• Rigel’s lead oncology drug candidate, R763, is a highly potent and specific inhibitor of Aurora kinase, which has been shown to block proliferation and trigger apoptosis in several tumor cell lines including cervical, colon, lung, pancreas and prostate.


• R763 has advantages over other existing Aurora kinase inhibitors in that it has the potential to be developed as both an oral and intravenous drug.

• In 2007 Merck Serono initiated two Phase 1 studies of R763, one in leukemia and the other a combination study in advanced malignancies.
• Merck Serono initiated a Phase 1 study of R763 in solid tumors in 2006.
• Rigel partnered with Merck Serono to develop R763, in a deal worth $160M.

• Merck Serono expects Phase 1 results and to initiate Phase 2 trials in 2009.

• Merck Serono Exercises Option to Rigel's R763/AS703569 and Aurora Kinase Inhibitors in the Japanese Territory
• Rigel Announces Start of Phase 1 Combination Therapy Study of R763/AS703569 in Advanced Malignancies

• Merck Serono Phase 1 in Solid Tumors

• Focusing on cell function, we are delivering targeted cancer molecules to our partners while retaining key product candidates.


• Rigel is a strategic partner of choice for pharmaceutical companies in oncology, having partnered with Merck Serono on Aurora kinase inhibitors and R763, Merck and Daiichi on ubiquitin ligase targets, Johnson & Johnson on cell cycle inhibition, and Novartis on anti-angiogenesis targets.

Disease background
Cancer is the second leading cause of death in the United States. More than one million people get cancer each year, and nearly half of all men and a little over one-third of all women in the United States will develop cancer during their lifetimes. Anyone can get cancer at any age, however approximately 77 percent of all cancers are diagnosed in people age 55 and older.