Eqitx selects pain drug candidates
Monday, 16 February, 2004
Perth biotechnology company EqiTX (ASX:EQX) has passed the first development milestone for its gingerol project, which aims to develop drugs to treat pain and inflammation from compounds isolated from the plant Zingiber officinale.
The company has been assessing a library of compounds synthesised by University of Sydney School of Pharmacy professor Basil Roufogalis in order to select lead candidates for further development.
According to CEO Noel Chambers, the compounds were screened for activity against the vallinoid receptor VR1 as well as COX1 and COX2, and benchmarked with gold standard compounds including capsaicin for VR1 activity and market-leading COX2 inhibitor Celebrex.
A number of compounds have been identified with either VR1 specific activity -- suitable for treating pain without having anti-inflammatory properties, COX2 specific activity -- which could be used to treat inflammation, or mixed VR1/COX2 activity.
Chambers said some compounds appeared to have super-agonist properties against VR1 -- that is, they were more active than capsaicin. Similarly, other compounds have been found with equal or better activity than Celebrex.
"We found a number of good candidates for both pain and inflammation," he said. "These results validate our focus on pain and inflammation."
The results have allowed the company to select pain management, in particular neuropathic pain, as the highest priority for development.
"The Milestone 1 studies have enabled us to select a number of drug candidates for further evaluation in 'Milestone 2', which will focus primarily on neuropathic pain," Chambers said. "Growth in the global pain management drug market is expected to driven by second-generation COX2 [cyclooxgenase] inhibitors and novel neuropathic pain therapies."
New and improved synthetic methods have also been developed, he said.
Eqitx is now investing a further AUD$680,00 into the project, boosting its equity in subsidiary ZingoTX, which has been assigned the IP rights to the project, to 40.5 per cent.
The next step, Chambers said, would be to perform animal studies to examine the activity of the compounds in models of chronic pain, in comparison to drugs such as gabapentin and morphine -- the two leading compounds for pain management.
He estimated that the next phase of development, which would lead up to selection of the lead candidate for a formal pre-clinical work-up, would be completed towards the end of the year.
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