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Rigel and Janssen Pharmaceutica form Oncology Drug Discovery Collaboration

New Generation of Functional Genomics Technology Enables Rapid Identification of Drug Targets

Sunnyvale, CA - January 14, 1999

Rigel, Inc. today announced that it has entered into a collaboration with Janssen Pharmaceutica N.V., a Johnson & Johnson (NYSE: JNJ ) company, to identify new drug targets that control the progression of cancer based on Rigel's advanced functional genomics technology. This new approach, which truly links genomics directly to biological cell function, uses Rigel's unique integration of technologies to quickly and thoroughly explore a cell's inner circuitry to find the target that is potentially critical in controlling cell function and could then be specifically modulated to treat disease.

The collaboration with Janssen will focus on the discovery and validation of drug targets that regulate cell cycle, a series of biological events that each cell undergoes in order to divide. In mutated cells, however, the genetic "switches" that regulate this process are disabled, which can lead to uncontrolled cell division and proliferation (cancer). The goal of this research collaboration is to identify targets that can restore a mutated cell's ability to stop uncontrolled cell division either by triggering the self-destruction (apoptosis) of a mutated cell or by stopping the abnormal cell cycle regulation process before a mutated cell can divide and spread. The discovery effort has the potential to result in several novel targets in different areas. Although the collaboration is focused on targets that can be regulated by small molecule (orally-active) agents, the agreement also covers the predictive, diagnostic and protein therapeutic utility of discovered targets.

"We are delighted to be working with Janssen, a recognized leader in pharmaceutical research and development," said James M. Gower, president and Chief Executive Officer of Rigel, Inc. We are confident that it will yield important, novel drug discovery targets and drugs that regulate them."

Under the terms of the agreement, Janssen will provide research funding for a minimum of three years, as well as a cash upfront payment and research milestone payments. Rigel would also receive royalty payments relating to the development and commercialization of pharmaceutical as well as protein therapeutic and diagnostic products resulting from the collaboration. In return, Janssen will retain exclusive worldwide rights to develop and market drugs against the targets that control cell cycle regulation. In addition, the Johnson & Johnson Development Corporation is participating in Rigel's Series D equity financing.

Janssen will also have non-exclusive rights to the use of some Rigel technology to discover targets in other areas of cancer therapy in exchange for milestones and royalties on products resulting from this work.

The Next Generation of Functional Genomics and 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.

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 1 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. Rigel's initial therapeutic programs are focused on inflammation and oncology. In addition to oncology research such as that sponsored by Janssen, programs at Rigel include identifying targets that regulate mast cell exocytosis and those that control the switch to Immunoglobulin E (IgE) in B cells as well as several other approaches to immunity and disease.