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Phenomix and Plexxikon to Develop Drug Candidate for Treatment of Inflammatory Disease

09 / 12 / 2004

Phenomix to advance two therapeutic programs into the clinic in 2005

Phenomix Corporation, a drug discovery and development company, announced today that a collaboration with Plexxikon has resulted in a drug candidate for the treatment of inflammation. The companies have agreed to initiate joint development of PLX647, a dual c-Kit and FMS kinase inhibitor that has demonstrated efficacy and preliminary safety in preclinical models including collagen-induced arthritis. The collaborators expect to begin human testing of the compound as an orally available treatment for rheumatoid arthritis by the end of 2005. Phenomix and Plexxikon will seek a development and commercialization partner for the program.

"By leveraging our in vivo pharmacology platform, we've been able to quickly and effectively identify an important new class of therapeutics for inflammatory disease," said Laura K. Shawver, Ph.D., chief executive officer of Phenomix. "This compound holds great promise to provide rheumatoid arthritis sufferers an alternative treatment that does not require injections."

Blocking c-Kit and FMS simultaneously with oral PLX647 intercepts two distinct biological pathways crucial to the inflammatory process. It represents a novel approach to the treatment of rheumatoid arthritis that has advantages over currently available disease modifying anti-rheumatic drugs. Inhibition of the c-Kit and FMS pathways mitigates inflammatory response by down-regulating mast cell and macrophage activity. This multi-pathway approach may make PLX647 effective in the treatment of other diseases such as inflammatory bowel disease, asthma, psoriasis and multiple sclerosis.

The discovery of PLX647 is the result of a collaboration between Phenomix and Plexxikon established in November 2003 to discover and develop novel drugs targeting specific kinase pathways critical in inflammation. During the collaboration, Phenomix conducted extensive in vivo pharmacology studies that provided key biological insight in the discovery process while Plexxikon applied its proprietary platform to develop and optimize small molecule inhibitors.

Phenomix Internally Advancing PHX1149 to Clinical Trials for Treatment of Type 2 Diabetes

Phenomix' proprietary program for treatment of type 2 diabetes, PHX1149, will also enter initial human trials in mid-2005. This potent and selective compound has shown excellent safety and efficacy in preclinical studies and may provide a once daily, oral treatment for people with type 2 diabetes that is superior to existing marketed and investigative therapies.

"Our identification of PHX1149 as a preclinical candidate in less than 12 months is a result of Phenomix' integrated approach to drug discovery that utilizes in vivo pharmacology combined with smart, focused medicinal chemistry to rapidly identify novel compounds that are demonstrated to be safe and effective in preclinical models of disease," said Shawver.

PHX1149 inhibits DPP4, a serine protease that is emerging as an important target for the treatment of type 2 diabetes. Inhibition of DPP4 increases the cellular concentration of regulatory peptides made by the body that are critical for the control of blood glucose. PHX1149 has shown promising preclinical results for improving glucose control and is expected to enter clinical trials in mid-2005.

About Phenomix
Phenomix is a drug discovery and development company building a therapeutic portfolio for treatment of immune disease and metabolic syndrome. By generating detailed physiological data in a mammalian system, Phenomix' in vivo technology provides biological insight that allows earlier and better informed decisions across discovery and development. The company's platform is complemented by expertise in drug discovery, translational medicine and clinical development. Phenomix is based in San Diego, California and Canberra, Australia. For more information, visit