Department of Gastroenterology, Universidade Federal de São Paulo, São Paulo, Brazil.
IBD Centre, Humanitas Clinical and Research Centre, Milan, Italy.
Expert Opin Biol Ther. 2020 Apr;20(4):413-420. doi: 10.1080/14712598.2020.1732919. Epub 2020 Feb 25.
: Sphingosine-1-phosphate (S1P) is a membrane-derived lysophospholipid signaling molecule implicated in various physiological and pathological processes, such as regulation of the immune, cardiovascular, pulmonary, and nervous systems and theoretical cancer-related risks, through extracellular activation of S1P1-5 receptors.: S1P receptor agonism is a novel strategy for the treatment of UC targeting lymphocyte recirculation, through blockade of lymphocyte egress from lymph nodes. We conducted an extensive literature review on PUBMED on currently available data on molecular aspects of S1P modulation, the mechanisms of action of S1PR agonists (fingolimod, ozanimod, etrasimod, and KRP-203), and their potential efficacy and safety for the treatment of patients with ulcerative colitis.: Selective S1P modulators have emerged to enlarge the efficacy and safety profile of this class of agents. Phase 3 programs should add the potential body of evidence to prove their benefit for the management of UC patients.
鞘氨醇-1-磷酸（S1P）是一种膜衍生的溶血磷脂信号分子，通过细胞外激活 S1P1-5 受体，参与多种生理和病理过程，如免疫系统、心血管系统、肺部和神经系统的调节以及理论上的癌症相关风险。S1P 受体激动剂是一种针对 UC 淋巴细胞再循环的新型治疗策略，通过阻断淋巴细胞从淋巴结中流出。我们在 PUBMED 上进行了广泛的文献综述，以了解目前关于 S1P 调节的分子方面、S1PR 激动剂（ fingolimod、ozanimod、etasimod 和 KRP-203）的作用机制及其在治疗溃疡性结肠炎患者方面的潜在疗效和安全性的可用数据。选择性 S1P 调节剂的出现扩大了此类药物的疗效和安全性特征。3 期计划应增加潜在的证据，以证明它们对 UC 患者管理的益处。
