CHARLOTTE, N.C., Nov. 13, 2008 -- Chelsea Therapeutics International, Ltd. (Nasdaq:CHTP) has begun dosing volunteers in the single ascending dose (SAD) study of its Phase I clinical program for CH-4051, the second drug candidate from its portfolio of orally available, non-metabolized antifolates engineered to provide potent anti-inflammatory activity without the liver and kidney toxicities or tolerability related side effects associated with chronic methotrexate (MTX) therapy.
The randomized, double-blind placebo controlled study will evaluate the safety, tolerability and pharmacokinetics of ascending doses of CH-4051 in healthy male volunteers and is being conducted at Kendle International's Clinical Pharmacology Unit in the Netherlands. The SAD study is expected to include 4 cohorts of 6 healthy subjects with a 5:1 randomization. Dose escalation for each cohort will be based on the safety and tolerability data from the previous cohort.
Following the SAD evaluation, the study will progress to a multiple ascending dose (MAD) evaluation and seek to determine a maximum tolerated dose (MTD). Though ultimately dependant on MTD, the MAD study is currently expected to evaluate 4 cohorts of 8 subjects in a 6:2 randomization. Each cohort will be treated for 14 days and dose escalation will be based on the safety and tolerability data from the previous cohort.
"We are excited to advance CH-4051 into clinical studies and further explore the potential of our portfolio of metabolically inert antifolates," commented Dr. Simon Pedder, Chelsea's President and Chief Executive Officer. "We believe there is a significant unmet market need for an effective oral antifolate therapy that can slow disease progression without the liver and kidney toxicity and tolerability issues associated with methotrexate. Based on our preclinical results to date, we believe CH-4051 could expand on the promise demonstrated by our lead antifolate, CH-1504, by broadening our target profile to include a potentially more efficacious treatment alternative to methotrexate while maintaining a highly tolerable safety profile. Together, both compounds represent a compelling development opportunity in this significant market."
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 the development of the I-3D 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.
CONTACT: Chelsea Therapeutics International, Ltd. Nick Riehle, Chief Financial Officer 704-973-4201 Investor/Media Relations Kathryn McNeil 718-788-2856