Oral fingolimod for the treatment of relapsing-remitting multiple sclerosis.
The sphingosine-1-phosphate receptor modulator fingolimod (FTY-720), which acts by preventing lymphocyte egress from lymph nodes thus reducing lymphocyte infiltration into the central nervous system (CNS), represents a novel therapeutic modality for the treatment of multiple sclerosis (MS). Results obtained from preclinical studies have also attributed a potential neuroprotective and reparative function to the agent within the CNS. Clinical evaluation in placebo-controlled trials in healthy individuals and MS patients revealed favorable safety and superior efficacy. Fingolimod was also reported to exhibit superiority, with respect to relapse rates and magnetic resonance imaging (MRI) outcomes, compared with the established MS therapeutic interferon beta-1a (IFN-beta-1a) in patients with relapsing-remitting MS in a 12-month clinical study. The oral route of administration of fingolimod renders it a more convenient therapeutic option than intramuscular IFN-beta-1a, while its lipophilicity which permits ready crossing of the blood-brain-barrier may result in enhanced activity. The positive risk-to-benefit profile of the agent supports the once-daily administration regimen for the treatment of MS.
Thomson Reuters, Barcelona, Spain. sylvia.vasiliou@thomsonreuters.com
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D000284:Administration, Oral; D000818:Animals; D002986:Clinical Trials as Topic; D004347:Drug Interactions; D000068876:Fingolimod Hydrochloride; D006801:Humans; D007166:Immunosuppressive Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D007654:Ketoconazole / Q000494:pharmacology; D020529:Multiple Sclerosis, Relapsing-Remitting / Q000188:drug therapy* / Q000503:physiopathology; D011409:Propylene Glycols / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D049349:Receptors, Lysosphingolipid / Q000187:drug effects / Q000378:metabolism; D013110:Sphingosine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use
D007166:Immunosuppressive Agents; D011409:Propylene Glycols; D049349:Receptors, Lysosphingolipid; D000068876:Fingolimod Hydrochloride; D013110:Sphingosine; D007654:Ketoconazole