Product Information
Registration Status: ActiveGILENYA CAPSULE 0.5MG is approved to be sold in Singapore with effective from 2012-05-30. It is marketed by NOVARTIS (SINGAPORE) PTE LTD, with the registration number of SIN14153P.
This product contains Fingolimod 0.5mg in the form of CAPSULE. It is approved for ORAL use.
This product is manufactured by Novartis Pharma Stein AG in SWITZERLAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Fingolimod is a sphingosine 1-phosphate receptor modulator indicated and approved for the treatment of relapsing-remitting multiple sclerosis.
Indication
Fingolimod is a sphingosine 1-phosphate receptor modulator indicated for the treatment of patients with relapsing forms of multiple sclerosis to reduce the frequency of clinical exacerbations and to delay the accumulation of physical disability.
Mechanism of Action
Fingolimod is metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate. Fingolimod-phosphate is a sphingosine 1-phosphate receptor modulator, and binds with high affinity to sphingosine 1-phosphate receptors 1, 3, 4, and 5. Fingolimod-phosphate blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which fingolimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system.
Pharmacokinetics
- Absorption
- The Tmax of fingolimod is 12-16 hours. Bioavailability: 93%
- Distribution
- about 1200±260 L.
- Metabolism
- 3 main pathways: -reversible stereoselective phosphorylation to the pharmacologically active (S)-enantiomer of fingolimod-phosphate. -oxidative biotransformation mainly via the cytochrome P450 4F2 isoenzyme and subsequent fatty acid-like degradation to inactive metabolites. -by formation of pharmacologically inactive non-polar ceramide analogs of fingolimod.
- Elimination
Clearance
Fingolimod blood clearance is 6.3±2.3 L/h.
Toxicity
Bradyarrhythmia and Atrioventricular Blocks Risk of infections Macular Edema Respiratory Effects Hepatic Effects Fetal Risk Blood Pressure Effects Immune System Effects Following Fingolimod Discontinuation
Active Ingredient/Synonyms
Fingolimodum | Fingolimod |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.