240 East Grand Avenue
South San Francisco, CA 94080
Phone: 650-624-1100
www.rigel.com

James M. Gower, president and CEO
NASDAQ:RIGL

Overview

Rigel Pharmaceuticals Inc. is a drug discovery and development company that uses functional genomics tools to discover novel drug targets. Its combinatorial biology technology is designed to identify molecules that play a role in regulating a human cell’s response to disease by testing a large number of proteins in cells to determine which proteins will change the cell’s response to the disease.

The technology includes the use of functional assays that model key events in the disease process at the cellular level, retroviral probes to identify potential protein targets, and two hybrid protein interaction and proteomics technologies to identify each of the other proteins involved in the intracellular process and prepare a map of their interactions, providing a comprehensive picture of the intracellular disease pathway.

Rigel has 10 programs under way that examine the biological mechanisms of disease, including asthma/allergy, autoimmunity, transplant rejection, rheumatoid arthritis/inflammatory bowel disease, hepatitis C and tumor growth. It has identified 23 new drug targets. Six programs have generated potential drug compounds, two of which have advanced to preclinical testing: one in the area of asthma/allergy and one in the area of cancer.

In September 2000, Rigel acquired certain antiviral technology from Questcor Pharmaceuticals Inc., including its hepatitis C drug discovery technology, for the research, development and commercialization of pharmaceutical products.

Partners

Rigel has collaborations in the following research programs: allergy/asthma (Pfizer Inc.), autoimmunity (Novartis Pharma AG), respiratory disease (Novartis Pharma AG), transplant rejection (Novartis Pharma AG), tumor growth/oncology (Cell Genesys Inc., Janssen Pharmaceutica NV and Novartis Pharma AG), and neurodegenerative disease (Neurocrine Biosciences Inc.). In 2000, it signed a technology access agreement for access to genomics tools in target identification and validation with Aurora Biosciences Inc.

In 2001, the company entered into collaborations with new partners, including a medicinal chemistry agreement for the optimization of small molecules on inhibitors of ubiquitin ligases with Evotec OAI AG; a structural proteomics collaboration for drug development, initially focused on ubiquitin ligases with MediChem LifeSciences Inc.; functional genomics technology access and collaborative research with Sequitur Inc.; medicinal chemistry services to support and accelerate Rigel’s product development for mast cell program with Albany Molecular Research Inc.; and a license to use DoubleTwist Inc.’s clustering and alignment tools.