Jul 5 2012
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".
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