瑞士制药商诺华公司(NVS)表示，美国食品与药品管理局(FDA)已批准其生产的Gilenya作为一款口服药物治疗复发型多发性硬化症。
芬戈莫德（Fingolimod）是由日本Mitsubishi制药公司研发， 后期全球经营权转让给瑞士Novartis制药公司， 2010 年9月21日获得美国FDA批准上市, 成为首个可经口服给药的用于治疗复发缓解型多发性硬化症(multiplesclerosis，MS)的新型免疫抑制剂，商品名为：Gilenya.可以阻止淋巴腺中的部分血细胞向大脑和脊髓移动，从而延缓多发性硬化症患者的病情恶化程度。
目前用于多发性硬化症的主要药物为：那他珠单抗、β-干扰素、盐酸米托蒽醌、格拉默等，但是这些药物多采用长时程的肠道外给药模式，既增加了患者的负担，又减少了药物应用的依从性。并且不能长效抑制病情，必需频繁注射给药，还会引发一些副作用，如流感样副作用及注射部位炎症反应等。
作用机制
一是促使淋巴细胞回迁至淋巴结（远离中枢神经系统）
二是调节神经细胞的S1P受体。
芬戈莫德为首个防止淋巴细胞从淋巴结中离开的鞘氨醇1-磷酸盐受体调节剂类药，降低多发性硬化症患者疾病复发的频率，延缓多发性硬化症患者的病情恶化程度。它还可以保持淋巴结内特定的免疫细胞，防止它们作用于中枢神经系统并造成损害，并且对淋巴细胞的保持力是可逆的，从而使患者在治疗停止后体内循环的淋巴细胞恢复到正常水平。
Gilenya（芬戈莫德胶囊)用于多发性硬化症说明书[附件:/uploadfile/article/uploadfile/201009/20100923032707119.pdf]
Manufacturer:
Novartis Pharmaceuticals Corp

Pharmacological Class:
Sphingosine 1-phosphate ­receptor modulator.

Active Ingredient(s):
Fingolimod (as HCl) 0.5mg; caps.
Indication(s):
For relapsing forms of multiple sclerosis (MS): to reduce the frequency of clinical exacerbations and to delay the accumulation of physical disability.

Pharmacology:
Fingolimod blocks lymphocytes from leaving lymph nodes, reducing the numbers of circulating lymphocytes. The exact mechanism for its ­effects on MS is not known, but it may involve the reduction of lymphocyte migration in the CNS.

Clinical Trials:
Two studies were conducted to assess the safety and efficacy of fingolimod in treating ­patients with relapsing remitting MS. Study 1 was a placebo-controlled study in patients who had not ­received ­interferon-beta or glatiramer acetate for at least the previous 3 months and had not received ­natalizumab for at least the previous 6 months. The primary endpoint was the annualized relapse rate. At randomization, patients had an Expanded Disability Status Score (EDSS) ranging from 0–5.5 (median 2.0). Patients given fingolimod 0.5mg daily had an annualized response rate of 0.18, compared to 0.4 for those given placebo. Seventy ­percent of patients in the fingolimod 0.5mg group were relapse-free, compared to 46% for placebo. The 1.25mg dose did not show any additional benefit.

Study 2 was a double-dummy, active-controlled study in patients who had not received any natalizumab in the previous 6 months; prior therapy with glatiramer acetate or interferon-beta was permitted up to the time of randomization. The median baseline EDSS score was 2.0. Patients were randomized to fingolimod 0.5mg/day, fingolimod 1.25mg/day, or interferon ­beta-1a 30mcg IM once weekly for up to 12 months. The annualized relapse rate for patients given fingolimod 0.5mg/day was 0.16, compared to 0.33 for those given interferon. Eighty-three percent of those on fingolimod 0.5mg were relapse-free, compared to 70% of those on interferon. There was no additional benefit seen with fingolimod dosed at 1.25mg daily. A secondary endpoint, the number of new or enlarging T2 lesions seen on MRI, showed an advantage for fingolimod as well.
Legal Classification:
Rx

Adults:
≥18years: 0.5mg once daily. Monitor 1st dose (6 hours).

Children:
<18years: not recommended.

Warnings/Precautions:
Active acute or chronic ­infection: do not start treatment until infection ­resolved. Obtain recent CBC before starting treatment. Consider suspending therapy if serious infection ­develops; monitor for infections during treatment and for 2 months after discontinuation. Test for antibodies to varicella zoster virus; consider immunization before starting fingolimod. Immunosuppressed. Cardiac risk factors: monitor for bradycardia for 6 hours after 1st dose; consider baseline ECG. Bradycardia (<55bpm). History of syncope. Sick ­sinus syndrome. 2nd or 3rd degree heart block. Cardiac ischemia. CHF. QT prolongation. Arrhythmias. Diabetes, history of uveitis: increased risk of macular edema. Monitor visual acuity and for visual disturbances. Do ophthalmic exam at baseline, and at 3–4 months after starting therapy. Recent LFTs (eg, within 6 months) should be available; monitor; discontinue if liver injury occurs. Respiratory dysfunc­tion. Renal or severe hepatic ­impairment. Pregnancy (Cat.C) (use effective contraception ­during and for 2 months after discontinuation), nursing mothers: not recommended.

Interaction(s):
Potentiated by ketoconazole. Class Ia (eg, quinidine, procainamide) or Class III anti­arrhythmics (eg, amiodarone, sotalol), β-blockers, calcium channel blockers: increased risk of bradycardia. Avoid live virus vaccines during treatment and for 2 months after discontinuing fingolimod; may have suboptimal response. Caution with antineo­plastic, immunosuppressant or immunomodulating therapies: increased risk of immunosuppression.

Adverse Reaction(s):
Headache, influenza, diarrhea, back pain, increased liver transaminases, cough, ­hypertension; transient decreased heart rate and AV conduction, increased infection risk, macular edema, decreased pulmonary function.
How Supplied:
Caps—7, 28