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Identification
NameFingolimod
Accession NumberDB08868
TypeSmall Molecule
GroupsApproved, 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 Identifiers
  • FTY-720A
  • FTY720
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gilenyacapsule.5 mg/1oralNovartis Pharmaceuticals Corporation2010-09-21Not applicableUs
Gilenyacapsule0.5 mgoralNovartis Pharmaceuticals Canada Inc2011-03-28Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
GileniaNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Fingolimod Hydrochloride
162359-56-0
Thumb
  • InChI Key: SWZTYAVBMYWFGS-UHFFFAOYSA-N
  • Monoisotopic Mass: 343.227807044
  • Average Mass: 343.932
DBSALT000580
Categories
UNII3QN8BYN5QF
CAS number162359-55-9
WeightAverage: 307.4708
Monoisotopic: 307.251129305
Chemical FormulaC19H33NO2
InChI KeyKKGQTZUTZRNORY-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
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpropylamines. These are compounds containing a phenylpropylamine moiety, which consists of a phenyl group substituted at the third carbon by an propan-1-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylpropylamines
Direct ParentPhenylpropylamines
Alternative Parents
Substituents
  • Phenylpropylamine
  • Aralkylamine
  • 1,2-aminoalcohol
  • Hydrocarbon derivative
  • Primary amine
  • Primary alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFingolimod 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.
PharmacodynamicsFingolimod 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 actionFingolimod 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.
Related Articles
AbsorptionThe 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 eliminationNot Available
Half life6-9 days
Clearance

Fingolimod blood clearance is 6.3±2.3 L/h.

ToxicityBradyarrhythmia 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral.5 mg/1
Capsuleoral0.5 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5604229 No1999-02-182019-02-18Us
US6004565 No1997-09-232017-09-23Us
US8324283 No2006-03-292026-03-29Us
US9187405 No2007-06-252027-06-25Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
boiling point479.498 °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-4.7ALOGPS
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot 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
ATC CodesL04AA27
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (423 KB)
MSDSDownload (351 KB)
Interactions
Drug Interactions
Drug
2-Methoxyethanol2-Methoxyethanol may increase the immunosuppressive activities of Fingolimod.
9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine may increase the immunosuppressive activities of Fingolimod.
AbataceptAbatacept may increase the immunosuppressive activities of Fingolimod.
abetimusabetimus may increase the immunosuppressive activities of Fingolimod.
AbirateroneThe metabolism of Fingolimod can be decreased when combined with Abiraterone.
ABR-215757ABR-215757 may increase the immunosuppressive activities of Fingolimod.
AcebutololAcebutolol may increase the bradycardic activities of Fingolimod.
AdalimumabAdalimumab may increase the immunosuppressive activities of Fingolimod.
AfelimomabAfelimomab may increase the immunosuppressive activities of Fingolimod.
AjmalineFingolimod may increase the arrhythmogenic activities of Ajmaline.
AlefaceptAlefacept may increase the immunosuppressive activities of Fingolimod.
AlemtuzumabAlemtuzumab may increase the immunosuppressive activities of Fingolimod.
alicaforsenalicaforsen may increase the immunosuppressive activities of Fingolimod.
AlprenololAlprenolol may increase the bradycardic activities of Fingolimod.
AltretamineAltretamine may increase the immunosuppressive activities of Fingolimod.
AmiodaroneFingolimod may increase the arrhythmogenic activities of Amiodarone.
AmiodaroneAmiodarone may increase the bradycardic activities of Fingolimod.
AmsacrineAmsacrine may increase the immunosuppressive activities of Fingolimod.
AnagrelideFingolimod may increase the QTc-prolonging activities of Anagrelide.
AnakinraAnakinra may increase the immunosuppressive activities of Fingolimod.
Anti-thymocyte Globulin (Rabbit)Anti-thymocyte Globulin (Rabbit) may increase the immunosuppressive activities of Fingolimod.
ApremilastApremilast may increase the immunosuppressive activities of Fingolimod.
AprepitantThe serum concentration of Fingolimod can be increased when it is combined with Aprepitant.
ArotinololArotinolol may increase the bradycardic activities of Fingolimod.
Arsenic trioxideFingolimod may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherFingolimod may increase the QTc-prolonging activities of Artemether.
ArtemetherThe metabolism of Fingolimod can be decreased when combined with Artemether.
AsenapineFingolimod may increase the QTc-prolonging activities of Asenapine.
AtazanavirThe metabolism of Fingolimod can be decreased when combined with Atazanavir.
AtenololAtenolol may increase the bradycardic activities of Fingolimod.
AtomoxetineThe metabolism of Fingolimod can be decreased when combined with Atomoxetine.
AzacitidineAzacitidine may increase the immunosuppressive activities of Fingolimod.
AzathioprineAzathioprine may increase the immunosuppressive activities of Fingolimod.
AzithromycinFingolimod may increase the QTc-prolonging activities of Azithromycin.
BasiliximabBasiliximab may increase the immunosuppressive activities of Fingolimod.
BedaquilineFingolimod may increase the QTc-prolonging activities of Bedaquiline.
BefunololBefunolol may increase the bradycardic activities of Fingolimod.
BelataceptBelatacept may increase the immunosuppressive activities of Fingolimod.
BelimumabBelimumab may increase the immunosuppressive activities of Fingolimod.
BendroflumethiazideBendroflumethiazide may increase the bradycardic activities of Fingolimod.
BeractantBeractant may increase the bradycardic activities of Fingolimod.
BetamethasoneBetamethasone may increase the immunosuppressive activities of Fingolimod.
BetaxololBetaxolol may increase the bradycardic activities of Fingolimod.
BevantololBevantolol may increase the bradycardic activities of Fingolimod.
BexaroteneThe serum concentration of Fingolimod can be decreased when it is combined with Bexarotene.
BisoprololBisoprolol may increase the bradycardic activities of Fingolimod.
BleomycinBleomycin may increase the immunosuppressive activities of Fingolimod.
BlinatumomabBlinatumomab may increase the immunosuppressive activities of Fingolimod.
BoceprevirThe metabolism of Fingolimod can be decreased when combined with Boceprevir.
BopindololBopindolol may increase the bradycardic activities of Fingolimod.
BortezomibThe metabolism of Fingolimod can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Fingolimod can be decreased when it is combined with Bosentan.
Brentuximab vedotinBrentuximab vedotin may increase the immunosuppressive activities of Fingolimod.
BretyliumBretylium may increase the bradycardic activities of Fingolimod.
BriakinumabBriakinumab may increase the immunosuppressive activities of Fingolimod.
BudesonideBudesonide may increase the immunosuppressive activities of Fingolimod.
BufuralolBufuralol may increase the bradycardic activities of Fingolimod.
BupranololBupranolol may increase the bradycardic activities of Fingolimod.
BupropionThe metabolism of Fingolimod can be decreased when combined with Bupropion.
BusulfanBusulfan may increase the immunosuppressive activities of Fingolimod.
CabazitaxelCabazitaxel may increase the immunosuppressive activities of Fingolimod.
CalfactantCalfactant may increase the bradycardic activities of Fingolimod.
CanakinumabCanakinumab may increase the immunosuppressive activities of Fingolimod.
CapecitabineCapecitabine may increase the immunosuppressive activities of Fingolimod.
CarbamazepineThe serum concentration of Fingolimod can be decreased when it is combined with Carbamazepine.
CarboplatinCarboplatin may increase the immunosuppressive activities of Fingolimod.
CarmustineCarmustine may increase the immunosuppressive activities of Fingolimod.
CarteololCarteolol may increase the bradycardic activities of Fingolimod.
CarvedilolCarvedilol may increase the bradycardic activities of Fingolimod.
CastanospermineCastanospermine may increase the immunosuppressive activities of Fingolimod.
CelecoxibThe metabolism of Fingolimod can be decreased when combined with Celecoxib.
CeliprololCeliprolol may increase the bradycardic activities of Fingolimod.
CeritinibFingolimod may increase the bradycardic activities of Ceritinib.
CeritinibThe serum concentration of Fingolimod can be increased when it is combined with Ceritinib.
Certolizumab pegolCertolizumab pegol may increase the immunosuppressive activities of Fingolimod.
ChlorambucilChlorambucil may increase the immunosuppressive activities of Fingolimod.
ChloroquineFingolimod may increase the QTc-prolonging activities of Chloroquine.
ChloroquineThe metabolism of Fingolimod can be decreased when combined with Chloroquine.
ChlorpromazineFingolimod may increase the QTc-prolonging activities of Chlorpromazine.
ChlorpromazineThe metabolism of Fingolimod can be decreased when combined with Chlorpromazine.
CholecalciferolThe metabolism of Fingolimod can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Fingolimod can be decreased when combined with Cimetidine.
CinacalcetThe metabolism of Fingolimod can be decreased when combined with Cinacalcet.
CiprofloxacinFingolimod may increase the QTc-prolonging activities of Ciprofloxacin.
CisaprideFingolimod may increase the QTc-prolonging activities of Cisapride.
CisplatinCisplatin may increase the immunosuppressive activities of Fingolimod.
CitalopramFingolimod may increase the QTc-prolonging activities of Citalopram.
CitalopramThe metabolism of Fingolimod can be decreased when combined with Citalopram.
CladribineCladribine may increase the immunosuppressive activities of Fingolimod.
ClarithromycinFingolimod may increase the QTc-prolonging activities of Clarithromycin.
ClarithromycinThe metabolism of Fingolimod can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Fingolimod can be decreased when combined with Clemastine.
ClobazamThe metabolism of Fingolimod can be decreased when combined with Clobazam.
ClofarabineClofarabine may increase the immunosuppressive activities of Fingolimod.
ClomipramineThe metabolism of Fingolimod can be decreased when combined with Clomipramine.
ClonidineClonidine may increase the bradycardic activities of Fingolimod.
ClotrimazoleThe metabolism of Fingolimod can be decreased when combined with Clotrimazole.
ClozapineFingolimod may increase the QTc-prolonging activities of Clozapine.
ClozapineThe metabolism of Fingolimod can be decreased when combined with Clozapine.
CobicistatThe serum concentration of Fingolimod can be increased when it is combined with Cobicistat.
CocaineThe metabolism of Fingolimod can be decreased when combined with Cocaine.
ConivaptanThe serum concentration of Fingolimod can be increased when it is combined with Conivaptan.
CorticotropinCorticotropin may increase the immunosuppressive activities of Fingolimod.
Cortisone acetateCortisone acetate may increase the immunosuppressive activities of Fingolimod.
CrizotinibFingolimod may increase the QTc-prolonging activities of Crizotinib.
CrizotinibThe metabolism of Fingolimod can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the immunosuppressive activities of Fingolimod.
CyclosporineThe metabolism of Fingolimod can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Fingolimod can be decreased when it is combined with Cyproterone acetate.
CytarabineCytarabine may increase the immunosuppressive activities of Fingolimod.
DabrafenibThe serum concentration of Fingolimod can be decreased when it is combined with Dabrafenib.
DacarbazineDacarbazine may increase the immunosuppressive activities of Fingolimod.
DaclizumabDaclizumab may increase the immunosuppressive activities of Fingolimod.
DactinomycinDactinomycin may increase the immunosuppressive activities of Fingolimod.
DarifenacinThe metabolism of Fingolimod can be decreased when combined with Darifenacin.
DarunavirThe serum concentration of Fingolimod can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Fingolimod can be increased when it is combined with Dasatinib.
DaunorubicinDaunorubicin may increase the immunosuppressive activities of Fingolimod.
DeferasiroxThe serum concentration of Fingolimod can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Fingolimod can be decreased when combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Fingolimod.
DesipramineThe metabolism of Fingolimod can be decreased when combined with Desipramine.
DexamethasoneThe serum concentration of Fingolimod can be decreased when it is combined with Dexamethasone.
DexmedetomidineDexmedetomidine may increase the bradycardic activities of Fingolimod.
DigoxinDigoxin may increase the bradycardic activities of Fingolimod.
DihydroergotamineThe metabolism of Fingolimod can be decreased when combined with Dihydroergotamine.
DiltiazemDiltiazem may increase the bradycardic activities of Fingolimod.
Dimethyl fumarateDimethyl fumarate may increase the immunosuppressive activities of Fingolimod.
DinutuximabDinutuximab may increase the immunosuppressive activities of Fingolimod.
DiphenhydramineThe metabolism of Fingolimod can be decreased when combined with Diphenhydramine.
DisopyramideFingolimod may increase the arrhythmogenic activities of Disopyramide.
DisulfiramThe metabolism of Fingolimod can be decreased when combined with Disulfiram.
DocetaxelDocetaxel may increase the immunosuppressive activities of Fingolimod.
DofetilideFingolimod may increase the arrhythmogenic activities of Dofetilide.
DolasetronFingolimod may increase the QTc-prolonging activities of Dolasetron.
DomperidoneFingolimod may increase the QTc-prolonging activities of Domperidone.
DonepezilDonepezil may increase the bradycardic activities of Fingolimod.
DoxorubicinDoxorubicin may increase the immunosuppressive activities of Fingolimod.
DoxycyclineThe metabolism of Fingolimod can be decreased when combined with Doxycycline.
DronedaroneFingolimod may increase the arrhythmogenic activities of Dronedarone.
DronedaroneThe metabolism of Fingolimod can be decreased when combined with Dronedarone.
DroperidolFingolimod may increase the QTc-prolonging activities of Droperidol.
DuloxetineThe metabolism of Fingolimod can be decreased when combined with Duloxetine.
EculizumabEculizumab may increase the immunosuppressive activities of Fingolimod.
EfalizumabEfalizumab may increase the immunosuppressive activities of Fingolimod.
EfavirenzThe serum concentration of Fingolimod can be decreased when it is combined with Efavirenz.
EliglustatFingolimod may increase the QTc-prolonging activities of Eliglustat.
EliglustatThe metabolism of Fingolimod can be decreased when combined with Eliglustat.
EnzalutamideThe serum concentration of Fingolimod can be decreased when it is combined with Enzalutamide.
EpirubicinEpirubicin may increase the immunosuppressive activities of Fingolimod.
ErythromycinFingolimod may increase the QTc-prolonging activities of Erythromycin.
ErythromycinThe metabolism of Fingolimod can be decreased when combined with Erythromycin.
EscitalopramFingolimod may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Fingolimod can be decreased when it is combined with Eslicarbazepine acetate.
EsmololEsmolol may increase the bradycardic activities of Fingolimod.
EstramustineEstramustine may increase the immunosuppressive activities of Fingolimod.
EtanerceptEtanercept may increase the immunosuppressive activities of Fingolimod.
EtoposideEtoposide may increase the immunosuppressive activities of Fingolimod.
EtravirineThe serum concentration of Fingolimod can be decreased when it is combined with Etravirine.
EverolimusEverolimus may increase the immunosuppressive activities of Fingolimod.
FlecainideFingolimod may increase the QTc-prolonging activities of Flecainide.
FloxuridineFloxuridine may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe metabolism of Fingolimod can be decreased when combined with Fluconazole.
FludarabineFludarabine may increase the immunosuppressive activities of Fingolimod.
FludrocortisoneFludrocortisone may increase the immunosuppressive activities of Fingolimod.
FluorouracilFluorouracil may increase the immunosuppressive activities of Fingolimod.
FluoxetineFingolimod may increase the QTc-prolonging activities of Fluoxetine.
FluoxetineThe metabolism of Fingolimod can be decreased when combined with Fluoxetine.
FlupentixolFingolimod may increase the QTc-prolonging activities of Flupentixol.
FluvoxamineThe metabolism of Fingolimod can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Fingolimod can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Fingolimod can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Fingolimod can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Fingolimod can be increased when it is combined with Fusidic Acid.
Gadobenic acidFingolimod may increase the QTc-prolonging activities of Gadobenic acid.
GalantamineGalantamine may increase the bradycardic activities of Fingolimod.
Gallium nitrateGallium nitrate may increase the immunosuppressive activities of Fingolimod.
GemcitabineGemcitabine may increase the immunosuppressive activities of Fingolimod.
GemifloxacinFingolimod may increase the QTc-prolonging activities of Gemifloxacin.
Gemtuzumab ozogamicinGemtuzumab ozogamicin may increase the immunosuppressive activities of Fingolimod.
Glatiramer AcetateGlatiramer Acetate may increase the immunosuppressive activities of Fingolimod.
GlimepirideGlimepiride may increase the immunosuppressive activities of Fingolimod.
GolimumabGolimumab may increase the immunosuppressive activities of Fingolimod.
GoserelinFingolimod may increase the QTc-prolonging activities of Goserelin.
GranisetronFingolimod may increase the QTc-prolonging activities of Granisetron.
GuanfacineGuanfacine may increase the bradycardic activities of Fingolimod.
HaloperidolFingolimod may increase the QTc-prolonging activities of Haloperidol.
HaloperidolThe metabolism of Fingolimod can be decreased when combined with Haloperidol.
HydrocortisoneHydrocortisone may increase the immunosuppressive activities of Fingolimod.
HydroxyureaHydroxyurea may increase the immunosuppressive activities of Fingolimod.
Ibritumomab tiuxetanIbritumomab tiuxetan may increase the immunosuppressive activities of Fingolimod.
IbrutinibIbrutinib may increase the immunosuppressive activities of Fingolimod.
IbutilideFingolimod may increase the arrhythmogenic activities of Ibutilide.
IcatibantIcatibant may increase the immunosuppressive activities of Fingolimod.
IdarubicinIdarubicin may increase the immunosuppressive activities of Fingolimod.
IdelalisibThe serum concentration of Fingolimod can be increased when it is combined with Idelalisib.
IfosfamideIfosfamide may increase the immunosuppressive activities of Fingolimod.
IloperidoneFingolimod may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Fingolimod can be decreased when combined with Imatinib.
ImipramineThe metabolism of Fingolimod can be decreased when combined with Imipramine.
ImiquimodImiquimod may increase the immunosuppressive activities of Fingolimod.
IndenololIndenolol may increase the bradycardic activities of Fingolimod.
IndinavirThe metabolism of Fingolimod can be decreased when combined with Indinavir.
InfliximabInfliximab may increase the immunosuppressive activities of Fingolimod.
IrinotecanIrinotecan may increase the immunosuppressive activities of Fingolimod.
IsavuconazoniumThe metabolism of Fingolimod can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Fingolimod can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Fingolimod can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Fingolimod can be decreased when combined with Itraconazole.
IvabradineFingolimod may increase the bradycardic activities of Ivabradine.
IvacaftorThe serum concentration of Fingolimod can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of the active metabolites of Fingolimod can be increased when Fingolimod is used in combination with Ketoconazole.
L-PhenylalanineL-Phenylalanine may increase the immunosuppressive activities of Fingolimod.
LabetalolLabetalol may increase the bradycardic activities of Fingolimod.
LacosamideFingolimod may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LanreotideLanreotide may increase the bradycardic activities of Fingolimod.
LeflunomideThe risk or severity of adverse effects can be increased when Fingolimod is combined with Leflunomide.
LeflunomideLeflunomide may increase the immunosuppressive activities of Fingolimod.
LenalidomideLenalidomide may increase the immunosuppressive activities of Fingolimod.
LenvatinibFingolimod may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideFingolimod may increase the QTc-prolonging activities of Leuprolide.
LevobunololLevobunolol may increase the bradycardic activities of Fingolimod.
LevofloxacinFingolimod may increase the QTc-prolonging activities of Levofloxacin.
LomustineLomustine may increase the immunosuppressive activities of Fingolimod.
LopinavirThe metabolism of Fingolimod can be decreased when combined with Lopinavir.
LopinavirFingolimod may increase the QTc-prolonging activities of Lopinavir.
LorcaserinThe metabolism of Fingolimod can be decreased when combined with Lorcaserin.
LovastatinThe metabolism of Fingolimod can be decreased when combined with Lovastatin.
LucinactantLucinactant may increase the bradycardic activities of Fingolimod.
LuliconazoleThe serum concentration of Fingolimod can be increased when it is combined with Luliconazole.
LumefantrineFingolimod may increase the QTc-prolonging activities of Lumefantrine.
LumefantrineThe metabolism of Fingolimod can be decreased when combined with Lumefantrine.
MechlorethamineMechlorethamine may increase the immunosuppressive activities of Fingolimod.
MelphalanMelphalan may increase the immunosuppressive activities of Fingolimod.
MepolizumabMepolizumab may increase the immunosuppressive activities of Fingolimod.
MercaptopurineMercaptopurine may increase the immunosuppressive activities of Fingolimod.
MethadoneFingolimod may increase the QTc-prolonging activities of Methadone.
MethadoneThe metabolism of Fingolimod can be decreased when combined with Methadone.
MethotrexateMethotrexate may increase the immunosuppressive activities of Fingolimod.
MethotrimeprazineThe metabolism of Fingolimod can be decreased when combined with Methotrimeprazine.
MethyldopaMethyldopa may increase the bradycardic activities of Fingolimod.
MethylprednisoloneMethylprednisolone may increase the immunosuppressive activities of Fingolimod.
MetipranololMetipranolol may increase the bradycardic activities of Fingolimod.
MetoprololMetoprolol may increase the bradycardic activities of Fingolimod.
MifepristoneThe metabolism of Fingolimod can be decreased when combined with Mifepristone.
MifepristoneFingolimod may increase the QTc-prolonging activities of Mifepristone.
MirabegronThe metabolism of Fingolimod can be decreased when combined with Mirabegron.
MitomycinMitomycin may increase the immunosuppressive activities of Fingolimod.
MitotaneThe serum concentration of Fingolimod can be decreased when it is combined with Mitotane.
MitoxantroneMitoxantrone may increase the immunosuppressive activities of Fingolimod.
ModafinilThe serum concentration of Fingolimod can be decreased when it is combined with Modafinil.
MoxifloxacinFingolimod may increase the QTc-prolonging activities of Moxifloxacin.
MuromonabMuromonab may increase the immunosuppressive activities of Fingolimod.
Mycophenolate mofetilMycophenolate mofetil may increase the immunosuppressive activities of Fingolimod.
Mycophenolic acidMycophenolic acid may increase the immunosuppressive activities of Fingolimod.
NadololNadolol may increase the bradycardic activities of Fingolimod.
NafcillinThe serum concentration of Fingolimod can be decreased when it is combined with Nafcillin.
NatalizumabThe risk or severity of adverse effects can be increased when Fingolimod is combined with Natalizumab.
NatalizumabNatalizumab may increase the immunosuppressive activities of Fingolimod.
NebivololNebivolol may increase the bradycardic activities of Fingolimod.
NefazodoneThe metabolism of Fingolimod can be decreased when combined with Nefazodone.
NelarabineNelarabine may increase the immunosuppressive activities of Fingolimod.
NelfinavirThe metabolism of Fingolimod can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Fingolimod can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Fingolimod can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Fingolimod can be decreased when combined with Nicardipine.
NicotineThe metabolism of Fingolimod can be decreased when combined with Nicotine.
NilotinibThe metabolism of Fingolimod can be decreased when combined with Nilotinib.
NilotinibFingolimod may increase the QTc-prolonging activities of Nilotinib.
ObinutuzumabObinutuzumab may increase the immunosuppressive activities of Fingolimod.
OctreotideOctreotide may increase the bradycardic activities of Fingolimod.
OfloxacinFingolimod may increase the QTc-prolonging activities of Ofloxacin.
OlaparibThe metabolism of Fingolimod can be decreased when combined with Olaparib.
OndansetronFingolimod may increase the QTc-prolonging activities of Ondansetron.
OsimertinibThe serum concentration of Fingolimod can be increased when it is combined with Osimertinib.
OxaliplatinOxaliplatin may increase the immunosuppressive activities of Fingolimod.
OxprenololOxprenolol may increase the bradycardic activities of Fingolimod.
PaclitaxelPaclitaxel may increase the immunosuppressive activities of Fingolimod.
PalbociclibThe serum concentration of Fingolimod can be increased when it is combined with Palbociclib.
PaliperidoneFingolimod may increase the QTc-prolonging activities of Paliperidone.
PanobinostatFingolimod may increase the QTc-prolonging activities of Panobinostat.
PanobinostatThe metabolism of Fingolimod can be decreased when combined with Panobinostat.
ParoxetineThe metabolism of Fingolimod can be decreased when combined with Paroxetine.
PasireotidePasireotide may increase the bradycardic activities of Fingolimod.
PazopanibPazopanib may increase the immunosuppressive activities of Fingolimod.
PazopanibFingolimod may increase the QTc-prolonging activities of Pazopanib.
PegaspargasePegaspargase may increase the immunosuppressive activities of Fingolimod.
Peginterferon alfa-2bThe serum concentration of Fingolimod can be decreased when it is combined with Peginterferon alfa-2b.
PemetrexedPemetrexed may increase the immunosuppressive activities of Fingolimod.
PenbutololPenbutolol may increase the bradycardic activities of Fingolimod.
PentamidineFingolimod may increase the QTc-prolonging activities of Pentamidine.
PentobarbitalThe metabolism of Fingolimod can be increased when combined with Pentobarbital.
PentostatinPentostatin may increase the immunosuppressive activities of Fingolimod.
PerflutrenFingolimod may increase the QTc-prolonging activities of Perflutren.
PhenobarbitalThe metabolism of Fingolimod can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Fingolimod can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Fingolimod.
PimozideFingolimod may increase the QTc-prolonging activities of Pimozide.
PindololPindolol may increase the bradycardic activities of Fingolimod.
PirfenidonePirfenidone may increase the immunosuppressive activities of Fingolimod.
PomalidomidePomalidomide may increase the immunosuppressive activities of Fingolimod.
Poractant alfaFingolimod may increase the bradycardic activities of Poractant alfa.
PosaconazoleThe metabolism of Fingolimod can be decreased when combined with Posaconazole.
PractololPractolol may increase the bradycardic activities of Fingolimod.
PralatrexatePralatrexate may increase the immunosuppressive activities of Fingolimod.
PrednisolonePrednisolone may increase the immunosuppressive activities of Fingolimod.
PrednisonePrednisone may increase the immunosuppressive activities of Fingolimod.
PrimaquineFingolimod may increase the QTc-prolonging activities of Primaquine.
PrimidoneThe metabolism of Fingolimod can be increased when combined with Primidone.
ProcainamideFingolimod may increase the arrhythmogenic activities of Procainamide.
ProcarbazineProcarbazine may increase the immunosuppressive activities of Fingolimod.
PromazineFingolimod may increase the QTc-prolonging activities of Promazine.
PromazineThe metabolism of Fingolimod can be decreased when combined with Promazine.
PropafenoneFingolimod may increase the QTc-prolonging activities of Propafenone.
PropafenonePropafenone may increase the bradycardic activities of Fingolimod.
PropranololPropranolol may increase the bradycardic activities of Fingolimod.
QuetiapineFingolimod may increase the QTc-prolonging activities of Quetiapine.
QuinidineFingolimod may increase the arrhythmogenic activities of Quinidine.
QuinidineThe metabolism of Fingolimod can be decreased when combined with Quinidine.
QuinineFingolimod may increase the QTc-prolonging activities of Quinine.
QuinineThe metabolism of Fingolimod can be decreased when combined with Quinine.
Rabies vaccineThe risk or severity of adverse effects can be increased when Fingolimod is combined with Rabies vaccine.
RanolazineThe metabolism of Fingolimod can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Fingolimod can be increased when combined with Rifabutin.
RifampicinThe metabolism of Fingolimod can be increased when combined with Rifampicin.
RifapentineThe metabolism of Fingolimod can be increased when combined with Rifapentine.
RilonaceptRilonacept may increase the immunosuppressive activities of Fingolimod.
RitonavirThe metabolism of Fingolimod can be decreased when combined with Ritonavir.
RituximabRituximab may increase the immunosuppressive activities of Fingolimod.
RivastigmineRivastigmine may increase the bradycardic activities of Fingolimod.
RoflumilastRoflumilast may increase the immunosuppressive activities of Fingolimod.
RolapitantThe metabolism of Fingolimod can be decreased when combined with Rolapitant.
RopiniroleThe metabolism of Fingolimod can be decreased when combined with Ropinirole.
RuxolitinibRuxolitinib may increase the bradycardic activities of Fingolimod.
SaquinavirFingolimod may increase the QTc-prolonging activities of Saquinavir.
SaquinavirThe metabolism of Fingolimod can be decreased when combined with Saquinavir.
SecukinumabSecukinumab may increase the immunosuppressive activities of Fingolimod.
SeocalcitolSeocalcitol may increase the immunosuppressive activities of Fingolimod.
SertralineThe metabolism of Fingolimod can be decreased when combined with Sertraline.
SildenafilThe metabolism of Fingolimod can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Fingolimod can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Fingolimod can be increased when it is combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Fingolimod.
SirolimusSirolimus may increase the immunosuppressive activities of Fingolimod.
SorafenibSorafenib may increase the immunosuppressive activities of Fingolimod.
SotalolSotalol may increase the bradycardic activities of Fingolimod.
SparteineFingolimod may increase the arrhythmogenic activities of Sparteine.
St. John's WortThe serum concentration of Fingolimod can be decreased when it is combined with St. John's Wort.
SteproninStepronin may increase the immunosuppressive activities of Fingolimod.
StiripentolThe serum concentration of Fingolimod can be increased when it is combined with Stiripentol.
StreptozocinStreptozocin may increase the immunosuppressive activities of Fingolimod.
SufentanilSufentanil may increase the bradycardic activities of Fingolimod.
SulfisoxazoleFingolimod may increase the QTc-prolonging activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Fingolimod can be decreased when combined with Sulfisoxazole.
SunitinibSunitinib may increase the immunosuppressive activities of Fingolimod.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fingolimod.
TedisamilFingolimod may increase the arrhythmogenic activities of Tedisamil.
TelaprevirThe metabolism of Fingolimod can be decreased when combined with Telaprevir.
TelavancinFingolimod may increase the QTc-prolonging activities of Telavancin.
TelithromycinFingolimod may increase the QTc-prolonging activities of Telithromycin.
TelithromycinThe metabolism of Fingolimod can be decreased when combined with Telithromycin.
TemozolomideTemozolomide may increase the immunosuppressive activities of Fingolimod.
TemsirolimusTemsirolimus may increase the immunosuppressive activities of Fingolimod.
TeniposideTeniposide may increase the immunosuppressive activities of Fingolimod.
TepoxalinTepoxalin may increase the immunosuppressive activities of Fingolimod.
TerbinafineThe metabolism of Fingolimod can be decreased when combined with Terbinafine.
TeriflunomideTeriflunomide may increase the immunosuppressive activities of Fingolimod.
TetrabenazineFingolimod may increase the QTc-prolonging activities of Tetrabenazine.
ThalidomideThalidomide may increase the immunosuppressive activities of Fingolimod.
ThioridazineFingolimod may increase the QTc-prolonging activities of Thioridazine.
ThioridazineThe metabolism of Fingolimod can be decreased when combined with Thioridazine.
ThiotepaThiotepa may increase the immunosuppressive activities of Fingolimod.
TiclopidineThe metabolism of Fingolimod can be decreased when combined with Ticlopidine.
TimololTimolol may increase the bradycardic activities of Fingolimod.
TioguanineTioguanine may increase the immunosuppressive activities of Fingolimod.
TipranavirThe metabolism of Fingolimod can be decreased when combined with Tipranavir.
TizanidineTizanidine may increase the bradycardic activities of Fingolimod.
TocilizumabThe serum concentration of Fingolimod can be decreased when it is combined with Tocilizumab.
TofacitinibFingolimod may increase the immunosuppressive activities of Tofacitinib.
TofacitinibTofacitinib may increase the bradycardic activities of Fingolimod.
TopotecanTopotecan may increase the immunosuppressive activities of Fingolimod.
ToremifeneFingolimod may increase the QTc-prolonging activities of Toremifene.
TositumomabTositumomab may increase the immunosuppressive activities of Fingolimod.
TrabectedinTrabectedin may increase the immunosuppressive activities of Fingolimod.
TranylcypromineThe metabolism of Fingolimod can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the neutropenic activities of Fingolimod.
Trastuzumab emtansineTrastuzumab emtansine may increase the immunosuppressive activities of Fingolimod.
TretinoinTretinoin may increase the immunosuppressive activities of Fingolimod.
TriamcinoloneTriamcinolone may increase the immunosuppressive activities of Fingolimod.
UstekinumabUstekinumab may increase the immunosuppressive activities of Fingolimod.
VandetanibFingolimod may increase the QTc-prolonging activities of Vandetanib.
VedolizumabVedolizumab may increase the immunosuppressive activities of Fingolimod.
VemurafenibFingolimod may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Fingolimod can be decreased when combined with Venlafaxine.
VerapamilVerapamil may increase the bradycardic activities of Fingolimod.
VilanterolVilanterol may increase the immunosuppressive activities of Fingolimod.
VinblastineVinblastine may increase the immunosuppressive activities of Fingolimod.
VincristineVincristine may increase the immunosuppressive activities of Fingolimod.
VindesineVindesine may increase the immunosuppressive activities of Fingolimod.
VinorelbineVinorelbine may increase the immunosuppressive activities of Fingolimod.
VoriconazoleThe metabolism of Fingolimod can be decreased when combined with Voriconazole.
ZiprasidoneThe metabolism of Fingolimod can be decreased when combined with Ziprasidone.
ZiprasidoneFingolimod may increase the QTc-prolonging activities of Ziprasidone.
ZuclopenthixolFingolimod may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

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 the G(i/0)alpha and G(12) subclass of heteromeric G-proteins (By similarity). May play a regulatory role in the transformation of radial glial cells into astrocytes and may affect proliferative activ...
Gene Name:
S1PR5
Uniprot ID:
Q9H228
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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
CYP4F2
Uniprot ID:
P78329
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 extent sphinganine, but not other lipids, such as D,L-threo-dihydrosphingosine, N,N-dimethylsphingosine, diacylglycerol, ceramide, or phosphatidylinositol.
Gene Name:
SPHK1
Uniprot ID:
Q9NYA1
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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
Molecular Weight:
60269.165 Da
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Drug created on April 28, 2013 14:17 / Updated on August 30, 2016 02:12