Relapsing forms of multiple sclerosis (MS) in:
- Adults
Dose: OD 0.5 mg orally
- Pediatric patients ≥10 years of age
Dose: OD 0.25 mg orally
- Includes clinically isolated syndrome (CIS), relapsing-remitting MS (RRMS), and active secondary progressive MS (SPMS)
- Capsules:0.25 mg, 0.5 mg
- Take orally once daily, with or without food
- Do not stop abruptly – may cause severe MS rebound
- Baseline evaluations needed before initiation:
- ECG
- CBC
- Liver function tests (LFTs)
- Ophthalmologic exam
- Varicella zoster antibody titer
- Class: Sphingosine 1-phosphate (S1P) receptor modulator
- Mechanism of Action:
- Binds S1P receptors → traps lymphocytes in lymph nodes → reduces CNS inflammation in MS
- Pharmacokinetics:
- Prodrug, phosphorylated in vivo
- Half-life: 6–9 days
- Metabolism: CYP4F2 (minor via other CYP enzymes)
- Headache
- Fatigue
- Diarrhea
- Back pain
- Cough
- Increased liver enzymes
- Flu-like symptoms
- Recent MI, unstable angina, stroke, TIA, decompensated heart failure
- Second-degree or third-degree AV block, unless paced
- Severe untreated sleep apnea
- Hypersensitivity to fingolimod or components
- Beta-blockers, calcium channel blockers, digoxin – additive bradycardia
- Ketoconazole – ↑ fingolimod levels (CYP inhibition)
- Live vaccines – avoid during and for 2 months after stopping treatment
- Other immunosuppressants – ↑ risk of infections
Drug Status
| Availability | |
| Pregnancy | |
| Breastfeeding | |
| Schedule |
| BRAND NAME | STRENGTH | FORMULATION | PACK SIZE | MANUFACTURER | DISTRIBUTOR |
|---|---|---|---|---|---|
| Gilenya | 0.5mg | Capsule | 28’s | Novartis Pharma | Novartis Kenya |