ActivX Biosciences, Inc.  Awarded SBIR/STTR Grant for Establishing Drug Toxicity Profiles with Activity-Based Proteomic Technology

August 1, 2002

LA JOLLA, California, August 1, 2002 . ActivX Biosciences, Inc. of La Jolla, California, a leader in the field of activity-based, chemo-proteomics, announced today it has received a Phase I award under the Small Business Innovation Research and Small Business Technology Transfer (SBIR/STTR) grant program of the National Cancer Institute (NCI) to increase the efficiency of the drug discovery process by developing protein activity profiles that can be used to screen novel compounds to avoid toxicities or side effects.  The grant, in the amount of $155,000, is the first SBIR grant received by ActivX and is intended to fund six months of research.  ActivX anticipates applying for a Phase II grant to continue and expand the initial study.

The Phase I grant will provide funding to identify key proteins involved in toxicities and adverse events for screening drug compounds indicated for diseases of interest to NCI, the National Institute for Diabetes, Digestive and Kidney Disorders (NIDDK) and the National Institute for Drug Abuse (NIDA).  ActivX will utilize the activity of certain sets of proteins as markers for toxicity, and will establish toxicity profiles that can be used to screen other compounds to rapidly eliminate those with similar profiles.  ActivX's activity-based chemical probes and high throughput protein analysis platform will be crucial for defining the toxicity profiles and developing databases of proteins in various cell types and tissues that are activated due to different but specific molecular mechanisms.  

"A major challenge facing pharmaceutical companies is reducing the drop-out rate of drug candidates in pre-clinical and clinical development, which currently averages about 90% industry-wide," said John W. Kozarich, Ph.D., President & CEO of ActivX.  "A large part of this drop-out is due to toxicities, and decreasing this even a few percentage points would save tens to hundreds of millions of dollars and result in better drugs for patients.  We believe the ability to characterize toxicities at the molecular level, and establish standard profiles for these toxicities that pharmaceutical researchers can employ as filters early in the discovery process, will significantly reduce the attrition rate of compounds in later stages of development.  Our preliminary work is very encouraging, and we feel there is a real opportunity for activity-based proteomics to offer different, and potentially more useful, information than other approaches such as gene transcript profiling or simple protein quantitation." 

About ActivX Biosciences

ActivX Biosciences, Inc., (www.activx.com), a privately held biotechnology company in La Jolla, California, is a pioneer in the field of activity-based, chemo-proteomics, the use of specially designed chemical tools to identify and analyze active proteins important in both normal and disease situations. By focusing on protein activity, ActivX addresses disease mechanisms directly, in contrast to standard genomics and proteomics techniques. ActivX technology includes novel chemical probes integrated with a high-throughput protein analysis platform to rapidly interrogate the activities of proteins in all ranges of abundance in any biological sample, a process it has termed "chemo-proteomics". ActivX is using its proprietary technology to solve key problems in drug discovery and development, including identifying novel drug targets and biomarkers, guiding the medicinal chemistry optimization of lead compounds through profiling and selectivity analysis against active proteins in target cells and tissues, and assessing efficacy and toxicity for candidate and established drugs.

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