Avexa in HIV therapy partnership

By Graeme O'Neill
Monday, 15 November, 2004

Infectious disease drug-developer Avexa (ASX:AVX) is to work with researchers at the University of Leuven's Rega Institute in Belgium to develop a new HIV/AIDS therapy that will block the virus' integrase enzyme.

Avexa, which was spun out of Victorian pharmaceutical company Amrad earlier this year to focus on anti-infective drugs, will work with the Rega Institute to evaluate several candidate integrase inhibitors developed by the institute's researchers.

Avexa CEO Dr Julian Chick said the Rega Institute was well known for its discoveries of anti-viral drugs, and had several HIV research projects. The partnership will allow Avexa to evaluate several candidate integrase inhibitors developed by the institute's researchers.

Avexa's own chemists have developed several promising inhibitors, and Chick said the Rega collaboration represented an option, rather than a formal agreement, that would allow Avexa to compare the rival compounds.

"It's a way of doing external due diligence without committing substantial resources to the project," Chick said.

The AIDS retrovirus replicates in CD4 helper-inducer lymphocytes and macrophages, employing its integrase enzyme to open up the chromosomes of the host cells and integrate its own genetic blueprint, which then provides a template for the synthesis of new virions.

Chick said an effective integrase inhibitor could stop the virus in its tracks, but effective integrase inhibitors have proved very difficult to develop. Major pharmaceutical companies like GlaxoSmithKline, Merck and Novartis have all tried, with little success.

Chick said Avexa researchers were developing an understanding of the enzyme's structure and function using X-ray crystallography and computational chemistry. "As we learn more, we expect to find hot pockets that we can target with drugs," he said.

"We've been going for a number of years, before we de-merged from Amrad, and we've done a lot of biology and activity assays. We're confident we will succeed in the space."

Chick said Avexa researchers had been screening a range of naturally occurring compounds from bioprospecting, as well as synthetic molecules developed by its own chemists.

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