ActivX Biosciences Awarded $1.1 Million Phase II SBIR/STTR Grant from National Cancer Institute for Establishing Drug Toxicity Profiles

June 30, 2003

LA JOLLA, California, June 30, 2003 – ActivX Biosciences, Inc., a privately held biotechnology company applying novel chemical technologies and high-throughput protein analysis to drug discovery, announced today it has received a $1.1. million Phase II award under the Small Business Innovation Research and Small Business Technology Transfer (SBIR/STTR) grant program of the National Cancer Institute (NCI).

The three-year grant, the first Phase II SBIR award received by ActivX, provides for $493,000 in approved funding for the first year with additional funding of $558,000 scheduled over the second and third years. The company was awarded a smaller, six-month Phase I SBIR grant in August 2002 to initiate drug toxicity profiling with its activity-based proteomics technology.

The Phase II grant will fund the establishment of toxicity profiles and the identification of key proteins involved in toxicities and adverse events associated with known toxic agents. This information will be used to evaluate candidate drug compounds for diseases of interest to the NCI, the National Institute for Diabetes, Digestive and Kidney Disorders (NIDDK), and the National Institute for Drug Abuse (NIDA). ActivX will retain worldwide rights to any inventions made in the course of this project.

The focus of the grant is to increase the efficiency of the drug discovery process by developing tools to better understand and more quickly characterize a compound’s toxic effects. The Principal Investigator on the grant is Jonathan Rosenblum, Ph.D., Group Leader, Proteomics Discovery at ActivX. Dr. Rosenblum and his team will establish a database focused on changes in protein activity that result from toxicant exposure. Due to the focus on protein activity, this database is expected to illuminate toxicological mechanisms more so than other methods. ActivX’s proprietary functional chemical probes and high-throughput protein analysis platform are uniquely suited for this project. The database will facilitate the optimization of lead compounds by enabling scientists to rapidly compare protein activity profiles of lead compounds with those of known toxic agents. The database generated as a result of this research should grow over time, providing a ready resource for drug discovery at all stages.

“Toxicity, in many cases driven by off-target activity, is a major concern and a significant contributor to preclinical and clinical failures,” said John W. Kozarich, Ph.D., President & CEO of ActivX. “We believe that understanding the basis for certain toxicities at the molecular level will result in more efficient drug discovery, reduced attrition rates for compounds in later stages of development and, ultimately, better products for patients.”

ActivX Biosciences, Inc. (www.activx.com), a privately held biotechnology company in La Jolla, California, is applying proprietary chemical technologies and high-throughput protein analysis to the drug discovery process. By focusing on functional proteins, ActivX addresses disease mechanisms directly, in contrast to other approaches like expression profiling, in which the analyte being measured is several steps removed from the site of drug action. ActivX and its partners are using its proprietary technology to address critical challenges in drug discovery, including selectivity profiling of candidate drug molecules across whole protein families in biological samples to guide their medicinal chemistry optimization; identifying novel drug targets and biomarkers; and characterizing off-target activities of candidate and established drugs to understand the basis for their efficacy and toxicity.

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Contact: John W. Kozarich, Ph.D.
             Chairman, President
             (858) 526-2502

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