Drug reference

Fingolimod

Immunosuppressant · Multiple Sclerosis drug

Also known as Gilenya, Fingolimod hydrochloride, FTY720

ImmunosuppressantMultiple Sclerosis drug

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Avoid—toxicity in animal studies.

FDA category + note

Top interactionssee all 12 →

AbarelixSevereDatabaseDDInter
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Mechanism

Fingolimod hydrochloride (FH) is metabolized to fingolimod phosphate, which binds to the sphingosine-1-phosphate (S1P) receptor subtype 1. This action controls the release of lymphocytes from lymph nodes and the thymus, ultimately decreasing circulating lymphocyte numbers in the periphery and central nervous system. S1P receptors are also expressed on neurons, suggesting FH may additionally affect neurodegeneration, gliosis, and endogenous repair mechanisms.

Indications

Highly active relapsing-remitting multiple sclerosis in patients with rapidly-evolving severe relapsing-remitting multiple sclerosis defined by 2 or more disabling relapses in 1 year and with 1 or more gadolinium-enhancing lesions on brain magnetic resonance imaging (MRI) or a significant increase in T2 lesion load compared with a previous recent MRIrelapsing-remitting ms

Dosing

Adult: the dose of either drug. Tizanidine p. 1192 or dantrolene sodium p. 1417 are second-line options; benzodiazepines may be used as third-line therapy and may also be effective in treating nocturnal spasms. A 4-week trial of cannabis extract p. 1190 can be offered as adjunctive treatment for moderate to severe spasticity in multiple sclerosis if other pharmacological treatments are not effective.…

Pharmacokinetics

Metabolism

Primarily by the cytochrome P450 system

Contraindications

Preexisting type II or III heart block
Prolonged QTc
Recent myocardial infarction
Heart failure
fetal risk
cardiac complications preclude use in individuals over the age of 50 and those with history of cardiac disease

Side effects

Common

Macular edemaElevated hepatic enzymesHeadacheDiarrheaCoughincreased risk of infectioncutaneous malignancies

Serious

Cardiac toxicity (bradycardia, prolongation of the QT interval, other abnormalities)
Lymphopenia
first dose effects: bradycardia, decreased atrioventricular conduction, increased qtc interval
vzv antibody testing must be conducted to mitigate risk of disseminated herpes zoster
ms may worsen if withdrawn