etrasimod

06/22/2021 - "In a phase 2, randomised, double-blind, placebo-controlled trial in adults with moderately-to-severely active ulcerative colitis [OASIS], etrasimod 2 mg provided significant benefit versus placebo and was generally well tolerated. "
04/01/2023 - "Efficacy of Etrasimod on Symptomatic Relief in Patients With Ulcerative Colitis: An Analysis of the Phase 3 ELEVATE UC 52 and ELEVATE UC 12 Trials."
01/01/2023 - "In these two phase 3 trials, we aimed to evaluate the safety and efficacy of etrasimod in adult patients with moderately to severely active ulcerative colitis. "
01/01/2023 - "Recently, etrasimod has demonstrated efficacy in the phase II OASIS study and its open-label extension for the treatment of ulcerative colitis patients. "
06/22/2021 - "Long-term Safety and Efficacy of Etrasimod for Ulcerative Colitis: Results from the Open-label Extension of the OASIS Study."

01/01/2023 - "Etrasimod treatment results in a substantial attenuation of liver injury and inflammation in murine NASH."
01/01/2023 - "Etrasimod helps to control the level of immune cells in the blood, which means that fewer immune cells reach the lining of the colon, reducing inflammation. "
01/01/2019 - "In preclinical pharmacology studies, etrasimod was a full agonist of recombinant human (6.1 nM EC50), mouse (3.65 nM EC50), dog (4.19 nM EC50), and monkey (8.7 nM EC50) S1P1 receptors, and a partial agonist of human S1P4 (147 nM EC50) and S1P5 (24.4 nM EC50), with relative efficacies of 63% and 73% of S1P response, respectively; whereas neither agonist nor antagonist activity was observed for human S1P2 or S1P3 A dose-dependent relationship was observed for etrasimod plasma concentration and lymphocyte count in mice, and chronic treatment with etrasimod resulted in attenuation of inflammation in a CD4+CD45RBhigh T-cell transfer mouse model of colitis."
01/01/2023 - "Consistent with the improvement in liver injury and inflammation, hepatic macrophage accumulation and the gene expression of proinflammatory markers such as Lgals3 and Mcp-1 were decreased in Etrasimod-treated FFC-fed mice. "

06/01/2021 - "Ozanimod and etrasimod have shown promising results in IBD; while in phase 2 clinical trials, ponesimod has shown improvement in 77% of the patients with psoriasis. "

01/01/2019 - "In preclinical pharmacology studies, etrasimod was a full agonist of recombinant human (6.1 nM EC50), mouse (3.65 nM EC50), dog (4.19 nM EC50), and monkey (8.7 nM EC50) S1P1 receptors, and a partial agonist of human S1P4 (147 nM EC50) and S1P5 (24.4 nM EC50), with relative efficacies of 63% and 73% of S1P response, respectively; whereas neither agonist nor antagonist activity was observed for human S1P2 or S1P3 A dose-dependent relationship was observed for etrasimod plasma concentration and lymphocyte count in mice, and chronic treatment with etrasimod resulted in attenuation of inflammation in a CD4+CD45RBhigh T-cell transfer mouse model of colitis."
03/01/2022 - "Der S1P-Rezeptor-Modulator Etrasimod wird aktuell in einer klinischen Phase-3-Studie bei Colitis ulcerosa getestet und der selektive JAK-1-Inhibitor Upadacitinib dürfte nächstes Jahr bei Colitis ulcerosa zugelassen werden. "
01/01/2019 - "The Selective Sphingosine 1-Phosphate Receptor Modulator Etrasimod Regulates Lymphocyte Trafficking and Alleviates Experimental Colitis."

01/05/2024 - "Taken together, our study highlights the value of etrasimod and its derivatives as potential antibacterial candidates for combating infections caused by Gram-positive bacteria."