About Actelion’s S1P1 Receptor Agonist program

Actelion has selected novel small molecules for clinical development on the basis of their S1P1 receptor selectivity. They also have high potency and a favorable pharmacokinetic profile after oral dosing, resulting in a substantial and rapidly reversible depletion of circulating lymphocytes. They are effective in animal models of T-cell mediated inflammation.

Actelion's S1P1 receptor agonists are potential therapeutic agents for immune disorders in which activated T cells play a critical role. In these pathological situations, traditional immunosuppressants have a high potential for toxicity, slow reversibility, and may increase the risk of infection or malignancy.

Current Status

Actelion and Roche entered into an exclusive worldwide collaboration in July 2006 to jointly develop and commercialize Actelion’s selective S1P1 receptor agonist, as an immunomodulator with the potential for once-a-day oral dosing for multiple autoimmune disorders.

Phase I safety and tolerability testing is ongoing.