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Identification
NameFingolimod
Accession NumberDB08868
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionFingolimod 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
GilenyaCapsule0.5 mgOralNovartis Europharm Ltd2011-03-17Not applicableEu
GilenyaCapsule.5 mg/1OralNovartis Pharmaceuticals Corporation2010-09-21Not applicableUs
GilenyaCapsule0.5 mgOralNovartis Europharm Ltd2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Pharmaceuticals Canada Inc2011-03-28Not applicableCanada
GilenyaCapsule0.5 mgOralNovartis Europharm Ltd2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Ltd2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Ltd2011-03-17Not applicableEu
GilenyaCapsule0.5 mgOralNovartis Europharm Ltd2011-03-17Not applicableEu
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
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.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Sphingosine 1-phosphate receptor 5Proteinyes
modulator
HumanQ9H228 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
2-Methoxyethanol2-Methoxyethanol may increase the immunosuppressive activities of Fingolimod.Experimental
9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine may increase the immunosuppressive activities of Fingolimod.Investigational
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
ABR-215757ABR-215757 may increase the immunosuppressive activities of Fingolimod.Investigational
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
Adefovir DipivoxilAdefovir Dipivoxil may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
AfelimomabAfelimomab may increase the immunosuppressive activities of Fingolimod.Investigational
AjmalineFingolimod may increase the arrhythmogenic activities of Ajmaline.Approved
AlefaceptAlefacept may increase the immunosuppressive activities of Fingolimod.Approved, 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
ALT-110The risk or severity of adverse effects can be increased when Fingolimod is combined with ALT-110.Investigational
AltretamineAltretamine may increase the immunosuppressive activities of Fingolimod.Approved
Amg 827Amg 827 may increase the immunosuppressive activities of Fingolimod.Investigational
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
Anti-thymocyte Globulin (Rabbit)Anti-thymocyte Globulin (Rabbit) may increase the immunosuppressive activities of Fingolimod.Approved
Aop200704Aop200704 may increase the bradycardic activities of Fingolimod.Investigational
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
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
BcgThe therapeutic efficacy of Bcg 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
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.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
BexaroteneThe serum concentration of Fingolimod can be decreased when it is combined with Bexarotene.Approved, Investigational
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
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
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
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
C1 Esterase Inhibitor (Human)C1 Esterase Inhibitor (Human) may increase the immunosuppressive activities of Fingolimod.Approved
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
CDX-110The risk or severity of adverse effects can be increased when Fingolimod is combined with CDX-110.Investigational
CelecoxibThe metabolism of Fingolimod can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololCeliprolol may increase the bradycardic activities of Fingolimod.Approved, Investigational
CeritinibFingolimod may increase the bradycardic activities of 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
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
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
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
DisulfiramThe metabolism of Fingolimod can be decreased when combined with Disulfiram.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
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
EfavirenzThe serum concentration of Fingolimod can be decreased when it is combined with Efavirenz.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
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
Eslicarbazepine acetateThe serum concentration of Fingolimod can be decreased when it is combined with Eslicarbazepine acetate.Approved
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
EtravirineThe serum concentration of Fingolimod can be decreased when it is combined with Etravirine.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 risk or severity of adverse effects can be increased when Fingolimod is combined with G17DT.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, Investigational, Withdrawn
GI-5005The risk or severity of adverse effects can be increased when Fingolimod is combined with GI-5005.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
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
HydrocortisoneHydrocortisone may increase the immunosuppressive activities of Fingolimod.Approved, Vet Approved
HydroxyureaHydroxyurea may increase the immunosuppressive activities of Fingolimod.Approved
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
IdelalisibThe serum concentration of Fingolimod can be increased when it is combined with Idelalisib.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 risk or severity of adverse effects can be increased when Fingolimod is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Fingolimod is combined with INGN 225.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 metabolism of Fingolimod can be decreased when combined with Ketoconazole.Approved, Investigational
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
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
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
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
Lx211Lx211 may increase the immunosuppressive activities of Fingolimod.Investigational
MechlorethamineMechlorethamine may increase the immunosuppressive activities of Fingolimod.Approved
MelphalanMelphalan may increase the immunosuppressive activities of Fingolimod.Approved
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
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
ModafinilThe serum concentration of Fingolimod can be decreased when it is combined with Modafinil.Approved, 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.Investigational
NafcillinThe serum concentration of Fingolimod can be decreased when it is combined with Nafcillin.Approved
NatalizumabThe risk or severity of adverse effects can be increased when Fingolimod is combined with Natalizumab.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
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
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with 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.Investigational
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
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 vaccineThe risk or severity of adverse effects can be increased when Fingolimod is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine 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
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
RuxolitinibRuxolitinib may increase the immunosuppressive activities of Fingolimod.Approved
SaquinavirThe metabolism of Fingolimod can be decreased when combined with Saquinavir.Approved, Investigational
SecukinumabSecukinumab may increase the immunosuppressive activities of Fingolimod.Approved
SeocalcitolSeocalcitol may increase the immunosuppressive activities of Fingolimod.Experimental
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 risk or severity of adverse effects can be increased when Fingolimod is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Fingolimod can be decreased when it is combined with St. John's Wort.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
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Fingolimod.Approved, Investigational
TacrolimusTacrolimus may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
TedisamilFingolimod may increase the arrhythmogenic activities of Tedisamil.Investigational
TelaprevirThe metabolism of Fingolimod can be decreased when combined with Telaprevir.Approved
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
TetrabenazineFingolimod may increase the QTc-prolonging activities of Tetrabenazine.Approved
TG4010The risk or severity of adverse effects can be increased when Fingolimod is combined with TG4010.Investigational
ThalidomideThalidomide may increase the immunosuppressive activities of Fingolimod.Approved, Investigational, Withdrawn
ThioridazineFingolimod may increase the QTc-prolonging activities of Thioridazine.Approved
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
TofacitinibFingolimod may increase the immunosuppressive activities of Tofacitinib.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
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
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
VinorelbineVinorelbine may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
VoriconazoleThe metabolism of Fingolimod can be decreased when combined with Voriconazole.Approved, Investigational
ZiprasidoneFingolimod may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolFingolimod may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot 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)
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
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

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
Comments
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Drug created on April 28, 2013 14:17 / Updated on December 09, 2016 02:39