Cancer Therapeutics reveals proof of concept for second development drug

Jul 4 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 3^rd 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).

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

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