Aphios Corporation

Anti-Influenza Therapeutics

Influenza is a common and serious respiratory illness that contributes to the reduction of quality-of-life and a significant loss of manpower hours each year. Every year 40 million Americans develop the flu and 20,000 to 40,000 Americans die from it, making it the deadliest infectious disease in the United States. In the case of a pandemic caused by a mutated H5N1 virus or other flu strain, the mortality rate will increase by several orders of magnitude. Tamiflu® is the lead antiviral that is effective against H5N1, and there are concerns that resistance may develop to the H5N1 virus and mutant strains. Thus, there is a need for more effective anti-influenza therapeutics. Nature is an excellent source of novel anti-influenza drugs; 71% of the antiviral NCEs approved in the last two decades, including Tamiflu®, are naturally derived or based on a natural product.

Aphios’ scientists and engineers are screening a unique library of diverse marine microorganisms, isolated from normal to extremeophilic environments in United States territorial waters, and medicinal plants to discover novel anti-influenza drugs. Research is being done under Biohazard Safety Level-3 conditions. The Company utilizes a patented SuperFluids™ CXF fractionation technology for the rapid discovery and development of anti-influenza drugs. This technology is utilized to effectively disrupt marine microorganisms and selectively extract bioactive compounds based on their polarities. In comparative screening programs with Bristol-Myers Squibb and Pfizer, SuperFluids™ CXF technology was shown to: (1) produce a unique spectrum of secondary metabolites, (2) reduce interference from nuisance compounds, (3) minimize background noise in sensitive molecular assays; and (4) enhance the probability of "clean" hits. A closely related SuperFluids™ CXP platform can be utilized to manufacture drugs for preclinical development and commercial production.

To date, utilizing proprietary enabling drug discovery technologies, we have screened about 1,000 marine molecule fractions (approximately 2% of our marine microorganism library) against influenza A (H3N2) and influenza B in biological assays. Hits were selected on the basis of a Selectivity Index (SI) that reflects therapeutic efficacy. We have identified 2 very active hits (SI >100) against influenza B, 13 active hits (SI >10) against influenza A and 21 moderately active hits (SI> 1) against influenza A. From screening medicinal plants utilizing proprietary drug discovery technologies, we have identified an anti-influenza hit that has a selective index against influenza A that is higher than the positive control utilized in the biological assays.

Our overall goal is to identify compounds from marine microorganisms and medicinal that are active against different strains of influenza A including H5N1 viruses and influenza B, and that act on viral proteins other than those targeted by current anti-influenza drugs. We have ongoing research agreements with the National Institute of Allergy and Infectious Diseases, NIH and United States Army Medical Research Institute of Infectious Diseases, DOD for testing compounds against different strains of influenza.

Aphios Corporation is seeking strategic corporate partners and investors to accelerate the discovery and development of novel anti-influenza drugs that are effective against H5N1 and other virulent strains of bird flu as well as circulating strains of influenza.