Rigel's Janus Kinase 3 inhibitors show benefit in organ transplant model

By E. Janene Geiss

Philadelphia, July 19 - Rigel Pharmaceuticals, Inc. said Wednesday that data from preclinical studies of multiple potent and selective inhibitors of Janus Kinase 3 were found to significantly extend allograft survival in animal heart transplant models.

These compounds effectively inhibit JAK3-dependent lymphocyte proliferation and are highly selective in an array of off-target assays, according to a company news release.

The compounds were discovered and characterized by Rigel, and the heart transplant models were conducted by researchers at Stanford University as part of a collaboration with Rigel.

The company said it will file an Investigational New Drug application with one of the JAK3 inhibitors and plans to pursue JAK3 inhibition in a variety of autoimmune diseases, in addition to transplant rejection therapy.

Organ recipients receive life-long treatment with immunosuppressive drugs to prevent organ rejection. With the currently available pharmaceuticals, fewer than 50% have a functioning replacement organ after 10 years.

Current anti-rejection therapy suppresses the immune system with a cocktail of drugs including cyclosporin and steroids, the long-term use of which has been shown to cause kidney damage, hypertension, atherosclerosis and diabetes, officials said.

The company will present the study results at the 2006 World Transplant Congress taking place next week in Boston.

Rigel is a South San Francisco, Calif., clinical-stage drug development company.

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