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Merck Serono Exercises Option to Rigel's R763/AS703569 and Aurora Kinase Inhibitors in the Japanese Territory

Wednesday, November 14, 2007 General News
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SOUTH SAN FRANCISCO, Calif., Nov. 14 RigelPharmaceuticals, Inc. (Nasdaq: RIGL) today announced that Merck Serono, adivision of Merck KGaA, has exercised its option to add the Japanese territoryto its current Aurora kinase collaboration that includes the lead product,R763/AS703569. In exchange for these extended development and marketingrights, Rigel will receive a $3 million payment.
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In October 2005, the two companies entered into a worldwide collaboration,excluding Japan, to develop R763/AS703569 and other Aurora kinase inhibitors.As part of this agreement, Merck Serono had the right to add Japan to itsterritory.
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R763/AS703569 is an oral, highly potent inhibitor of Aurora kinases andhas exhibited anti-tumor activity against a broad range of cancer cell lines.To date, three Phase 1 clinical trials with R763/AS703569, sponsored by MerckSerono, have been initiated and are ongoing in patients with solid tumors andleukemia.

"Developing a novel, effective, oral therapeutic for cancer patients isthe primary goal of our Aurora kinase collaboration with Merck Serono," saidRigel's chief operating officer, Raul Rodriguez. "We are proud that MerckSerono has re-affirmed its commitment to this program."

If proven safe and efficacious, this regimen could dramatically alter thelives of patients with a variety of cancers including pancreatic, ovarian,breast, non-small cell lung and colorectal as well as those with hematologicalmalignancies.

Aurora Kinase Inhibitors and Cancer

Cancer continues to be a leading cause of death in the U.S. with 2 millionnew cases diagnosed each year. The over-expression of Aurora kinase can causecells to rapidly develop an abnormal number of chromosomes. Elevated levels ofAurora kinase are frequently associated with various human cancers andinhibition of this enzyme disrupts cell division and promotes programmed celldeath (apoptosis).

Rigel's lead oncology drug candidate, R763/AS703569, is a highly potentinhibitor of Aurora kinases A and B, which is administered orally allowingpatients to take the drug at home as prescribed. R763/AS703569 has exhibitedpotent anti-tumor activity against a broad panel of cancer cell lines.Leukemia cells, lung, breast, pancreas, ovarian and cervical carcinoma cells,and histiocytic cells are particularly sensitive to R763/AS703569. Rigeldiscovered R763/AS703569 using its proprietary high-content cell-basedscreening technologies applied to tumor cell lines.

About Rigel

Rigel is a clinical-stage drug development company that discovers anddevelops novel, small-molecule drugs for the treatment ofinflammatory/autoimmune diseases and cancer, as well as viral and metabolicdiseases. Our goal is to file one new investigational new drug (IND)application in a significant indication each year. Rigel has achieved thisgoal every year since 2002. Our pioneering research focuses on intracellularsignaling pathways and related targets that are critical to diseasemechanisms. Rigel's productivity has resulted in strategic collaborations withlarge pharmaceutical partners to develop and market our product candidates.Rigel has product development programs in inflammatory/autoimmune diseasessuch as rheumatoid arthritis, thrombocytopenia and asthma, as well as incancer.

This press release contains "forward-looking" statements, includingstatements related to the potential efficacy and safety of Rigel's productcandidates. Any statements contained in this press release that are notstatements of historical fact may be deemed to be forward-looking statements.Words such as "plans," "goal," "if," "could," and similar expressions areintended to identify these forward-looking statements. There are a number ofimportant factors that could cause Rigel's results to differ materially fromthose indicated by these forward-looking statements, including risksassociated with the t
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