Cancer Therapeutics proves concept behind new drug

Drug discovery company Cancer Therapeutics has demonstrated proof of concept for its second targeted drug, and developed a new screening platform to help discover more small molecule candidates.

The Melbourne-based company has revealed results from a preclinical trial of CTx-294886, a small molecule drug, when used in combination with bevacizumab.

Bevacizumab is a monoclonal antibody marketed by Genentech and Roche as Avastin, which is in use to treat various cancers including colorectal, kidney and ovarian cancer.

CTx-294886 is an inhibitor of Focal Adhesion Kinase (FAK) and Vascular Endothelial Growth Factor Receptor 3 (VEGFR3).

Administering the drug in combination with Avastin delivered a statistically significant increase in median survival time compared to the Avastin only group during the preclinical study.

The combination also delivered superior results to using Avastin in conjunction with Cancer Therapeutics' first product, CTx0294945, a selective FAK inhibitor.

“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,” Cancer Therapeutics CEO Dr Warick Tong said.

The company has also announced it has developed a new High Throughput Screening (HTS) platform to help identify small molecule inhibitors of protein ubiquitination.

The Ubiquitin HTS platform replicates cellular ubiquitination pathways. Ubiquitins are small regulatory proteins that attach to target proteins, allowing their destruction and recycling.

E6AP, an E3 ligase which was the target during the proof-of-concept for the platform, ubiquinates the proteins p53 and PML. Both these proteins are known inhibitors of tumour growth in HPV-related and other cancers.

Inhibitors of E6AP could therefore have applications in retarding tumour growth in cervical and other cancers. The platform has identified several potential small molecule inhibitors, which are now being further studied.

Cancer Therapeutics will be presenting the results of the early studies of both CTx-294886 and the Ubiquitin HTS platform at the EACR Conference in Barcelona, which runs from July 7-10.