fingolimod

Generic name: Fingolimod/fingolimod

Specification: 0.25mg-28 capsules/bottle (box)

[Indications]

Suitable for the treatment of patients with relapsing multiple sclerosis to reduce the frequency of clinical exacerbations and delay the accumulation of physical disability.

[Dosage]

The recommended dose of fingolimod is 0.5 mg orally once daily. Doses higher than 0.5 mg of fingolimod are associated with a higher incidence of adverse reactions and do not increase benefit. Fingolimod can be taken with or without food.

[Adverse Reactions]

The most common adverse reactions: headache, flu, diarrhea, back pain, elevated liver transaminases and cough.

[Contraindications]

(1) Recent (within the past 6 months): myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or Class III/IV heart failure

(2) Presence or history of Mobitz type II second or third degree AV block or sick sinus syndrome, unless the patient has a pacemaker.

(3) Baseline QTc interval 500 ms

(4) Treatment with Class Ia or Class III antiarrhythmic drugs

[Precautions]

(1) Slowing of heart rate and/or atrioventricular conduction after the first dose of fingolimod: monitor the patient.

(2) Infection: Fingolimod may increase the risk of infection. A recent complete blood count (CBC) should be obtained before initiating treatment with fingolimod. Monitor for signs and symptoms of infection during treatment and for 2 months after discontinuation. Do not initiate fingolimod therapy in patients with active acute or chronic infection.

(3) Macular edema: may occur with or without visual symptoms. An ophthalmological evaluation should be performed before starting fingolimod and 3-4 months after starting treatment. Monitor visual acuity at baseline and at routine patient evaluations. Patients with diabetes mellitus or a history of uveitis are at increased risk and should receive routine ophthalmological evaluation.

(4) Pulmonary function test with fingolimod reduction: Obtain vital capacity and lung diffusion of carbon monoxide when clinically indicated.

(5) Liver effects: Fingolimod may increase liver transaminases. Recent liver enzyme results should be obtained before starting fingolimod. Evaluate liver enzymes if liver injury is suspected. Discontinue fingolimod if significant hepatic injury occurs.

(6) Fetal risk: Women of childbearing potential should use effective contraceptives when taking fingolimod and 2 months after stopping.

[Storage]

Stored at 25ºC (77ºF); allowed to go out to 15-30ºC (59-86ºF). Protected from moisture.

[Mechanism of action]

There are two main mechanisms of action:

One is to promote lymphocytes to migrate back to lymph nodes (away from the central nervous system),

The other is to regulate the S1P receptor of nerve cells.

[Safety and Efficacy]

Further analysis of the FREEDOMS trial found that treatment with fingolimod can reduce inflammation and brain atrophy in patients with multiple sclerosis. Researchers from the FREEDOMS (FTY720 Research Evaluating Effects of Daily Oral Therapy in MS) trial previously reported that fingolimod reduced the rate of disease relapse and the risk of progression to disability compared with placebo. The latest analysis showed that the fingolimod group was able to improve patients' MRI indicators, including brain atrophy (expressed as total brain volume). During the 24 months of the trial, 418 patients treated with placebo experienced a reduction in brain volume of approximately 1.2%; while 854 patients treated with fingolimod, both doses (0.5 or 1.25 mg/day) reduced the reduction in brain volume. Compared with placebo treatment, brain volume reduction at each time point decreased by 22.7% and 44.7% for both doses.