Therapeutic Potential of Etrasimod in the Management of Moderately-to-Severely Active Ulcerative Colitis: Evidence to Date

Abstract

Etrasimod is a sphingosine 1 phosphate (S1P) receptor modulator approved for the treatment of moderate to severely active ulcerative colitis (UC). Etrasimod selectively activates S1P_1,4,5 receptors with no detectable activity on S1P_2,3. The ELEVATE clinical trials evaluated the efficacy and safety of etrasimod for UC. Etrasimod showed clinically significant improvement in clinical remission at weeks 12 and 52 compared to placebo. Etrasimod showed greater efficacy in patients who were biologic naive. Etrasimod was also effective in a subgroup of patients with isolated proctitis. The medication should be avoided in pregnancy and lactation, certain cardiac conditions including brady-arrythmias, and those with a history of skin cancer. Etrasimod has a shorter half-life and fewer drug-drug and food interactions as compared to the S1P receptor modulator ozanimod. In addition, no dosing titration is required. Etrasimod is a promising treatment option for UC patients with moderate to severe inflammation, particularly those who have no prior biologic exposure, are not considering pregnancy, and prefer oral therapy.

Keywords: etrasimod; inflammation; small molecule; sphingosine 1 phosphate modulator; ulcerative colitis.

Figure 1

Mechanism of action of etrasimod: Etrasimod works on the sphingosine-1 phosphate receptors that prevent the migration of T cells from lymph nodes to reduce their trafficking to inflammation sites in the colon in ulcerative colitis.