Uses

Indicated for the treatment of relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting MS, and active secondary progressive MS, in patients 10 years and older.

Do not use if

Contraindicated in patients who have experienced myocardial infarction, unstable angina, stroke, or TIA in the past 6 months, those with Mobitz type II or third-degree AV block, sick sinus syndrome, severe untreated sleep apnea, or active serious infections.

Side effects

Common adverse effects include bradycardia and AV conduction blocks (first dose), headache, liver enzyme elevations, lymphopenia, diarrhea, and back pain. Serious risks include infections, progressive multifocal leukoencephalopathy (PML), macular edema, and posterior reversible encephalopathy syndrome.

Warnings

Requires first-dose monitoring for at least 6 hours for bradycardia. Complete blood count should be obtained before initiation. Monitor liver function tests. Screen for varicella immunity before starting; vaccination is recommended if non-immune. Avoid live vaccines during and for 2 months after treatment.

How it works

Fingolimod is phosphorylated to its active form fingolimod-phosphate by sphingosine kinase. The active metabolite acts as a functional antagonist at sphingosine 1-phosphate (S1P) receptors 1, 3, 4, and 5, sequestering lymphocytes within lymph nodes and reducing circulating autoreactive lymphocytes that attack the CNS myelin.

Storage

Store at room temperature 15–30°C in the original container. Protect from moisture.