Gilenya: first oral treatment for multiple sclerosis

Gilenya (fingolimod) is a novel drug indicated in the treatment of relapsing-remitting multiple sclerosis (MS) with high disease activity despite treatment with interferon beta or rapidly evolving severe relapsing-remitting MS.

Gilenya: a new option for MS
Gilenya: a new option for MS

Gilenya (fingolimod) is a sphingosine 1-phosphate receptor modulator that is metabolised by sphingosine kinase to the active metabolite fingolimod phosphate. This binds at low nanomolar concentrations to sphingosine 1-phosphate (S1P) receptor 1 on lymphocytes, thereby preventing their release from lymph nodes. This causes a redistribution, rather than depletion, of lymphocytes, which in turn reduces the infiltration of pathogenic lymphocyte cells into the central nervous system (CNS), where they would be involved in nerve inflammation and nervous tissue damage.1 Preclinical findings suggest that fingolimod may also promote neuroprotective and reparative processes in the CNS via interaction with S1P receptors on neural cells.2,3

The superior efficacy of fingolimod compared with placebo and intramuscular interferon beta-1a was demonstrated in 2 randomised controlled trials involving 2564 patients with relapsing-remitting multiple sclerosis. Patients were aged 18 to 55 years with 1 or more relapses in the previous year or 2 or more in the previous 2 years and a score of 0 to 5.5 on the Expanded Disability Status Scale (EDSS).

In the FREEDOMS study (n=1272), patients were randomised to receive oral fingolimod 500 microgram or 1.25mg or placebo once daily for 24 months.2 The annual relapse rate (defined as number of confirmed relapses per year) over 24 months was significantly lower in the fingolimod groups (0.18 and 0.16 in the 500 microgram and 1.25mg groups, respectively, versus 0.40 for placebo [p<0.001 for both comparisons]). More than two thirds of patients in the fingolimod 500 microgram and 1.25mg groups remained relapse-free at 24 months compared with less than half of patients in the placebo group (70.4 and 74.7%, respectively, versus 45.6% [p<0.001 for both comparisons]).

In addition, the risk of disability progression over 24 months was significantly reduced in the fingolimod groups (cumulative probability [1-point increase in EDSS confirmed after three months] 17.7% and 16.6% for the 500 microgram and 1.25mg groups, respectively, versus 24.1% for placebo). Fingolimod treatment was also associated with improved MRI-related measures compared with placebo (p<0.001 for all comparisons at 24 months).

In the double-blind, double-dummy TRANSFORMS study (n=1292), patients were randomised to receive oral fingolimod 500 microgram or 1.25mg once daily or intramuscular interferon beta-1a 30 microgram once weekly for 12 months.3 A significantly lower annual relapse rate was observed in the fingolimod groups compared with interferon beta-1a (0.16 and 0.20 in the 500 microgram and 1.25mg groups, respectively, versus 0.33 [p<0.001 for both comparisons]).

Fingolimod was also associated with a greater reduction in lesion activity and brain volume loss than interferon beta-1a. The progression of disability did not significantly differ between the three groups.

Adverse events associated with fingolimod 500 microgram daily in the two studies were similar, taking into account the differences in study duration. The most serious reactions reported were infections, macular oedema and transient atrioventricular block at treatment initiation.1 The most frequently reported adverse events (≥10%) with fingolimod 500 microgram daily were headache, influenza, diarrhoea, back pain, raised liver enzymes and cough.1 In the study using interferon beta-1a as the comparator, the incidence of adverse events was similar in the three treatment groups.3


  1. Gilenya Summary of Product Characteristics, March 2011.
  2. Kappos L et al. N Engl J Med 2010; 362: 387–401.
  3. Cohen J et al. N Engl J Med 2010; 362: 402–15.

View Gilenya drug record

Further Information: Novartis

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