Aphios Corporation Awarded Innovative Research Grant to Develop Novel ANTI-HIV Therapeutics

26-Mar-2004

Aphios Corporation has been awarded a Small Business Innovative Research (SBIR) Advanced Technology Phase I grant from the National Institute of Allergy and Infectious diseases (NIAID), National Institutes of Health (NIH) to develop novel anti-HIV therapeutics from its unique library of marine microorganisms. Currently, there are 42 million AIDS cases worldwide, with a majority present in the third world; 3.1 million deaths can be attributed to HIV and AIDS in 2002 alone. There is no vaccine against HIV, and AIDS, if untreated, will lead to the death of over 95% of infected individuals 10 years post-infection. In the last few years, significant therapeutic breakthroughs have been made. Mixtures of drugs directed at viral protease and reverse transcriptase have proven to be effective in lowering plasma viral load and slowing the progression of AIDS. However, these cocktail therapies have serious side effects and are financially unattainable by a majority of the HIV-infected population. In addition, resistant strains of HIV are emerging that contribute to the decline in efficacy of these drug mixtures. Thus, new and cost-effective drugs, preferably directed at different viral proteins, need to be developed to keep ahead of this viral pandemic. Aphios has established a unique library of diverse marine microorganisms and marine molecule fractions from normal to extremophilic environments for the rapid discovery and development of novel anti-infectives (HIV, influenza, smallpox, bacterial, MDR). The marine environment represents an enormous and poorly explored resource for anti-infective therapeutics because of its genetic and chemical biodiversity. It is also extremely diversified due to the variety of marine habitats, depending on numerous differences in natural salinities, temperatures and pressures. Aphios has screened over 10,000 partially-purified marine molecule fractions (more than 1 million molecular entities) from its unique marine microorganism library for activity against HIV-1 in cytoprotection and cytotoxicity assays and has identified over 300 "hits," for a hit rate of 3%, that are effective against HIV-1. In this research, Aphios plans to prioritize and confirm a sub-fraction of these "hits" in first a cytoprotection assay and second in a direct viral reduction assay. High priority "leads," such as APP-069 with a selective index (cytoprotection/cytotoxicity) of 250 that compares extremely well with AZT, will be subjected to bioassay guided fractionation, chemical structure elucidation and dereplication.

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