Cited by 131Sphingolipid Metabolism and SignalingMultiple Sclerosis Research StudiesLysosomal Storage Disorders Research

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Fingolimod: Lessons Learned and New Opportunities for Treating Multiple Sclerosis and Other Disorders

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Chun, Jerold, Kihara, Yasuyuki, Jonnalagadda, Deepa, Blaho, Victoria A.·2019·Annual Review of Pharmacology and Toxicology

DOI 10.1146/annurev-pharmtox-010818-021358PMC PMC6392001

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Abstract

Fingolimod (FTY720, Gilenya) was the first US Food and Drug Administration–approved oral therapy for relapsing forms of multiple sclerosis (MS). Research on modified fungal metabolites converged with basic science studies that had identified lysophospholipid (LP) sphingosine 1-phosphate (S1P) receptors, providing mechanistic insights on fingolimod while validating LP receptors as drug targets. Mechanism of action (MOA) studies identified receptor-mediated processes involving the immune system and the central nervous system (CNS). These dual actions represent a more general theme for S1P and likely other LP receptor modulators. Fingolimod's direct CNS activities likely contribute to its efficacy in MS, with particular relevance to treating progressive disease stages and forms that involve neurodegeneration. The evolving understanding of fingolimod's MOA has provided strategies for developing next-generation compounds with superior attributes, suggesting new ways to target S1P as well as other LP receptor modulators for novel therapeutics in the CNS and other organ systems.

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Authors: Chun, J., Kihara, Y., Jonnalagadda, D., & Blaho, V. A.
Affiliations: Sanford Burnham Prebys Medical Discovery Institute (US)
Corresponding author: Chun, Jerold
ORCID: Chun, Jerold
Kihara, Yasuyuki
Jonnalagadda, Deepa
Blaho, Victoria A.
Venue: Annual Review of Pharmacology and Toxicology
Publisher: Annual Reviews
Published: 2019-01-06
Volume: 59
Issue: 1
Pages: 149-170
ISSN: 0362-1642 (ISSN-L)
1545-4304
DOI: 10.1146/annurev-pharmtox-010818-021358
PMC: PMC6392001
OpenAlex: W2909092545
Cited by: 131
References: 165
Citations by year: 2026: 19 · 2025: 16 · 2024: 13 · 2023: 18 · 2022: 22 · 2021: 12 · 2020: 18 · 2019: 10
FWCI: 1.39
Type: journal article
Language: en
Open access: bronze
doi.org
Locations: The Annual Review of Pharmacology and Toxicology (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
Funders: U.S. Department of Defense (#W81XWH-17, W81XWH1710455, W81XWH)
American Heart Association (16SDG27020014)
National Institutes of Health (W81XWH, NS103940)
National Institute of Neurological Disorders and Stroke (R01NS103940, R01NS084398)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Sphingolipid Metabolism and Signaling
Health Sciences › Medicine › Clinical Neurology › Multiple Sclerosis Research Studies
Health Sciences › Medicine › Genetics (clinical) › Lysosomal Storage Disorders Research
Keywords: fingolimod, multiple sclerosis, sphingosine-1-phosphate receptor, lysophospholipid receptors, mechanism of action, relapsing multiple sclerosis, neurodegeneration, oral therapy, fungal metabolites, CNS drug targets, drug development
MeSH terms: Fingolimod Hydrochloride, Sphingosine-1-Phosphate Receptors, Animals, Central Nervous System, Humans, Lysophospholipids, Multiple Sclerosis

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Fingolimod: Lessons Learned and New Opportunities for Treating Multiple Sclerosis and Other Disorders

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