Etrasimod: Modulating Sphingosine-1-Phosphate Receptors to Treat Ulcerative Colitis

Abstract

This review aimed to provide a comprehensive overview of the current landscape of etrasimod. Etrasimod is an oral, once-daily selective modulator of sphingosine 1-phosphate receptors (S1PR), developed for the treatment of moderately to severely active ulcerative colitis and currently being explored for its potential in other immune-mediated inflammatory diseases. It selectively targets the S1PR subtypes S1PR1, S1PR4, and S1PR5, with limited activity on S1PR3 and no activity on S1PR2. Clinical trials have demonstrated that etrasimod significantly reduces symptoms and induces endoscopic improvement in patients with moderate to severe ulcerative colitis who are refractory or intolerant to at least one conventional therapy, biologic agent, or Janus kinase inhibitor, while maintaining a favourable safety profile. At the end of 2023, etrasimod was approved in the United States and Europe, and it is currently under review for ulcerative colitis in several other regions. Etrasimod offers a novel therapeutic option with unique characteristics that may help address the persistent unmet needs of real-world patients with moderately to severely active ulcerative colitis.