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Fingolimod

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Also known as FTY-720GilenyaFingolimod hydrochlorideÊFingolimod hydrochlorideÂFingolimod (FTY720) HClFingolimod

Summary

Fingolimod (CHEMBL314854) is an approved small-molecule immunosuppressive agent (ATC L04AE01) targeting S1PR1, S1PR5, and KCNJ5; indicated across 17 conditions including chronic progressive multiple sclerosis and relapsing-remitting multiple sclerosis.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L04AE01
  • Targets: 4 (S1PR1, S1PR5, KCNJ5…)
  • Indications: 17 conditions
  • Clinical trials: 75
  • Chemistry: 307.5 Da · C19H33NO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL314854
NameFingolimod
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID107970
ChEBICHEBI:63115
ATCL04AE01
Molecular formulaC19H33NO2
Molecular weight307.5
InChIKeyKKGQTZUTZRNORY-UHFFFAOYSA-N

SMILES: CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N

IUPAC name: 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol

ChEBI definition: An aminodiol that consists of propane-1,3-diol having amino and 2-(4-octylphenyl)ethyl substituents at the 2-position. It is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis. A prodrug, fingolimod is phosphorylated by sphingosine kinase to active metabolite fingolimod-phosphate, a structural analogue of sphingosine 1-phosphate.

Pharmacological roles (ChEBI): immunosuppressive agent, prodrug, antineoplastic agent, sphingosine-1-phosphate receptor agonist, CB1 receptor antagonist.

Also known as: Fingolimod, FTY-720, fingolimod, FINGOLIMOD, Gilenya, Fingolimod hydrochlorideÊ, Fingolimod hydrochlorideÂ, Fingolimod (FTY720) HCl, Fingolimod; Gilenya

Parent form; salt/anhydrous children: CHEMBL544665, CHEMBL3526818, CHEMBL5095050

Patent coverage: 4,423 distinct patent families (16,015 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
S1PR1S1P1 receptorAgonist6.080.2%P21453
S1PR5S1P5 receptorAgonist5.680%Q9H228
KCNJ5Kir3.4Agonist0%P48544
TRPM7TRPM7Inhibition6.1462.2%Q96QT4

Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: Troponin C, slow skeletal and cardiac muscles, Sphingosine 1-phosphate receptor 5, Sphingosine 1-phosphate receptor 4, G-protein coupled receptor 183, Sphingosine-1-phosphate lyase 1, Transient receptor potential cation channel subfamily M member 7, Sphingosine 1-phosphate receptor 3, Sphingosine 1-phosphate receptor 1, Sphingosine-1-phosphate lyase 1, Ceramide synthase 2.

Bioactivity

ChEMBL activities: 19 potent at pChembl ≥ 5 of 23 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
S1PR59.52EC500.3nMCHEMBL_ACT_13828999
S1PR49.52EC500.3nMCHEMBL_ACT_13829000
S1PR19.52EC500.3nMCHEMBL_ACT_13829002
S1PR18.7EC502nMCHEMBL_ACT_8012213
S1PR38.52EC503nMCHEMBL_ACT_13829001
S1PR18.14EC507.2nMCHEMBL_ACT_16449672
S1PR17.2EC5062.65nMCHEMBL_ACT_25751498
S1PR16.22IC50603.8nMCHEMBL_ACT_24868303
Q923J16.14IC50720nMCHEMBL_ACT_25716662
S1PR16.1EC50794.3nMCHEMBL_ACT_25708623
S1PR16.08IC50840nMCHEMBL_ACT_1841862
S1PR55.68IC502100nMCHEMBL_ACT_1841902
CERS25.67Ki2150nMCHEMBL_ACT_24982861
S1PR35.6EC502512nMCHEMBL_ACT_18479391
S1PR55.5EC503162nMCHEMBL_ACT_18479453
GPR1835.38IC504219nMCHEMBL_ACT_25751497
TNNC15.3Kd5000nMCHEMBL_ACT_25551934
TNNC15.21Kd6200nMCHEMBL_ACT_25551940
CERS25.19IC506400nMCHEMBL_ACT_24982860

Target pathways

Aggregated over 4 target gene(s): S1PR1, S1PR5, KCNJ5, TRPM7.

Top Reactome pathways

28 total, by targets touching each:

PathwayTargetsGenes
Signal Transduction2S1PR1, S1PR5
Signaling by GPCR2S1PR1, S1PR5
Class A/1 (Rhodopsin-like receptors)2S1PR1, S1PR5
Lysosphingolipid and LPA receptors2S1PR1, S1PR5
GPCR ligand binding2S1PR1, S1PR5
Neurotransmitter receptors and postsynaptic signal transmission1KCNJ5
Transmission across Chemical Synapses1KCNJ5
Neuronal System1KCNJ5
Cytokine Signaling in Immune system1S1PR1
Activation of G protein gated Potassium channels1KCNJ5
G protein gated Potassium channels1KCNJ5
Inwardly rectifying K+ channels1KCNJ5
Potassium Channels1KCNJ5
Disease1S1PR1
Immune System1S1PR1
TRP channels1TRPM7
GPCR downstream signalling1S1PR5
G alpha (i) signalling events1S1PR5
Signaling by Interleukins1S1PR1
Infectious disease1S1PR1
Interleukin-4 and Interleukin-13 signaling1S1PR1
Potential therapeutics for SARS1S1PR1
SARS-CoV Infections1S1PR1
GABA receptor activation1KCNJ5
GABA B receptor activation1KCNJ5
Viral Infection Pathways1S1PR1
Activation of GABAB receptors1KCNJ5
Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits1KCNJ5

Dominant GO biological processes

GO termTargets
sphingosine-1-phosphate receptor signaling pathway2
G protein-coupled receptor signaling pathway2
adenylate cyclase-activating G protein-coupled receptor signaling pathway2
signal transduction2
monoatomic ion transport2
monoatomic ion transmembrane transport2
monoatomic cation transmembrane transport2
angiogenesis1
blood vessel maturation1
cardiac muscle tissue growth involved in heart morphogenesis1
chemotaxis1
cell adhesion1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway1
phospholipase C-activating G protein-coupled receptor signaling pathway1
brain development1

Indications & clinical

Indications

17 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
chronic progressive multiple sclerosis3MONDO:0005284EFO:0003840
relapsing-remitting multiple sclerosis3MONDO:0005314EFO:0003929
chronic inflammatory demyelinating polyradiculoneuropathy3MONDO:0006702EFO:1000868
primary progressive multiple sclerosis3MONDO:0000451EFO:0008520
multiple sclerosis3MONDO:0005301MONDO:0005301
stroke disorder2MONDO:0005098EFO:0000712
uveitis2MONDO:0020283EFO:1001231
optic neuritis2MONDO:0005885EFO:0007405
severe acute respiratory syndrome2MONDO:0005091MONDO:0100096
asthma2MONDO:0004979MONDO:0004979
breast carcinoma1MONDO:0004989EFO:0000305
kidney failure1MONDO:0001106HP:0000083
Rett syndrome1MONDO:0010726MONDO:0010726
intracerebral hemorrhage1MONDO:0013792EFO:0005669
glioblastoma0MONDO:0018177EFO:0000519
anaplastic astrocytoma0MONDO:0016684EFO:0002499

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 75.

Phase distribution

PhaseTrials
PHASE425
PHASE316
Not specified12
PHASE211
PHASE14
EARLY_PHASE13
PHASE2/PHASE32
PHASE1/PHASE22

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04480853PHASE4RECRUITINGSafety and Efficacy Study of Fingolimod in Taiwanese Adults (≥ 20years) With Relapsing Remitting Multiple Sclerosis
NCT05307731PHASE4RECRUITINGFingolimod for Type 2 Diabetes Mellitus
NCT01216072PHASE4COMPLETEDA 6-month, Randomized, Open-label, Patient OutComes, Safety and Tolerability Study of Fingolimod (FTY720) 0.5 mg/Day vs. Comparator in Patients With Relapsing Forms of Multiple Sclerosis
NCT01310166PHASE4COMPLETEDBiomarker Study After Initiation of Treatment With Fingolimod (FTY720) in Patients With Relapsing-remitting Multiple Sclerosis
NCT01317004PHASE4COMPLETEDPatients With Relapse Remitting Multiple Sclerosis (RRMS): Candidates for MS Therapy Change
NCT01333501PHASE4COMPLETEDFingolimod Versus Interferon Beta 1b in Cognitive Symptoms
NCT01420055PHASE4COMPLETEDFingolimod -Response According to Coping - Evaluation
NCT01436643PHASE4TERMINATEDCombination of Antidepressants and Fingolimod Relapsing-remitting Multiple Sclerosis (RRMS) Patients With Depression
NCT01498887PHASE4COMPLETEDEfficacy of Fingolimod in de Novo Patients Versus Fingolimod in Patients Previously Treated With a First Line Disease Modifying Therapy
NCT01534182PHASE4COMPLETEDEvaluation of Patient Reported Outcomes in RRMS Patients Candidates for MS Therapy Change and Transitioned to Fingolimod 0.5 mg (EPOC)
NCT01578330PHASE4COMPLETEDA 12 -Month, Open-label, Multi-center Study to Explore the Health Outcomes of FTY720
NCT01621269PHASE4WITHDRAWNENGYNE Exploring Gilenya in Patients With Neutralizing Antibodies Against Interferon
NCT01623596PHASE4COMPLETEDEvaluation of Patient Retention of Fingolimod vs. Currently Approved Disease Modifying Therapy in Patients With Relapsing Remitting Multiple Sclerosis.
NCT01705236PHASE4COMPLETEDA 3-year Multi-center Study to Describe Changes of OCT Parameters Under Treatment With Gilenya®
NCT01755871PHASE4TERMINATEDLong-term Effect of Fingolimod on Circulating Immunocompetent Mononuclear Cells in Patients With Multiple Sclerosis
NCT02048072PHASE4COMPLETEDEvaluation of the Autonomic Nervous System During First-dosing With 0.5mg of Fingolimod (Gilenya) in Patients With Relapsing-remitting MS
NCT02232061PHASE4COMPLETEDLong-term, Open-label, Multicenter Study Assessing Long-term Cardiovascular Risks
NCT02325440PHASE4UNKNOWNStudy to Assess Immune Function and MRI Disease Activity in RRMS Patients When Switching From Natalizumab to Gilenya
NCT02342704PHASE4TERMINATEDImpact of Natalizumab Versus Fingolimod in Relapsing-Remitting Multiple Sclerosis (RRMS) Participants
NCT02373098PHASE4COMPLETEDFingolimod Effect on Cytokine and Chemokine Levels
NCT02575365PHASE4TERMINATEDEffect of Fingolimod on Neurodegeneration
NCT02720107PHASE4COMPLETEDFollow up Study of Patients on Fingolimod Who Were Enrolled in the Original Biobank Study (CFTY720DDE01)
NCT03257358PHASE4COMPLETEDA Study of Immune Phenotype Biomarkers in Patients With Relapsing Multiple Sclerosis (RMS) After Treatment With 0.5mg Fingolimod
NCT03345940PHASE4TERMINATEDFingolimod Versus Dimethyl-fumarate in Multiple Sclerosis
NCT04667949PHASE4COMPLETEDStudy of Efficacy and Safety of Fingolimod (Gilenya) 0.5 mg in Chinese Patients With Relapsing Multiple Sclerosis (RMS) Patients
NCT01892722PHASE3ACTIVE_NOT_RECRUITINGSafety and Efficacy of Fingolimod in Pediatric Patients With Multiple Sclerosis
NCT04926818PHASE3ACTIVE_NOT_RECRUITINGEfficacy and Safety of Ofatumumab and Siponimod Compared to Fingolimod in Pediatric Patients With Multiple Sclerosis
NCT05123703PHASE3ACTIVE_NOT_RECRUITINGA Study to Evaluate Safety and Efficacy of Ocrelizumab in Comparison With Fingolimod in Children and Adolescents With Relapsing-Remitting Multiple Sclerosis (RRMS)
NCT06408259PHASE3RECRUITINGStudy to Evaluate the Effectiveness and Safety of Ozanimod Compared to Fingolimod in Children and Adolescents With Relapsing Remitting Multiple Sclerosis
NCT07220252PHASE2/PHASE3NOT_YET_RECRUITINGStudy to Assess Effects of Ublituximab in Pediatric Participants With Relapsing Forms of Multiple Sclerosis
NCT07483632PHASE3NOT_YET_RECRUITINGA Study to Learn About the Safety of Diroximel Fumarate (DRF) and Dimethyl Fumarate (DMF) and Their Effects on Relapses in Pediatric Participants With Relapsing Forms of Multiple Sclerosis (RMS)
NCT00289978PHASE3COMPLETEDEfficacy and Safety of Fingolimod in Patients With Relapsing-remitting Multiple Sclerosis
NCT00340834PHASE3COMPLETEDEfficacy and Safety of Fingolimod in Patients With Relapsing-remitting Multiple Sclerosis With Optional Extension Phase
NCT00355134PHASE3COMPLETEDEfficacy and Safety of Fingolimod (FTY720) in Patients With Relapsing-remitting Multiple Sclerosis
NCT00662649PHASE3COMPLETEDLong-term Efficacy and Safety of Fingolimod (FTY720) in Patients With Relapsing-remitting Multiple Sclerosis
NCT01199861PHASE3COMPLETEDEffect of Treatment With Fingolimod on the Immune Response Following Seasonal Flu Vaccination and Tetanus Booster Injection in Patients With Relapsing Multiple Sclerosis (MS)
NCT01201356PHASE3COMPLETEDLong-term Safety and Tolerability of 0.5 mg Fingolimod in Patients With Relapsing Forms of Multiple Sclerosis
NCT01497262PHASE3COMPLETEDSafety and Tolerability of Fingolimod in Patients With Relapsing-remitting Multiple Sclerosis
NCT01499667PHASE3TERMINATEDDisease Control and Safety in Patients With Relapsing Remitting Multiple Sclerosis (RRMS) Switching From Natalizumab to Fingolimod
NCT01625182PHASE3COMPLETEDEvaluate Efficacy and Safety of Fingolimod 0.5 mg Orally Once Daily Versus Placebo in Chronic Inflammatory Demyelinating Polyradiculoneuropathy Patients.

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

15 molecules share ≥1 primary target. Top 15 by shared-target count:

MoleculeSourceStatusShared targets
ETRASIMODChEMBL + PubChemPhase 4 (approved)S1PR1, S1PR5
OZANIMODChEMBL + PubChemPhase 4 (approved)S1PR1, S1PR5
SIPONIMODChEMBL + PubChemPhase 4 (approved)S1PR1, S1PR5
PONESIMODChEMBLPhase 4 (approved)S1PR1
CENERIMODChEMBLPhase 3S1PR1
AMISELIMODChEMBLPhase 2S1PR1
ICANBELIMODChEMBLPhase 2S1PR1
NIGULDIPINEChEMBLPhase 2S1PR1
PINAFIDEChEMBLPhase 2S1PR1
AlosetronPubChemApprovedKCNJ5
glyburidePubChemApprovedKCNJ5
ImipraminePubChemApprovedKCNJ5
MefloquinePubChemApprovedKCNJ5
PropafenonePubChemApprovedKCNJ5
SildenafilPubChemApprovedKCNJ5

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot