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Locus Pharmaceuticals Awarded NIH/SBIR Grant for HIV/AIDS Program.

Business Editors/Health/Medical Writers

BLUE BELL, Pa.--(BUSINESS WIRE)--April 29, 2004

Funding to Support Identification of Novel, Orally Active Drug

Leads Targeting Viral Entry Inhibition Mediated by gp41

Locus Pharmaceuticals today announced that is was awarded a Phase I Small Business Innovation Research (SBIR) grant from the National Institutes of Health for "The Design and Development of Potent gp41 Inhibitors." This fully funded award of $180,000 will be used to support the development of novel, drug-like small molecules that disrupt the gp41 mediated viral fusion process. Inhibition of this critical step in the HIV viral life cycle is expected to lead to more effective treatments preventing HIV-1 viral infection.

"Recognition by the National Institutes of Health of Locus's efforts in this highly competitive and important disease area represents a validation of our unique, computationally-directed drug discovery technology, in particular when applied to challenging drug targets like HIV. This award will enhance our extensive work in the area of identifying orally active fusion inhibitors targeting the virus-host cell fusion process. To date, we have made significant progress in the identification of two lead small molecule series and are working toward the selection of an optimal drug candidate to advance into human clinical trials in 2005," said Dr. Bruce Dorsey, Principal Investigator and Director of Chemistry of Locus Pharmaceuticals.

Locus's Novel Approach to HIV

Locus uses three highly integrated technologies to deploy its innovative approach in developing novel, small molecule drug candidates. This powerful approach deploys proprietary computationally-driven algorithms to identify viable binding sites on a target protein and automatically builds the most effective and synthesizable compounds de novo from Locus's 40,000 fragment data set. While such a process may traditionally take years to realize, Locus's in-house 2.3 teraflop super computer allows for a more rapid and efficient process that can often be completed in 4-6 months. By also deploying its in-house crystallography capabilities, Locus is able to affirm the appropriate binding of lead compounds and assure the final selection of clinical compounds. Locus has applied its core technologies to the published gp41 crystal structure identified by Dr. Peter Kim, Dr. Min Lu and other leading HIV research experts as a basis for selecting an IND candidate by early 2005.

"HIV has become increasingly resistant to existing antiviral therapies and there is a pressing need for new drug targets. Viruses that are resistant to existing drugs are sensitive to entry inhibitors. Small molecule inhibitors that block gp41 would be highly desirable since they could be taken by mouth, would be effective against viruses that are resistant to existing therapies, and target a region of the virus that is highly conserved," said Dr. Robert Doms, M.D., Chairman, Dept. of Microbiology, University of Pennsylvania.

HIV: Significant Medical Need

Human immunodeficiency virus (HIV), the etiologic agent of acquired immune deficiency syndrome (AIDS) has infected over 40 million people worldwide. In the U.S., nearly one million Americans are infected with HIV with 40,000 additional cases diagnosed annually according to CDC data. Despite recent improvements in antiretroviral therapy, there remains an urgent need for novel and improved methods of treatment for individuals who are suffering from AIDS. Although highly active antiretroviral therapy (HAART) has dramatically improved patient outcomes, the limitations of treatment options include the emergence of resistant viruses, poor pharmacokinetics, and reduced patient compliance as a result of adverse side effects and treatment regimens. Therefore, the need for additional therapeutic modalities that are safe and convenient remains high.

About Locus Pharmaceuticals

Locus Pharmaceuticals is a privately held pharmaceutical company focused on developing novel, small molecule therapeutics to address major unmet medical needs. Locus combines powerful and proprietary, fragment-based, computational technology with one of the world's fastest Linux-based supercomputer clusters to simultaneously identify relevant binding sites on protein disease targets and rapidly generate novel, drug-like small molecules that bind specifically to those protein sites. Locus further enhances this process through its in-house crystallography effort to assure the most competitive outcome. In contrast to other computational or drug discovery approaches, the Locus technology requires only a high-resolution, 3-dimensional structure of the target protein to implement its drug discovery process. Presently, Locus Pharmaceuticals is synthesizing and developing novel, computationally predicted, drug candidates for the treatment of debilitating and life-threatening human diseases including HIV/AIDS, cancer and inflammation.
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Date:Apr 29, 2004
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