Identification

Name
Fingolimod
Accession Number
DB08868
Type
Small Molecule
Groups
Approved, Investigational
Description

Fingolimod is a sphingosine 1-phosphate receptor modulator indicated and approved for the treatment of relapsing-remitting multiple sclerosis.

Structure
Thumb
Synonyms
  • Fingolimodum
External IDs
FTY-720A / FTY720
Product Ingredients
IngredientUNIICASInChI Key
Fingolimod HydrochlorideG926EC510T162359-56-0SWZTYAVBMYWFGS-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
GilenyaCapsule0.5 mgOralNovartis2011-03-28Not applicableCanada
GilenyaCapsule0.5 mgOralNovartis Europharm Limited2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Limited2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Limited2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Limited2011-03-17Not applicableEu
GilenyaCapsule.5 mg/1OralNovartis2010-09-21Not applicableUs
GilenyaCapsule0.5 mgOralNovartis Europharm Limited2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Limited2011-03-17Not applicableEu
International/Other Brands
Gilenia
Categories
UNII
3QN8BYN5QF
CAS number
162359-55-9
Weight
Average: 307.4708
Monoisotopic: 307.251129305
Chemical Formula
C19H33NO2
InChI Key
KKGQTZUTZRNORY-UHFFFAOYSA-N
InChI
InChI=1S/C19H33NO2/c1-2-3-4-5-6-7-8-17-9-11-18(12-10-17)13-14-19(20,15-21)16-22/h9-12,21-22H,2-8,13-16,20H2,1H3
IUPAC Name
2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol
SMILES
CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1

Pharmacology

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.

Structured Indications
Pharmacodynamics

Fingolimod causes a transient reduction in heart rate and AV conduction at treatment initiation. Potential to prolong the QT interval. Effects on immune cell numbers in the blood- decreased lymphocyte counts. Mild decrease in the neutrophil count- about 80% of original pre-therapy count. Compared to placebo, antigen-specific IgM titers were decreased by 91% and 25% in response to KLH and PPV, respectively. IgG titers were decreased by 45% and 50%, in response to KLH and PPV. The capacity to mount a skin delayed-type hypersensitivity reaction to Candida and tetanus toxoid was decreased by approximately 30% in subjects on fingolimod 0.5 mg daily, compared to placebo. Immunologic responses were further decreased with fingolimod 1.25 mg (a dose higher than recommended for MS). Single fingolimod doses ≥5 mg (10-fold the recommended dose) are associated with a dose-dependent increase in airway resistance.

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.

TargetActionsOrganism
ASphingosine 1-phosphate receptor 5
modulator
Human
UHistone deacetylase 1
inhibitor
Human
Absorption

The Tmax of fingolimod is 12-16 hours. Bioavailability: 93%

Volume of distribution

about 1200±260 L.

Protein binding

>99.7%

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.

Route of elimination
Not Available
Half life

6-9 days

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

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2-Methoxyethanol2-Methoxyethanol may increase the immunosuppressive activities of Fingolimod.Experimental
AbataceptAbatacept may increase the immunosuppressive activities of Fingolimod.Approved
abetimusabetimus may increase the immunosuppressive activities of Fingolimod.Investigational
AbirateroneThe serum concentration of Fingolimod can be increased when it is combined with Abiraterone.Approved
AcebutololAcebutolol may increase the bradycardic activities of Fingolimod.Approved
ActeosideActeoside may increase the immunosuppressive activities of Fingolimod.Investigational
AdalimumabAdalimumab may increase the immunosuppressive activities of Fingolimod.Approved
AdefovirAdefovir may increase the immunosuppressive activities of Fingolimod.Investigational
AfelimomabAfelimomab may increase the immunosuppressive activities of Fingolimod.Investigational
AjmalineFingolimod may increase the arrhythmogenic activities of Ajmaline.Approved, Investigational
AlefaceptAlefacept may increase the immunosuppressive activities of Fingolimod.Approved, Investigational, Withdrawn
AlemtuzumabAlemtuzumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
AlicaforsenAlicaforsen may increase the immunosuppressive activities of Fingolimod.Investigational
AlprenololAlprenolol may increase the bradycardic activities of Fingolimod.Approved, Withdrawn
AltretamineAltretamine may increase the immunosuppressive activities of Fingolimod.Approved
AmiodaroneFingolimod may increase the arrhythmogenic activities of Amiodarone.Approved, Investigational
AmsacrineAmsacrine may increase the immunosuppressive activities of Fingolimod.Approved
AnagrelideFingolimod may increase the QTc-prolonging activities of Anagrelide.Approved
AnakinraAnakinra may increase the immunosuppressive activities of Fingolimod.Approved
Antilymphocyte immunoglobulin (horse)Antilymphocyte immunoglobulin (horse) may increase the immunosuppressive activities of Fingolimod.Approved
Antithymocyte immunoglobulin (rabbit)Antithymocyte immunoglobulin (rabbit) may increase the immunosuppressive activities of Fingolimod.Approved
ApremilastApremilast may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
AprepitantThe serum concentration of Fingolimod can be increased when it is combined with Aprepitant.Approved, Investigational
ArotinololArotinolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
Arsenic trioxideFingolimod may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherFingolimod may increase the QTc-prolonging activities of Artemether.Approved
AsenapineFingolimod may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirThe metabolism of Fingolimod can be decreased when combined with Atazanavir.Approved, Investigational
AtenololAtenolol may increase the bradycardic activities of Fingolimod.Approved
AtomoxetineThe metabolism of Fingolimod can be decreased when combined with Atomoxetine.Approved
AzacitidineAzacitidine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
AzathioprineAzathioprine may increase the immunosuppressive activities of Fingolimod.Approved
AzithromycinFingolimod may increase the QTc-prolonging activities of Azithromycin.Approved
BasiliximabBasiliximab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Fingolimod.Investigational
BedaquilineFingolimod may increase the QTc-prolonging activities of Bedaquiline.Approved
BefunololBefunolol may increase the bradycardic activities of Fingolimod.Experimental
BegelomabBegelomab may increase the immunosuppressive activities of Fingolimod.Experimental, Investigational
BelataceptBelatacept may increase the immunosuppressive activities of Fingolimod.Approved
BelimumabBelimumab may increase the immunosuppressive activities of Fingolimod.Approved
BendroflumethiazideBendroflumethiazide may increase the bradycardic activities of Fingolimod.Approved
BenznidazoleBenznidazole may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
BeractantBeractant may increase the bradycardic activities of Fingolimod.Approved
BetamethasoneBetamethasone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
BetaxololBetaxolol may increase the bradycardic activities of Fingolimod.Approved
BevantololBevantolol may increase the bradycardic activities of Fingolimod.Approved
BisoprololBisoprolol may increase the bradycardic activities of Fingolimod.Approved
BleomycinBleomycin may increase the immunosuppressive activities of Fingolimod.Approved
BlinatumomabBlinatumomab may increase the immunosuppressive activities of Fingolimod.Approved
BoceprevirThe metabolism of Fingolimod can be decreased when combined with Boceprevir.Approved, Withdrawn
BopindololBopindolol may increase the bradycardic activities of Fingolimod.Approved
BortezomibThe metabolism of Fingolimod can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Fingolimod can be decreased when it is combined with Bosentan.Approved, Investigational
Brentuximab vedotinBrentuximab vedotin may increase the immunosuppressive activities of Fingolimod.Approved
BretyliumBretylium may increase the bradycardic activities of Fingolimod.Approved
BriakinumabBriakinumab may increase the immunosuppressive activities of Fingolimod.Investigational
BrodalumabBrodalumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
BucindololBucindolol may increase the bradycardic activities of Fingolimod.Investigational
BudesonideBudesonide may increase the immunosuppressive activities of Fingolimod.Approved
BufuralolBufuralol may increase the bradycardic activities of Fingolimod.Experimental, Investigational
BunaftineFingolimod may increase the arrhythmogenic activities of Bunaftine.Experimental
BupranololBupranolol may increase the bradycardic activities of Fingolimod.Approved
BupropionThe metabolism of Fingolimod can be decreased when combined with Bupropion.Approved
BusulfanBusulfan may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
CabazitaxelCabazitaxel may increase the immunosuppressive activities of Fingolimod.Approved
CalfactantCalfactant may increase the bradycardic activities of Fingolimod.Approved
CanakinumabCanakinumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
CapecitabineCapecitabine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
CarbamazepineThe serum concentration of Fingolimod can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarboplatinCarboplatin may increase the immunosuppressive activities of Fingolimod.Approved
CarmustineCarmustine may increase the immunosuppressive activities of Fingolimod.Approved
CarteololCarteolol may increase the bradycardic activities of Fingolimod.Approved
CarvedilolCarvedilol may increase the bradycardic activities of Fingolimod.Approved, Investigational
CastanospermineCastanospermine may increase the immunosuppressive activities of Fingolimod.Experimental
CelecoxibThe metabolism of Fingolimod can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololCeliprolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
CeritinibThe serum concentration of Fingolimod can be increased when it is combined with Ceritinib.Approved
Certolizumab pegolCertolizumab pegol may increase the immunosuppressive activities of Fingolimod.Approved
ChlorambucilChlorambucil may increase the immunosuppressive activities of Fingolimod.Approved
ChloroquineFingolimod may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineFingolimod may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Fingolimod can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Fingolimod can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Fingolimod can be decreased when combined with Cinacalcet.Approved
CiprofloxacinFingolimod may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideFingolimod may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CisplatinCisplatin may increase the immunosuppressive activities of Fingolimod.Approved
CitalopramFingolimod may increase the QTc-prolonging activities of Citalopram.Approved
CladribineCladribine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
ClarithromycinThe metabolism of Fingolimod can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Fingolimod can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Fingolimod can be decreased when combined with Clobazam.Approved, Illicit
ClofarabineClofarabine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
ClomipramineThe metabolism of Fingolimod can be decreased when combined with Clomipramine.Approved, Vet Approved
ClonidineClonidine may increase the bradycardic activities of Fingolimod.Approved
CloranololCloranolol may increase the bradycardic activities of Fingolimod.Experimental
Clostridium tetani toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Fingolimod.Approved
ClotrimazoleThe metabolism of Fingolimod can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineFingolimod may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe serum concentration of Fingolimod can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Fingolimod can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Fingolimod can be increased when it is combined with Conivaptan.Approved, Investigational
CorticotropinCorticotropin may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
Cortisone acetateCortisone acetate may increase the immunosuppressive activities of Fingolimod.Approved
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Fingolimod.Approved
CrizotinibFingolimod may increase the QTc-prolonging activities of Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
CyclosporineCyclosporine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Fingolimod can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
CytarabineCytarabine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DabrafenibThe serum concentration of Fingolimod can be decreased when it is combined with Dabrafenib.Approved
DacarbazineDacarbazine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DaclizumabDaclizumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DactinomycinDactinomycin may increase the immunosuppressive activities of Fingolimod.Approved
DarifenacinThe metabolism of Fingolimod can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Fingolimod can be increased when it is combined with Darunavir.Approved
DasatinibDasatinib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DaunorubicinDaunorubicin may increase the immunosuppressive activities of Fingolimod.Approved
DeferasiroxThe serum concentration of Fingolimod can be decreased when it is combined with Deferasirox.Approved, Investigational
DeflazacortDeflazacort may increase the immunosuppressive activities of Fingolimod.Approved
DelavirdineThe metabolism of Fingolimod can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Fingolimod.Approved
DeoxyspergualinDeoxyspergualin may increase the immunosuppressive activities of Fingolimod.Investigational
DesipramineThe metabolism of Fingolimod can be decreased when combined with Desipramine.Approved
DexamethasoneDexamethasone may increase the immunosuppressive activities of Fingolimod.Approved, Investigational, Vet Approved
DexmedetomidineDexmedetomidine may increase the bradycardic activities of Fingolimod.Approved, Vet Approved
DigoxinDigoxin may increase the bradycardic activities of Fingolimod.Approved
DihydroergotamineThe metabolism of Fingolimod can be decreased when combined with Dihydroergotamine.Approved
DiltiazemDiltiazem may increase the bradycardic activities of Fingolimod.Approved
Dimethyl fumarateDimethyl fumarate may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DinutuximabDinutuximab may increase the immunosuppressive activities of Fingolimod.Approved
DiphenhydramineThe metabolism of Fingolimod can be decreased when combined with Diphenhydramine.Approved
DisopyramideFingolimod may increase the arrhythmogenic activities of Disopyramide.Approved
DocetaxelDocetaxel may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DofetilideFingolimod may increase the arrhythmogenic activities of Dofetilide.Approved
DolasetronFingolimod may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneFingolimod may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DonepezilDonepezil may increase the bradycardic activities of Fingolimod.Approved
DosulepinThe metabolism of Fingolimod can be decreased when combined with Dosulepin.Approved
DoxifluridineDoxifluridine may increase the immunosuppressive activities of Fingolimod.Investigational
DoxorubicinDoxorubicin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
DoxycyclineThe metabolism of Fingolimod can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneFingolimod may increase the arrhythmogenic activities of Dronedarone.Approved
DroperidolFingolimod may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DuloxetineThe metabolism of Fingolimod can be decreased when combined with Duloxetine.Approved
EculizumabEculizumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
EfalizumabEfalizumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
EliglustatFingolimod may increase the QTc-prolonging activities of Eliglustat.Approved
EnzalutamideThe serum concentration of Fingolimod can be decreased when it is combined with Enzalutamide.Approved
EpanololEpanolol may increase the bradycardic activities of Fingolimod.Experimental
EpirubicinEpirubicin may increase the immunosuppressive activities of Fingolimod.Approved
ErythromycinFingolimod may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramFingolimod may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
EsmololEsmolol may increase the bradycardic activities of Fingolimod.Approved
EstramustineEstramustine may increase the immunosuppressive activities of Fingolimod.Approved
EtanerceptEtanercept may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
EtoposideEtoposide may increase the immunosuppressive activities of Fingolimod.Approved
EverolimusEverolimus may increase the immunosuppressive activities of Fingolimod.Approved
FlecainideFingolimod may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FloxuridineFloxuridine may increase the immunosuppressive activities of Fingolimod.Approved
FluconazoleThe metabolism of Fingolimod can be decreased when combined with Fluconazole.Approved
FludarabineFludarabine may increase the immunosuppressive activities of Fingolimod.Approved
FludrocortisoneFludrocortisone may increase the immunosuppressive activities of Fingolimod.Approved
FluorouracilFluorouracil may increase the immunosuppressive activities of Fingolimod.Approved
FluoxetineFingolimod may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolFingolimod may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvoxamineThe metabolism of Fingolimod can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Fingolimod can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Fingolimod can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Fingolimod can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Fingolimod can be increased when it is combined with Fusidic Acid.Approved
G17DTThe therapeutic efficacy of G17DT can be decreased when used in combination with Fingolimod.Investigational
Gadobenic acidFingolimod may increase the QTc-prolonging activities of Gadobenic acid.Approved
GalantamineGalantamine may increase the bradycardic activities of Fingolimod.Approved
Gallium nitrateGallium nitrate may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
GemcitabineGemcitabine may increase the immunosuppressive activities of Fingolimod.Approved
GemifloxacinFingolimod may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
Gemtuzumab ozogamicinGemtuzumab ozogamicin may increase the immunosuppressive activities of Fingolimod.Approved
GI-5005The therapeutic efficacy of GI-5005 can be decreased when used in combination with Fingolimod.Investigational
Glatiramer AcetateGlatiramer Acetate may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
GlimepirideGlimepiride may increase the immunosuppressive activities of Fingolimod.Approved
GolimumabGolimumab may increase the immunosuppressive activities of Fingolimod.Approved
GoserelinFingolimod may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronFingolimod may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GS 0573GS 0573 may increase the immunosuppressive activities of Fingolimod.Investigational
GuanfacineGuanfacine may increase the bradycardic activities of Fingolimod.Approved, Investigational
GusperimusGusperimus may increase the immunosuppressive activities of Fingolimod.Investigational
HaloperidolFingolimod may increase the QTc-prolonging activities of Haloperidol.Approved
Hepatitis A VaccineThe therapeutic efficacy of Hepatitis A Vaccine can be decreased when used in combination with Fingolimod.Approved
Hepatitis B Vaccine (Recombinant)The therapeutic efficacy of Hepatitis B Vaccine (Recombinant) can be decreased when used in combination with Fingolimod.Approved, Withdrawn
Human C1-esterase inhibitorHuman C1-esterase inhibitor may increase the immunosuppressive activities of Fingolimod.Approved
HydrocortisoneHydrocortisone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
HydroxyureaHydroxyurea may increase the immunosuppressive activities of Fingolimod.Approved
HypericinHypericin may increase the immunosuppressive activities of Fingolimod.Investigational
Ibritumomab tiuxetanIbritumomab tiuxetan may increase the immunosuppressive activities of Fingolimod.Approved
IbrutinibIbrutinib may increase the immunosuppressive activities of Fingolimod.Approved
IbutilideFingolimod may increase the arrhythmogenic activities of Ibutilide.Approved
IcatibantIcatibant may increase the immunosuppressive activities of Fingolimod.Approved
IdarubicinIdarubicin may increase the immunosuppressive activities of Fingolimod.Approved
IdelalisibIdelalisib may increase the immunosuppressive activities of Fingolimod.Approved
IfosfamideIfosfamide may increase the immunosuppressive activities of Fingolimod.Approved
IloperidoneFingolimod may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibImatinib may increase the immunosuppressive activities of Fingolimod.Approved
ImipramineThe metabolism of Fingolimod can be decreased when combined with Imipramine.Approved
ImiquimodImiquimod may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
IndenololIndenolol may increase the bradycardic activities of Fingolimod.Withdrawn
IndinavirThe metabolism of Fingolimod can be decreased when combined with Indinavir.Approved
InfliximabInfliximab may increase the immunosuppressive activities of Fingolimod.Approved
INGN 201The therapeutic efficacy of INGN 201 can be decreased when used in combination with Fingolimod.Investigational
INGN 225The therapeutic efficacy of INGN 225 can be decreased when used in combination with Fingolimod.Investigational
IrinotecanIrinotecan may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
IsavuconazoniumThe metabolism of Fingolimod can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Fingolimod can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Fingolimod can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Fingolimod can be decreased when combined with Itraconazole.Approved, Investigational
IvabradineFingolimod may increase the bradycardic activities of Ivabradine.Approved
IvacaftorThe serum concentration of Fingolimod can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe serum concentration of the active metabolites of Fingolimod can be increased when Fingolimod is used in combination with Ketoconazole.Approved, Investigational
L-PhenylalanineL-Phenylalanine may increase the immunosuppressive activities of Fingolimod.Approved, Nutraceutical
LabetalolLabetalol may increase the bradycardic activities of Fingolimod.Approved
LacosamideFingolimod may increase the atrioventricular blocking (AV block) activities of Lacosamide.Approved
LandiololLandiolol may increase the bradycardic activities of Fingolimod.Investigational
LanreotideLanreotide may increase the bradycardic activities of Fingolimod.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Fingolimod is combined with Leflunomide.Approved, Investigational
LenalidomideLenalidomide may increase the immunosuppressive activities of Fingolimod.Approved
LenvatinibFingolimod may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideFingolimod may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevobunololLevobunolol may increase the bradycardic activities of Fingolimod.Approved
LevofloxacinFingolimod may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LisofyllineLisofylline may increase the immunosuppressive activities of Fingolimod.Investigational
LomustineLomustine may increase the immunosuppressive activities of Fingolimod.Approved
LopinavirThe metabolism of Fingolimod can be decreased when combined with Lopinavir.Approved
LorajmineFingolimod may increase the arrhythmogenic activities of Lorajmine.Experimental
LorcaserinThe metabolism of Fingolimod can be decreased when combined with Lorcaserin.Approved
LovastatinThe metabolism of Fingolimod can be decreased when combined with Lovastatin.Approved, Investigational
LucinactantLucinactant may increase the bradycardic activities of Fingolimod.Approved, Investigational
LuliconazoleThe serum concentration of Fingolimod can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Fingolimod can be increased when combined with Lumacaftor.Approved
LumefantrineFingolimod may increase the QTc-prolonging activities of Lumefantrine.Approved
ManidipineThe metabolism of Fingolimod can be decreased when combined with Manidipine.Approved, Investigational
MechlorethamineMechlorethamine may increase the immunosuppressive activities of Fingolimod.Approved
MelphalanMelphalan may increase the immunosuppressive activities of Fingolimod.Approved
MepindololMepindolol may increase the bradycardic activities of Fingolimod.Experimental
MepolizumabMepolizumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
MercaptopurineMercaptopurine may increase the immunosuppressive activities of Fingolimod.Approved
MethadoneFingolimod may increase the QTc-prolonging activities of Methadone.Approved
MethotrexateMethotrexate may increase the immunosuppressive activities of Fingolimod.Approved
MethotrimeprazineThe metabolism of Fingolimod can be decreased when combined with Methotrimeprazine.Approved
MethyldopaMethyldopa may increase the bradycardic activities of Fingolimod.Approved
MethylprednisoloneMethylprednisolone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
MetipranololMetipranolol may increase the bradycardic activities of Fingolimod.Approved
MetoprololMetoprolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
MidostaurinThe metabolism of Fingolimod can be decreased when combined with Midostaurin.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Fingolimod.Approved, Investigational
MirabegronThe metabolism of Fingolimod can be decreased when combined with Mirabegron.Approved
MitomycinMitomycin may increase the immunosuppressive activities of Fingolimod.Approved
MitotaneThe serum concentration of Fingolimod can be decreased when it is combined with Mitotane.Approved
MitoxantroneMitoxantrone may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
MizoribineMizoribine may increase the immunosuppressive activities of Fingolimod.Investigational
MoxifloxacinFingolimod may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
MuromonabMuromonab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
Mycophenolate mofetilMycophenolate mofetil may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
Mycophenolic acidMycophenolic acid may increase the immunosuppressive activities of Fingolimod.Approved
NadololNadolol may increase the bradycardic activities of Fingolimod.Approved
NafamostatNafamostat may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
NatalizumabNatalizumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
NebivololNebivolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
NefazodoneThe metabolism of Fingolimod can be decreased when combined with Nefazodone.Approved, Withdrawn
NelarabineNelarabine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
NelfinavirThe metabolism of Fingolimod can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Fingolimod can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Fingolimod can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Fingolimod can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Fingolimod can be decreased when combined with Nicotine.Approved
NilotinibNilotinib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
ObinutuzumabObinutuzumab may increase the immunosuppressive activities of Fingolimod.Approved
OctreotideOctreotide may increase the bradycardic activities of Fingolimod.Approved, Investigational
OfloxacinFingolimod may increase the QTc-prolonging activities of Ofloxacin.Approved
OlaparibThe metabolism of Fingolimod can be decreased when combined with Olaparib.Approved
OndansetronFingolimod may increase the QTc-prolonging activities of Ondansetron.Approved
OsimertinibThe serum concentration of Fingolimod can be increased when it is combined with Osimertinib.Approved
OxaliplatinOxaliplatin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
OxprenololOxprenolol may increase the bradycardic activities of Fingolimod.Approved
PaclitaxelPaclitaxel may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
PalbociclibPalbociclib may increase the immunosuppressive activities of Fingolimod.Approved
PaliperidoneFingolimod may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatPanobinostat may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
PaquinimodPaquinimod may increase the immunosuppressive activities of Fingolimod.Investigational
ParoxetineThe metabolism of Fingolimod can be decreased when combined with Paroxetine.Approved, Investigational
PasireotidePasireotide may increase the bradycardic activities of Fingolimod.Approved
PazopanibPazopanib may increase the immunosuppressive activities of Fingolimod.Approved
PegaspargasePegaspargase may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Fingolimod can be decreased when it is combined with Peginterferon alfa-2b.Approved
PemetrexedPemetrexed may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
PenbutololPenbutolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
PentamidineFingolimod may increase the QTc-prolonging activities of Pentamidine.Approved
PentobarbitalThe metabolism of Fingolimod can be increased when combined with Pentobarbital.Approved, Vet Approved
PentostatinPentostatin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
PerflutrenFingolimod may increase the QTc-prolonging activities of Perflutren.Approved
PhenobarbitalThe metabolism of Fingolimod can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Fingolimod can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusPimecrolimus may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
PimozideFingolimod may increase the QTc-prolonging activities of Pimozide.Approved
PindololPindolol may increase the bradycardic activities of Fingolimod.Approved
PirarubicinPirarubicin may increase the immunosuppressive activities of Fingolimod.Investigational
PirfenidonePirfenidone may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
Platelet Activating FactorPlatelet Activating Factor may increase the bradycardic activities of Fingolimod.Experimental
PomalidomidePomalidomide may increase the immunosuppressive activities of Fingolimod.Approved
Poractant alfaFingolimod may increase the bradycardic activities of Poractant alfa.Approved
PosaconazoleThe metabolism of Fingolimod can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PractololPractolol may increase the bradycardic activities of Fingolimod.Approved
PrajmalineFingolimod may increase the arrhythmogenic activities of Prajmaline.Experimental
PralatrexatePralatrexate may increase the immunosuppressive activities of Fingolimod.Approved
PrednisolonePrednisolone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
PrednisonePrednisone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
PrimaquineFingolimod may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe metabolism of Fingolimod can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideFingolimod may increase the arrhythmogenic activities of Procainamide.Approved
ProcarbazineProcarbazine may increase the immunosuppressive activities of Fingolimod.Approved
PromazineFingolimod may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneFingolimod may increase the QTc-prolonging activities of Propafenone.Approved
PropranololPropranolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
QuetiapineFingolimod may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineFingolimod may increase the arrhythmogenic activities of Quinidine.Approved
QuinineFingolimod may increase the QTc-prolonging activities of Quinine.Approved
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Fingolimod is combined with Rabies virus inactivated antigen, A.Approved
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Fingolimod.Approved
RanolazineThe metabolism of Fingolimod can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Fingolimod can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Fingolimod can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Fingolimod can be increased when combined with Rifapentine.Approved
RilonaceptRilonacept may increase the immunosuppressive activities of Fingolimod.Approved
RindopepimutThe therapeutic efficacy of Rindopepimut can be decreased when used in combination with Fingolimod.Investigational
RitonavirThe metabolism of Fingolimod can be decreased when combined with Ritonavir.Approved, Investigational
RituximabRituximab may increase the immunosuppressive activities of Fingolimod.Approved
RivastigmineRivastigmine may increase the bradycardic activities of Fingolimod.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Fingolimod.Approved
RolapitantThe metabolism of Fingolimod can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Fingolimod can be decreased when combined with Ropinirole.Approved, Investigational
Rotavirus VaccineThe therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Fingolimod.Approved
Rubella virus vaccineThe therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Fingolimod.Approved
RuxolitinibRuxolitinib may increase the immunosuppressive activities of Fingolimod.Approved
Salmonella typhi ty21a live antigenThe therapeutic efficacy of Salmonella typhi ty21a live antigen can be decreased when used in combination with Fingolimod.Approved
SaquinavirThe metabolism of Fingolimod can be decreased when combined with Saquinavir.Approved, Investigational
SecukinumabSecukinumab may increase the immunosuppressive activities of Fingolimod.Approved
SemapimodSemapimod may increase the immunosuppressive activities of Fingolimod.Investigational
SeocalcitolSeocalcitol may increase the immunosuppressive activities of Fingolimod.Experimental, Investigational
SertralineThe metabolism of Fingolimod can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Fingolimod can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabSiltuximab may increase the immunosuppressive activities of Fingolimod.Approved
SimeprevirThe serum concentration of Fingolimod can be increased when it is combined with Simeprevir.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Fingolimod.Approved
SirolimusSirolimus may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
SorafenibSorafenib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
SotalolSotalol may increase the bradycardic activities of Fingolimod.Approved
SparteineFingolimod may increase the arrhythmogenic activities of Sparteine.Experimental
SRP 299The therapeutic efficacy of SRP 299 can be decreased when used in combination with Fingolimod.Investigational
St. John's WortThe serum concentration of Fingolimod can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
SteproninStepronin may increase the immunosuppressive activities of Fingolimod.Approved
StiripentolThe serum concentration of Fingolimod can be increased when it is combined with Stiripentol.Approved
StreptozocinStreptozocin may increase the immunosuppressive activities of Fingolimod.Approved
SufentanilSufentanil may increase the bradycardic activities of Fingolimod.Approved, Investigational
SulfisoxazoleFingolimod may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SunitinibSunitinib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TacrolimusTacrolimus may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TalinololTalinolol may increase the bradycardic activities of Fingolimod.Investigational
TecemotideThe therapeutic efficacy of Tecemotide can be decreased when used in combination with Fingolimod.Investigational
TedisamilFingolimod may increase the arrhythmogenic activities of Tedisamil.Investigational
TelaprevirThe metabolism of Fingolimod can be decreased when combined with Telaprevir.Approved, Withdrawn
TelavancinFingolimod may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe metabolism of Fingolimod can be decreased when combined with Telithromycin.Approved
TemozolomideTemozolomide may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TemsirolimusTemsirolimus may increase the immunosuppressive activities of Fingolimod.Approved
TeniposideTeniposide may increase the immunosuppressive activities of Fingolimod.Approved
TepoxalinTepoxalin may increase the immunosuppressive activities of Fingolimod.Vet Approved
TerbinafineThe metabolism of Fingolimod can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TeriflunomideTeriflunomide may increase the immunosuppressive activities of Fingolimod.Approved
TertatololTertatolol may increase the bradycardic activities of Fingolimod.Experimental
TetrabenazineFingolimod may increase the QTc-prolonging activities of Tetrabenazine.Approved
TG4010The therapeutic efficacy of TG4010 can be decreased when used in combination with Fingolimod.Investigational
ThalidomideThalidomide may increase the immunosuppressive activities of Fingolimod.Approved, Investigational, Withdrawn
ThioridazineFingolimod may increase the QTc-prolonging activities of Thioridazine.Approved, Withdrawn
ThiotepaThiotepa may increase the immunosuppressive activities of Fingolimod.Approved
TiclopidineThe metabolism of Fingolimod can be decreased when combined with Ticlopidine.Approved
TimololTimolol may increase the bradycardic activities of Fingolimod.Approved
TioguanineTioguanine may increase the immunosuppressive activities of Fingolimod.Approved
TipranavirThe metabolism of Fingolimod can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineTizanidine may increase the bradycardic activities of Fingolimod.Approved
TocilizumabTocilizumab may increase the immunosuppressive activities of Fingolimod.Approved
TofacitinibTofacitinib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TopotecanTopotecan may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
ToremifeneFingolimod may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TositumomabTositumomab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TrabectedinTrabectedin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TranylcypromineThe metabolism of Fingolimod can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the neutropenic activities of Fingolimod.Approved, Investigational
Trastuzumab emtansineTrastuzumab emtansine may increase the immunosuppressive activities of Fingolimod.Approved
TretinoinTretinoin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational, Nutraceutical
TriamcinoloneTriamcinolone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
TriptolideTriptolide may increase the immunosuppressive activities of Fingolimod.Investigational
TrofosfamideTrofosfamide may increase the immunosuppressive activities of Fingolimod.Investigational
UstekinumabUstekinumab may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
VandetanibFingolimod may increase the QTc-prolonging activities of Vandetanib.Approved
VedolizumabVedolizumab may increase the immunosuppressive activities of Fingolimod.Approved
VemurafenibFingolimod may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineThe metabolism of Fingolimod can be decreased when combined with Venlafaxine.Approved
VerapamilVerapamil may increase the bradycardic activities of Fingolimod.Approved
VilanterolVilanterol may increase the immunosuppressive activities of Fingolimod.Approved
VinblastineVinblastine may increase the immunosuppressive activities of Fingolimod.Approved
VincristineVincristine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
VindesineVindesine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
VinorelbineVinorelbine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
VoclosporinVoclosporin may increase the immunosuppressive activities of Fingolimod.Investigational
VoriconazoleThe metabolism of Fingolimod can be decreased when combined with Voriconazole.Approved, Investigational
Yellow fever vaccineThe therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Fingolimod.Approved
ZiprasidoneFingolimod may increase the QTc-prolonging activities of Ziprasidone.Approved
Zoster vaccineThe risk or severity of adverse effects can be increased when Fingolimod is combined with Zoster vaccine.Approved
ZuclopenthixolFingolimod may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference

Ramesh Matioram Gidwani, Channaveerayya Hiremath, "PROCESS FOR PRODUCING FINGOLIMOD SALTS." U.S. Patent US20120184617, issued July 19, 2012.

US20120184617
General References
  1. An X, Kezuka T, Usui Y, Matsunaga Y, Matsuda R, Yamakawa N, Goto H: Suppression of experimental autoimmune optic neuritis by the novel agent fingolimod. J Neuroophthalmol. 2013 Jun;33(2):143-8. doi: 10.1097/WNO.0b013e31828ea2fc. [PubMed:23609767]
  2. Ali R, Nicholas RS, Muraro PA: Drugs in development for relapsing multiple sclerosis. Drugs. 2013 May;73(7):625-50. doi: 10.1007/s40265-013-0030-6. [PubMed:23609782]
External Links
KEGG Drug
D10001
PubChem Compound
107970
PubChem Substance
175427125
ChemSpider
97087
BindingDB
50158336
ChEBI
63115
ChEMBL
CHEMBL314854
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fingolimod
ATC Codes
L04AA27 — Fingolimod
AHFS Codes
  • 92:44.00 — Immunosuppressive Agents
FDA label
Download (423 KB)
MSDS
Download (351 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedOtherAnaplastic Astrocytoma (AA) / Glioblastomas1
1CompletedNot AvailableImpaired Renal Function1
1CompletedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
1CompletedTreatmentAutoimmune Diseases / Disseminated or Multiple Sclerosis Nos / Disseminated Sclerosis / Multiple Sclerosis, Acute Relapsing / Multiple Sclerosis, Chronic Progressive / Multiple Sclerosis, Primary Progressive1
1CompletedTreatmentHealthy Volunteers1
1, 2Active Not RecruitingTreatmentRett's Syndrome1
2Active Not RecruitingTreatmentSchizophrenic Disorders1
2CompletedTreatmentAmyotrophic Lateral Sclerosis (ALS)1
2CompletedTreatmentAsthma Bronchial1
2CompletedTreatmentDisseminated Sclerosis3
2CompletedTreatmentTransplantation, Renal2
2Not Yet RecruitingTreatmentInflammatory Reaction / Strokes1
2TerminatedTreatmentAcute Demylelinating Optic Neuritis1
2Unknown StatusTreatmentCerebral Stroke / Ischemic Cerebrovascular Accident / Stroke, Acute / Strokes / Vascular Accident1
2WithdrawnTreatmentAcute Noninfectious Posterior, Intermediate, or Pan Uveitis1
2, 3CompletedTreatmentDisseminated Sclerosis1
2, 3RecruitingTreatmentDisseminated Sclerosis / Relapsing Remitting Multiple Sclerosis (RRMS)1
2, 3TerminatedTreatmentDisseminated Sclerosis1
3Active Not RecruitingTreatmentDisseminated Sclerosis1
3Active Not RecruitingTreatmentRelapsing Forms of Multiple Sclerosis1
3CompletedTreatmentDisseminated Sclerosis4
3CompletedTreatmentMultiple Sclerosis, Primary Progressive2
3CompletedTreatmentPolyradiculoneuropathy, Chronic Inflammatory Demyelinating1
3CompletedTreatmentRelapsing Multiple Sclerosis (RMS)2
3CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
3CompletedTreatmentTransplantation, Kidney3
3CompletedTreatmentTransplantation, Renal4
3TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
3WithdrawnTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4Active Not RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedBasic ScienceAutonomic Nervous System Dysfunction / Disseminated Sclerosis1
4CompletedBasic ScienceRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedSupportive CareDisseminated Sclerosis / Relapsing-Remitting1
4CompletedTreatmentDisseminated Sclerosis2
4CompletedTreatmentRelapsing Forms of Multiple Sclerosis1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)6
4RecruitingNot AvailableDisseminated Sclerosis1
4RecruitingBasic ScienceRelapsing Multiple Sclerosis (RMS)1
4RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedTreatmentDepression / Relapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2
4Unknown StatusTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4WithdrawnTreatmentDisseminated Sclerosis1
Not AvailableActive Not RecruitingNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
Not AvailableCompletedNot AvailableDisseminated Sclerosis2
Not AvailableRecruitingNot AvailableDisseminated Sclerosis3
Not AvailableRecruitingNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral.5 mg/1
CapsuleOral0.5 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9187405No2007-06-252027-06-25Us
US6004565No1997-09-232017-09-23Us
US5604229No1999-02-182019-02-18Us
US8324283No2006-03-292026-03-29Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)479.498 °C at 760 mmHgACD/PhysChem
water solubilitySolublehttp://www.medsafe.govt.nz/profs/datasheet/g/gilenyacap.pdf
logP4.178ACD/PhysChem
Predicted Properties
PropertyValueSource
Water Solubility0.0069 mg/mLALOGPS
logP4ALOGPS
logP4.06ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)14.41ChemAxon
pKa (Strongest Basic)9.38ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area66.48 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity93.28 m3·mol-1ChemAxon
Polarizability38.81 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9884
Blood Brain Barrier+0.5779
Caco-2 permeable-0.5055
P-glycoprotein substrateSubstrate0.6975
P-glycoprotein inhibitor INon-inhibitor0.9505
P-glycoprotein inhibitor IINon-inhibitor0.9391
Renal organic cation transporterNon-inhibitor0.823
CYP450 2C9 substrateNon-substrate0.8251
CYP450 2D6 substrateNon-substrate0.6702
CYP450 3A4 substrateNon-substrate0.7685
CYP450 1A2 substrateInhibitor0.5519
CYP450 2C9 inhibitorNon-inhibitor0.8526
CYP450 2D6 inhibitorInhibitor0.6567
CYP450 2C19 inhibitorNon-inhibitor0.8152
CYP450 3A4 inhibitorNon-inhibitor0.7348
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8945
Ames testNon AMES toxic0.8647
CarcinogenicityNon-carcinogens0.8562
BiodegradationNot ready biodegradable0.9062
Rat acute toxicity1.9996 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.933
hERG inhibition (predictor II)Non-inhibitor0.7302
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as aralkylamines. These are alkylamines in which the alkyl group is substituted at one carbon atom by an aromatic hydrocarbyl group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Amines
Direct Parent
Aralkylamines
Alternative Parents
Benzene and substituted derivatives / 1,2-aminoalcohols / Primary alcohols / Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives
Substituents
Aralkylamine / Benzenoid / Monocyclic benzene moiety / 1,2-aminoalcohol / Organic oxygen compound / Organopnictogen compound / Hydrocarbon derivative / Primary amine / Primary alcohol / Organooxygen compound
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
primary amino compound, aminodiol (CHEBI:63115)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Modulator
General Function
Sphingosine-1-phosphate receptor activity
Specific Function
Receptor for the lysosphingolipid sphingosine 1-phosphate (S1P). S1P is a bioactive lysophospholipid that elicits diverse physiological effect on most types of cells and tissues. Is coupled to both...
Gene Name
S1PR5
Uniprot ID
Q9H228
Uniprot Name
Sphingosine 1-phosphate receptor 5
Molecular Weight
41774.515 Da
References
  1. Zu Heringdorf DM, Ihlefeld K, Pfeilschifter J: Pharmacology of the sphingosine-1-phosphate signalling system. Handb Exp Pharmacol. 2013;(215):239-53. doi: 10.1007/978-3-7091-1368-4_13. [PubMed:23579459]
  2. Bhabak KP, Arenz C: Novel drugs targeting sphingolipid metabolism. Handb Exp Pharmacol. 2013;(215):187-96. doi: 10.1007/978-3-7091-1368-4_10. [PubMed:23579456]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transcription regulatory region sequence-specific dna binding
Specific Function
Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an impo...
Gene Name
HDAC1
Uniprot ID
Q13547
Uniprot Name
Histone deacetylase 1
Molecular Weight
55102.615 Da
References
  1. Hait NC, Wise LE, Allegood JC, O'Brien M, Avni D, Reeves TM, Knapp PE, Lu J, Luo C, Miles MF, Milstien S, Lichtman AH, Spiegel S: Active, phosphorylated fingolimod inhibits histone deacetylases and facilitates fear extinction memory. Nat Neurosci. 2014 Jul;17(7):971-80. doi: 10.1038/nn.3728. Epub 2014 May 25. [PubMed:24859201]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Not Available
Gene Name
CYP4F2
Uniprot ID
P78329
Uniprot Name
Phylloquinone omega-hydroxylase CYP4F2
Molecular Weight
59852.825 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sphingosine-1-phosphate receptor activity
Specific Function
Catalyzes the phosphorylation of sphingosine to form sphingosine 1-phosphate (SPP), a lipid mediator with both intra- and extracellular functions. Also acts on D-erythro-sphingosine and to a lesser...
Gene Name
SPHK1
Uniprot ID
Q9NYA1
Uniprot Name
Sphingosine kinase 1
Molecular Weight
42517.245 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Leukotriene-b4 20-monooxygenase activity
Specific Function
Catalyzes leukotriene B4 omega-hydroxylation and arachidonic acid omega-hydroxylation but with an activity much lower than that of CYP4F2. Catalyzes the hydroxylation of the antihistamine ebastine.
Gene Name
CYP4F12
Uniprot ID
Q9HCS2
Uniprot Name
Cytochrome P450 4F12
Molecular Weight
60269.165 Da

Drug created on April 28, 2013 14:17 / Updated on November 22, 2017 12:37