The Multiple Sclerosis and Movement Disorders Center at Advance Neurology at Cornerstone Health Care, Winston-Salem, NC 27006, USA.
Expert Rev Neurother. 2011 Feb;11(2):165-83. doi: 10.1586/ern.10.193. Epub 2010 Dec 16.
Fingolimod is the first oral agent approved in the USA for the treatment of relapsing forms of multiple sclerosis. Fingolimod is a sphingosine 1-phosphate receptor modulator that binds to sphingosine 1-phosphate receptors on lymphocytes, resulting in a downregulation of the receptor and a reversible sequestration of lymphocytes in lymphoid tissue. Effector memory T cells are not sequestered so that immune surveillance may be minimally affected. Two large-scale Phase III clinical trials have demonstrated the efficacy of fingolimod compared with placebo and intramuscular interferon β-1a in relapsing-remitting multiple sclerosis. Due to its mechanism of action, fingolimod administration may be associated with first-dose bradycardia and macular edema. Therefore, patients should be observed for 6 h at the time of their first dose and undergo ophthalmologic evaluation prior to treatment initiation and at 3-4 months after initiation.
芬戈莫德是美国批准的首个用于治疗复发型多发性硬化的口服药物。芬戈莫德是一种鞘氨醇 1-磷酸受体调节剂，它与淋巴细胞上的鞘氨醇 1-磷酸受体结合，导致受体下调和淋巴细胞在淋巴组织中的可逆隔离。效应记忆 T 细胞不会被隔离，因此免疫监测可能受到最小影响。两项大规模的 III 期临床试验表明，与安慰剂和肌内注射干扰素 β-1a 相比，芬戈莫德在复发缓解型多发性硬化中的疗效。由于其作用机制，芬戈莫德给药可能与首剂量心动过缓和黄斑水肿有关。因此，患者在首次给药时应观察 6 小时，并在治疗开始前和开始后 3-4 个月进行眼科评估。
