April 28, 2009 (FinancialWire) — Data from Chelsea Therapeutics International’s (NASDAQ: CHTP) Phase I dosing trial of CH-4051, the L-isomer of CH-1504, shows it is tolerable up to a dose of 7.5mg in healthy male volunteers. The randomized, double-blind, placebo-controlled study was conducted at Kendle International’s Clinical Pharmacology Unit in the Netherlands.

Chelsea said the drug shows promise for use in multiple autoimmune disorders.

The single ascending dose phase of the study evaluated 5mg, 10mg, 20mg and 40mg doses of CH-4051. Each group contained six volunteers randomized 5:1 to receive either CH-4051 or placebo. In this escalating dose study, each cohort of subjects received a higher dose of the drug than the preceding cohort.

Based on the findings, Chelsea selected 5mg, 7.5mg, 10mg and 20mg of CH-4051 for evaluation in a multiple ascending dose (MAD) study with the objective of exploring a wide range of doses, including and exceeding those believed to be therapeutically relevant. In the MAD study, 32 subjects in four cohorts of eight volunteers were randomized 6:2 to receive repeat daily oral doses of CH-4051 or placebo for 14 consecutive days.

Results demonstrated that CH-4051 was well tolerated at doses up to and including 7.5mg, a dose range likely to be effective. The 5mg dose was as well tolerated as placebo. High doses demonstrated mostly mild toxicities, with the 10mg and 20mg doses groups reporting both gastrointestinal side-effects and reversible liver enzyme elevations. No serious adverse events occurred during the study.

The dose range determined to be safe and well tolerated in this study is substantially higher than the 0.25mg to 1.0mg dose range of CH-1504 that demonstrated comparable efficacy and improved safety and tolerability to methotrexate in a recent Phase II rheumatoid arthritis trial.

Consistent with preclinical findings to date, a comparison of data from this study and the results of prior Phase I evaluations of CH-1504 suggests that CH-4051 has improved absorption with an approximately two-fold improvement in bioavailability compared to CH-1504, yet is better tolerated on the basis of both its dose to side-effect profile and plasma concentration to side-effect profile.

Dr. Simon Pedder, Chelsea’s president and chief executive officer, said, “Having recently demonstrated proof-of-concept with our first antifolate, CH-1504, in rheumatoid arthritis, we are particularly pleased to see the results from this trial further support the potential of CH-4051 to be an equally well tolerated drug candidate at doses up to 7.5mg.”

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