Rigel reports progress in cancer programme

Rigel Pharmaceuticals, from South San Francisco, CA, US, has identified R763 as a lead compound in its aurora kinase inhibition program, targeting cancer cell proliferation, and plans to file an investigational new drug (IND) application by Q3, 2005.

Aurora kinase plays a central role in the cell division process. An overabundance of aurora kinase can be linked to the transformation of normal cells into cancer cells and has been identified in many tumour types, including colon cancer, breast cancer and leukaemia. R763 is a potent, highly-selective, small-molecule inhibitor of aurora kinase. Rigel discovered the R763 compound class using a high-content cell-based phenotype assay that simultaneously measures cell proliferation, apoptosis, cellular morphology and normal cell cycling.

'Aurora kinases are one of the most promising targets in oncology drug discovery,' said Dr Elliott Grossbard, senior vice president of medical development. 'Rigel's R763 is one of the most potent aurora kinase inhibitors known and potentially can be delivered both orally and intravenously, a valuable property not reported for previously described compounds.'

'Aurora kinase inhibition provides a promising, novel approach for the treatment of multiple human malignancies,' said Dr David Alberts, MD of the Arizona Cancer Center of the University of Arizona. 'Rigel's program signals an important step toward unlocking the potential for a new class of drugs that could significantly impact the future of cancer treatment.'

Aurora Kinases and cancer

The overexpression of aurora kinase can cause cells to quickly form an abnormal number of chromosomes. As such, aurora kinase is frequently associated with various human cancers such as breast, bladder, colon, ovary, head and neck, and pancreas. Increased knowledge of aurora kinase and its regulation potential may be the basis for treating and even preventing cancer.