Based on the encouraging results presented at the EORTC-NCI-AACR
Symposium, BI 6727 will advance further in clinical development. The
Phase II programme will assess the efficacy and safety of BI 6727 in
several tumour types.
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.
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.
Boehringer Ingelheim is working in close collaboration with the
international scientific community and a number of the world's
leading cancer centres to research and develop these potential new
treatments for cancer.
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
1. Schöffski, P et al. A phase I single dose escalation study of
the novel polo-like kinase I inhibitor BI 6727 in patients with
advanced solid tumours. Presented Thursday 23 October 2008 at the
20th EORTC-NCI-AACR. Plenary session 5. Molecular targets-state of
the science 10:15-12:00. Abstract Number: 36.
2. Rudolph, D et al. Characterisation of BI 6727, a novel
polo-like kinase inhibitor with a distinct pharmacokinetic profile
and efficacy in a model of taxane-resistant colon cancer. Presented
Thursday 23 October 2008 at the 20th EORTC-NCI-AACR. Poster Display
Period: 12:00PM -15:00PM; Abstract Number: 430.
3. Hilberg F et al. Eur J Cancer Suppl. 2004;2:50.

Contact:

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

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