Aphios scores grant for green drug discovery technology

SBIR grant will fund development of prototype tech to unearth potential therapeutic chemicals in biomass

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WOBURN, Mass.—Plants and microorganisms provide the raw ingredients for a large number of drugs that have received regulatory approval in recent decades. But the potential for discovering valuable new chemical entities (NCEs) in the Earth’s biomass has been limited by technical challenges involved in extracting bioactive natural molecules, in addition to changing research priorities.
A drug discovery technology under development by Aphios Corp. could make it easier for researchers to untap the therapeutic potential found in biomass. Last month, Aphios—an emerging biotechnology company focusing on the development of green technology platforms—announced that it received a Small Business Innovation Research (SBIR) grant that will fund the development of a prototype for its technology. “This is significant both internally, because this technology will help us advance our own drug discovery program, and externally, because it could be a tremendous boon to other researchers at academic research institutions and pharmaceutical companies,” Dr. Trevor Castor, CEO of Aphios, tells DDNews.
The patented technology platform that the SBIR grant funds is designed to facilitate the rapid discovery of therapeutic drugs and quality-of-life medicines from terrestrial plants and marine organisms. Pure compounds provide the clearest benefit in bioactive screens during the process of discovering complex natural moleules. Currently, however, it is prohibitively expensive to isolate and purify new natural product molecules without a predefined biological activity. Moreover, many potent biologically active compounds occur in trace amounts that are likely to be missed in any broad-scale purification of natural products from a complex matrix.
To address these problems, Aphios patented its method of critical fluid fractionation (CXF), which produces partially purified compounds through a rapid process that can be automated. The CXF technology places biomass into contact with environmentally friendly SuperFluids such as carbon dioxide, with or without small quantities of polar co-solvents (in Aphios’ SuperFluids CRY process, a supercritical or near-critical fluid is slowly added to a conventional organic liquid solvent containing the solute to be crystallized). This enables the rapid preparation of partially purified natural product mixtures that minimize false positives and negatives in sensitive biological screens.
“In a direct, large-scale, head-to-head comparison with conventional organic phase extraction used by Bristol-Myers Squibb Co., we have demonstrated that the CXF process increases the recovery and diversity of secondary metabolites,” says Castor. “Additionally, this collaboration determined that the hit rate from over 40 screens was 200 percent higher in SuperFluids fractions than in either butanol or aqueous fractions.”
One of the most attractive features of the new technology, says Castor, is its potential for automation. “Researchers can press a button, move on to something else and then come back to retrieve the results,” he tells DDNews. “There’s a sequential process with standard protocols, but there will also be software capabilities to customize the process for different needs.”
The SBIR grant was awarded by the National Center for Complementary and Alternative Medicine (NCCAM), a division of the National Institutes of Health (NIH) that is tasked with supporting the study of the usefulness and safety of complementary and integrative medical interventions and their roles in improving health and healthcare. NIH’s SBIR program funds early-stage small businesses commercializing innovative biomedical technologies.
Castor says that the Aphios technology may help to fill a gap in the drug development community left by the elimination of natural products research programs at many pharmaceutical companies. This shift came about  in part due to a new emphasis on using high-throughput screening of mass-produced combinatorial libraries against the many disease targets developed as a result of the explosion of biologic and genetic information, and the sequencing of the human genome.
According to Castor, this paradigm shift has not resulted in the expected surge in productivity in the discovery pipeline, due in part to the shift from screening natural products molecules that have been honed by millions of years of evolutionary development to screening simple organic structures that can be readily manipulated by combinatorial chemistry. One of the driving forces behind the paradigm shift from natural to synthetic, however, was the difficulties associated with the discovery of bioactive natural molecules. The CXF platform is expected to reduce these difficulties.

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