Research Division, Mitsubishi Tanabe Pharma Corporation, Yokohama, Kanagawa, 227-0033, Japan. chiba.kenji@ mk.mt-pharma.co.jp
Future Med Chem. 2012 Apr;4(6):771-81. doi: 10.4155/fmc.12.25.
Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor type 1 (S1P(1)), inhibits lymphocyte egress from secondary lymphoid organs and shows immunomodulating effects. Phase III studies in multiple sclerosis demonstrated that oral FTY720 had superior efficacy compared with intramuscular IFN-β1a (AVONEX(®)) with regard to reducing the rate of relapse and the number of inflammatory lesions in the CNS. FTY720 has been approved as a new therapeutic drug for multiple sclerosis in more than 50 countries, including the USA, Japan and some of those in the EU.
芬戈莫德（FTY720）是一种首创的、口服活性的、鞘氨醇 1-磷酸（S1P）受体调节剂，其结构与鞘氨醇密切相关。该化合物是通过对天然产物——霉酚酸进行化学修饰而发现的。FTY720 的磷酸化形式作为 S1P 受体 1（S1P(1)）的功能拮抗剂，抑制淋巴细胞从次级淋巴器官迁出，并具有免疫调节作用。多发性硬化症的 III 期研究表明，与肌内注射 IFN-β1a（AVONEX(®)）相比，口服 FTY720 能更有效地降低复发率和中枢神经系统炎症病灶数量。FTY720 已在包括美国、日本和一些欧盟国家在内的 50 多个国家被批准为多发性硬化症的新型治疗药物。
