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GSK2018682 is a potent and selective small molecule agonist of the sphingosine-1-phosphate receptor 1 (S1P1) and sphingosine-1-phosphate receptor 5 (S1P5), with selectivity over S1P2, S1P3, and S1P4 receptors. It was developed by GSK as an oral agent for the potential treatment of relapsing-remitting multiple sclerosis. The drug acts as an immunomodulator by modulating lymphocyte trafficking through its action on S1P receptors, leading to a dose-dependent reduction in absolute lymphocyte count. Clinical studies have shown that it induces acute, transient decreases in heart rate and blood pressure but is generally tolerated at tested doses. As of now, it remains investigational and has not been approved for any indication.
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