Chelsea Therapeutics Reports Significant Efficacy of CH-4051 in Reduction of Collagen-Induced Arthritis in Animal Model

Chelsea Therapeutics Reports Significant Efficacy of CH-4051 in Reduction of Collagen-Induced Arthritis in Animal Model

CHARLOTTE, N.C., March 25, 2008 -- Chelsea Therapeutics International, Ltd. (Nasdaq:CHTP) announced positive results from a preclinical study to investigate the use of CH-4051, the second compound from its portfolio of metabolically inert antifolates, to treat rheumatoid arthritis. 

This 17-day study was designed to test the efficacy of CH-4051 in a rat collagen-induced arthritis (CIA) model. The results reveal a remarkable level of efficacy in delaying the onset of the disease, significantly decreasing the severity and, at certain doses, completely blocking all development of rheumatoid arthritis (RA). The most significant finding from this study was that once daily dosing of 10mg/kg of CH-4051 administered from day 0 completely prevented the onset of arthritis. Similarly, twice daily 5mg/kg doses of CH-4051 reduced the severity of disease in all animals and prevented disease onset in some. Both the once daily dose of 10mg/kg and the twice-daily dose of 5mg/kg dose of CH-4051 demonstrated better prevention of disease than 0.25mg/kg of methotrexate (a known efficacious dose in this model) administered every 3 days. Dr. Simon Pedder, President and CEO, will present the results from this study at the BioCentury Future Leaders Industry Conference on Thursday, March 27th at 2:30 p.m. EDT.

"The CIA model is the standard by which anti-inflammatory activity is measured and the results for CH-4051 are highly consistent with the data generated by other compounds known to be efficacious in the treatment of RA," commented Dr. Simon Pedder, President and Chief Executive Officer. "Having already initiated our human Phase II proof-of-concept trial of CH-1504 in RA, we are pleased to now begin the process of validating the potency of additional compounds in this portfolio. This new data further supports the activity previously demonstrated by CH-1504 in a pilot human study and underscores the promise of our full portfolio of metabolically inert antifolates. This study was conducted in parallel with our ongoing IND-enabling toxicology work for CH-4051 and reflects our commitment to expanding the development of our existing pipeline."

About Chelsea Therapeutics

Chelsea Therapeutics is a biopharmaceutical development company that acquires and develops innovative products for the treatment of a variety of human diseases. The Company is currently developing a library of metabolically inert antifolate compounds engineered to have potent anti-inflammatory and anti-tumor activity to treat a range of immunological disorders. Early clinical data suggests that Chelsea's lead antifolate compound, CH-1504, is a safe and effective treatment alternative to methotrexate for RA and may have further applications for psoriasis, IBD and certain cancers. Chelsea's antifolate program is complemented by a strategic partnership with Active Biotech AB for the joint development of a portfolio of therapeutics targeting immune-mediated inflammatory disorders and transplantation. In addition to its autoimmune pipeline, Chelsea is developing Droxidopa, an orally active synthetic precursor of norepinephrine, for the treatment of neurogenic orthostatic hypotension. Currently approved and marketed in Japan, Droxidopa has accumulated over 15 years of proven safety and efficacy, historically generating annual revenues of approximately $50 million in Japan.

This press release contains forward-looking statements regarding future events. These statements are just predictions and are subject to risks and uncertainties that could cause the actual events or results to differ materially. These risks and uncertainties include reliance on collaborations and licenses, risks and costs of drug development, regulatory approvals, intellectual property risks, our reliance on our lead drug candidate CH-1504, our history of losses and need to raise more money, competition, market acceptance for our products if any are approved for marketing, reliance on key personnel including specifically Dr. Pedder, management of rapid growth, and the need to acquire or develop additional products.