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Rigel Announces Collaboration with Pfizer to Identify Drug Targets in Allergy and Asthma

Second Corporate Partner Signed in a Month

Sunnyvale, CA - February 01, 1999

Rigel, Inc. today announced that it has entered into a research collaboration with Pfizer, Inc. (NYSE:PFE) to identify new drug targets that control the body's allergic response using Rigel's advanced functional genomics technology. This agreement marks Rigel's second drug discovery collaboration in a month.

Researchers from the two companies will use Rigel's unique integration of technologies to quickly and thoroughly explore the inner circuitry of cells to identify and validate drug targets that prevent B cells from producing immunoglobulin E (IgE), a key mediator in allergic reactions and asthma. The collaboration is focused on targets that can be regulated by small molecule (orally active) drugs, a complementary approach to the successful intravenous anti-IgE antibody products currently in development.

Under the terms of the agreement, Pfizer will provide research funding to Rigel for a minimum of two years, as well as cash and equity upfront payments and research milestones. Rigel will also receive royalty payments relating to the development and commercialization of any human or animal therapeutics resulting from the collaboration. In return, Pfizer will have worldwide rights to develop and market human and veterinary drugs against the targets that inhibit the switch to IgE in B cells.

"Our collaboration with Pfizer comes at a very exciting time for Rigel," said James M. Gower, President and Chief Executive Officer of Rigel, Inc. "Not only does it come on the heels of our oncology drug discovery collaboration with Janssen Pharmaceutica, but also as we prepare to move into new, larger, custom-built facilities where we can continue our pioneering drug discovery work."

A New Era In Drug Discovery

Unlike current functional genomics approaches, which begin with an assumption of how a given gene or product works in a disease process and then undertake validation steps to confirm it actually affects biological function in a useful way, Rigel's approach starts with functionally-validated targets for drug intervention and then looks for the relevant genes. This revolutionary approach of beginning with pharmaceutically interesting function offers a faster, more efficient process that has the potential to cut dramatically the timelines on early drug discovery.

The process begins with the introduction of Rigel's proprietary retroviral probes -- which can be directed to a specific location within the cell (e.g., nucleus, cytoplasm) -- into cells representative of the disease. A stimulus is then applied to make the cells display the behavior (phenotype) of that disease process. Using Rigel's specially designed functional biology screens that allow sorting of more than 60,000 cells/second -- which means that a study of 100 million cells can be completed in just a few hours -- data is collected on up to 10 different parameters that describe how each cell responded to the stimulus. By analyzing the resultant one billion data points, this approach can rapidly identify the cells containing the probe that has, due to its interaction with a target in the cell's internal circuitry, caused the desired phenotypic change.

By using the probes as "fish hooks" in proprietary genetic target identification screens, Rigel can then extract the resident target that the probe has affected and begin to characterize it by its functional relationship. Rigel's retroviral-based approach allows the use of the cell's progeny (i.e. "offspring") or additional naive cells, which carry the same phenotype-changing probe, to conduct subsequent tests to confirm and further define the target. The integration of these technologies yields not only functionally validated targets but also a functionally defined signaling pathway map of the cell's inner circuitry, structure-activity relationship information that can be valuable in subsequent drug design and a competitive binding element in drug screening.

Rigel, Inc., a privately held company founded in 1996, is focused on the discovery of novel therapeutic agents. The Company's rapid target identification and validation technology integrates proprietary advances in gene transfer techniques with combinatorial chemistry, genomics and ultra high-throughput screening. The company currently has research collaborations with Janssen Pharmaceutica to discover oncology therapeutics and diagnostics based on cell cycle regulation and with Pfizer Inc. to discover human and veterinary drugs for asthma and allergy based on IgE regulation in B cells. Rigel also has research programs exploring the regulation of mast cell exocytosis in allergy/asthma as well as T and B cells in other immunological settings.