Cancer Therapeutics, a company focused on translating cancer biology
research into novel treatments for cancer, today announced the
validation and performance of a new targeted drug, CTx-294886, in
combination with Avastin™ (bevacizumab – Genentech/Roche) in a
preclinical model of breast cancer. At the same time the Company
announced that it has developed a new High Throughput Screening (HTS)
platform for the identification of small molecule inhibitors of protein
ubiquitination, a key element in the essential cellular process of
protein homeostasis, which is an exciting new target pathway for cancer
treatment. Both scientific developments will be presented as posters at
the EACR conference in Barcelona Spain on July 7-10 2012.
The anti-tumour response to CTx-0294886, a potent small molecule
inhibitor of Focal Adhesion Kinase (FAK) and Vascular Endothelial Growth
Factor Receptor 3 (VEGFR3), was compared with that of the Company’s
first product CTx-0294945, a potent selective FAK inhibitor. CTx-0294886
in combination with Avastin™, showed additional benefits to
those previously demonstrated by CTx-294945 (previously presented at the
AACR conference in Chicago on the 3rd of April this year). In
both cases the small molecules in combination with Avastin™ inhibited
angiogenesis, and increased the duration of tumour response in a model
of basal breast cancer. In addition CTx-294886 in combination with
Avastin™ also provided a highly statistically significant increase in
the median survival time compared to the Avastin™ only group.
The new Ubiquitin HTS platform closely replicates cellular
ubiquitination pathways, and provides a mechanism for HTS of multiple
targets. Ubiquitins are small regulatory proteins that attach to other
target proteins allowing their destruction and recycling. This process
requires a family of dedicated enzymes, such as ligases, for completion.
E6AP, an E3 ligase, was selected to validate the platform. E6AP
ubiquitinates p53 and PML in human papilloma virus (HPV) related and
other cancers. Both p53 and PML are well known suppressors of tumour
growth so substances that inhibit E6AP would be expected to retard
tumour growth in cancers such as cervical and head and neck cancers. The
platform was able to identify several small molecules that are now
undergoing further investigation.
Dr Warwick Tong, CEO of Cancer Therapeutics, commented:
“Having achieved preclinical validation for our first product candidate
in conjunction with Avastin, we are delighted to be announcing that our
second candidate is even more potent at prolonging and strengthening the
effects of Avastin. We are excited to have two targeted molecules that
will allow rational combinations with other therapies in the fight
against cancer. We are now starting to reap the benefits of our highly
collaborative approach to drug discovery, working hand in hand with some
of the top research institutes in Australia and our international
partner, Cancer Research Technology UK”.
Dr Ian Street, Chief Scientific Officer of Cancer Therapeutics, added:
“The launch of our new Ubiquitin HTS platform opens up the potential to
collaborate with industry by screening chemical libraries to address
multiple targets in this new and exciting area of cancer biology. We are
ready to begin discussions with other companies who would like to work
with us to include their targets of interest and screen their chemical
libraries using this platform”.
The titles of the posters being presented throughout the conference are:
Poster 846: “Inhibition of Focal Adhesion Kinase in Combination With
Bevacizumab Reduces the Rate of Tumour Revascularization and Increases
Survival in a Pre-clinical Model of Basal Breast Cancer” by I. Street et
al.
Poster 1039: “A High Throughput Screening Platform for the
Identification of Small Molecule Inhibitors of the E3 Ligase E6AP” by I.
Street et al.
Cancer Therapeutics will be available at the EACR to discuss both
posters: at Sunday 8 July: 16:00−17:30 CET (Poster 846) and
Monday 9 July at 16:00−17:30 CET (Poster 1039).
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About Cancer Therapeutics CRC
Cancer Therapeutics is a small molecule drug discovery company that is
translating innovative cancer biology research into lead and preclinical
stage drug candidates. In particular it is targeting novel cancer
pathways associated with the tumour microenvironment or growth, to
develop novel treatments for breast, prostate, melanoma, lung and brain
cancers. Cancer Therapeutics’ business strategy is to license or forge
collaborations to take its quality lead and preclinical stage small
molecule drug candidate assets to international pharmaceutical or
biotechnology companies for clinical development. Located in Melbourne,
Australia the Company was founded in January 2007 through a
collaboration between a number of Australia's leading research
institutions and commercial organisations. Further information can be
found at www.cancercrc.com
About CRC Australia
The Cooperative Research Centres (CRC) program is an Australian
Government Initiative.
The CRC program supports end-user driven research collaborations to
address the major challenges facing Australia. Australia’s network of
CRCs operates across all sectors of Australia’s economy and society.
Further information about the CRC program is available from www.crc.gov.au
