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Identification
NameEliglustat
Accession NumberDB09039
TypeSmall Molecule
GroupsApproved
DescriptionEliglustat, marketed by Genzyme as CERDELGA, is a glucosylceramide synthase inhibitor indicated for the long-term treatment of type 1 Gaucher disease. Patients selected for treatment with Eliglustat undergo an FDA approved genotype test to establish if they are CYP2D6 EM (extensive metabolizers), IM (intermediate metabolizers), or PM (poor metabolizers), as the results of this test dictate the dosage of Eliglustat recommended. Eliglustat was approved for use by the FDA in August 2014.
Structure
Thumb
Synonyms
N-[(1R,2R)-1-(2,3-Dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-(1-pyrrolidinyl)-2-propanyl]octanamide
External Identifiers
  • A16AX10
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CerdelgaCapsule84 mg/1OralGenzyme Corporation2014-09-03Not applicableUs
CerdelgaCapsule84 mgOralGenzyme Europe Bv2015-01-19Not applicableEu
CerdelgaCapsule84 mgOralGenzyme Europe Bv2015-01-19Not applicableEu
CerdelgaCapsule84 mgOralGenzyme Europe Bv2015-01-19Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
eliglustat tartrate
ThumbNot applicableDBSALT001106
Categories
UNIIDR40J4WA67
CAS number491833-29-5
WeightAverage: 404.551
Monoisotopic: 404.267507647
Chemical FormulaC23H36N2O4
InChI KeyFJZZPCZKBUKGGU-AUSIDOKSSA-N
InChI
InChI=1S/C23H36N2O4/c1-2-3-4-5-6-9-22(26)24-19(17-25-12-7-8-13-25)23(27)18-10-11-20-21(16-18)29-15-14-28-20/h10-11,16,19,23,27H,2-9,12-15,17H2,1H3,(H,24,26)/t19-,23-/m1/s1
IUPAC Name
N-[(1R,2R)-1-(2,3-dihydro-1,4-benzodioxin-6-yl)-1-hydroxy-3-(pyrrolidin-1-yl)propan-2-yl]octanimidic acid
SMILES
[H][C@](CN1CCCC1)(N=C(O)CCCCCCC)[C@]([H])(O)C1=CC2=C(OCCO2)C=C1
Pharmacology
IndicationEliglustat is indicated for the long-term treatment of type 1 Gaucher disease in patients who are CYP2D6 extensive metabolizers (EMs), intermediate metabolizers (IMs), or poor metabolizers (PMs) in treatment-naive and treatment-experienced adult patients.
Structured Indications
PharmacodynamicsAccording to pharmacokinetic and pharmacodynamic modelling, plasma concentrations of 500ng/mL of eliglustat are predicted to increase mean concentration in the PR, QRS, and QTcF intervals of 22, 7, and 13 msec, respectively. (Taken from Cerdelga prescribing information).
Mechanism of actionEliglustat is a glucosylceramide synthase (IC50 = 10 ng/mL) specific inhibitor that acts as a substrate inhibitor of glucosylceramide.
TargetKindPharmacological actionActionsOrganismUniProt ID
Ceramide glucosyltransferaseProteinyes
antagonist
HumanQ16739 details
Related Articles
AbsorptionIn CYP2D6 EMs (extensive metabolizers), median time to reach maximum plasma concentrations (tmax) occurs at 1.5 to 2 hours following multiple doses of eliglustat 84 mg twice daily.
Volume of distribution

835 L in CYP2D6 EMs (extensive metabolizers).

Protein binding76 to 83%.
Metabolism

Extensively metabolized, primarily by CYP2D6 and less so by CYP3A4. No active metabolites have been identified.

Route of eliminationUrine (41.8%) and feces (51.4%), mainly as metabolites after oral administration.
Half life6.5 hours in EM (extensive metabolizers) and 8.9 hours in PM (poor metabolizers).
Clearance

88 L/h (8.8%) in CYP2D6 EM (extensive metabolizers).

ToxicityIn rats, eliglustat increased pre-implantation loss at 30 and 100 mg/kg/day. In male mature rats, eliglustat showed reversible adverse affects on sperm morphology, germ cell necrosis, and sloughed cells in the epididymis.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Eliglustat.Experimental, Illicit
AbirateroneThe serum concentration of Eliglustat can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Eliglustat.Approved
AcetylcholineThe metabolism of Acetylcholine can be decreased when combined with Eliglustat.Approved
AjmalineThe metabolism of Ajmaline can be decreased when combined with Eliglustat.Approved
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Eliglustat.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Eliglustat.Approved
AlprenololThe metabolism of Alprenolol can be decreased when combined with Eliglustat.Approved, Withdrawn
AmantadineAmantadine may increase the QTc-prolonging activities of Eliglustat.Approved
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Eliglustat.Approved, Withdrawn
AmiodaroneThe serum concentration of Eliglustat can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Eliglustat.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Eliglustat.Approved
AmphetamineThe metabolism of Amphetamine can be decreased when combined with Eliglustat.Approved, Illicit
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Eliglustat.Approved
AmsacrineThe metabolism of Amsacrine can be decreased when combined with Eliglustat.Approved
AnagrelideAnagrelide may increase the QTc-prolonging activities of Eliglustat.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Eliglustat.Approved
ApomorphineApomorphine may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
AprepitantThe serum concentration of Eliglustat can be increased when it is combined with Aprepitant.Approved, Investigational
AprindineThe metabolism of Aprindine can be decreased when combined with Eliglustat.Approved
ArformoterolArformoterol may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Eliglustat.Approved, Investigational
Arsenic trioxideArsenic trioxide may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
ArtemetherThe serum concentration of Eliglustat can be increased when it is combined with Artemether.Approved
AsenapineAsenapine may increase the QTc-prolonging activities of Eliglustat.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Eliglustat.Approved, Withdrawn
AtazanavirThe serum concentration of Eliglustat can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Eliglustat can be increased when it is combined with Atomoxetine.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Eliglustat.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Eliglustat.Approved
BedaquilineBedaquiline may increase the QTc-prolonging activities of Eliglustat.Approved
BenzatropineThe metabolism of Benzatropine can be decreased when combined with Eliglustat.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Eliglustat.Approved
BepridilThe metabolism of Bepridil can be decreased when combined with Eliglustat.Approved, Withdrawn
BetaxololThe serum concentration of Eliglustat can be increased when it is combined with Betaxolol.Approved
BexaroteneThe serum concentration of Eliglustat can be decreased when it is combined with Bexarotene.Approved, Investigational
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Eliglustat.Approved
BoceprevirThe serum concentration of Eliglustat can be increased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Eliglustat can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Eliglustat can be decreased when it is combined with Bosentan.Approved, Investigational
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Eliglustat.Approved
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Eliglustat.Approved
BufuralolThe metabolism of Bufuralol can be decreased when combined with Eliglustat.Experimental, Investigational
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Eliglustat.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Eliglustat.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of Eliglustat can be increased when it is combined with Bupropion.Approved
BuserelinBuserelin may increase the QTc-prolonging activities of Eliglustat.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Eliglustat.Approved, Investigational
CaffeineThe metabolism of Caffeine can be decreased when combined with Eliglustat.Approved
CaptoprilThe metabolism of Captopril can be decreased when combined with Eliglustat.Approved
CarbamazepineThe serum concentration of Eliglustat can be decreased when it is combined with Carbamazepine.Approved, Investigational
CariprazineThe metabolism of Cariprazine can be decreased when combined with Eliglustat.Approved
CarteololThe metabolism of Carteolol can be decreased when combined with Eliglustat.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Eliglustat.Approved, Investigational
CelecoxibThe serum concentration of Eliglustat can be increased when it is combined with Celecoxib.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Eliglustat.Approved, Vet Approved
CeritinibThe serum concentration of Eliglustat can be increased when it is combined with Ceritinib.Approved
CevimelineThe metabolism of Cevimeline can be decreased when combined with Eliglustat.Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Eliglustat.Approved, Illicit
ChloroquineThe serum concentration of Eliglustat can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Eliglustat.Approved
ChlorpromazineThe serum concentration of Eliglustat can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Eliglustat.Approved
CholecalciferolThe serum concentration of Eliglustat can be increased when it is combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe metabolism of Cilostazol can be decreased when combined with Eliglustat.Approved
CimetidineThe serum concentration of Eliglustat can be increased when it is combined with Cimetidine.Approved
CinacalcetThe serum concentration of Eliglustat can be increased when it is combined with Cinacalcet.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Eliglustat.Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
CisaprideCisapride may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational, Withdrawn
CitalopramThe serum concentration of Eliglustat can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Eliglustat can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Eliglustat can be increased when it is combined with Clemastine.Approved
ClevidipineThe metabolism of Clevidipine can be decreased when combined with Eliglustat.Approved
ClobazamThe serum concentration of Eliglustat can be increased when it is combined with Clobazam.Approved, Illicit
ClomipramineThe serum concentration of Eliglustat can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineThe metabolism of Clonidine can be decreased when combined with Eliglustat.Approved
ClotrimazoleThe serum concentration of Eliglustat can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Eliglustat can be increased when it is combined with Clozapine.Approved
CobicistatThe serum concentration of Eliglustat can be increased when it is combined with Cobicistat.Approved
CocaineThe serum concentration of Eliglustat can be increased when it is combined with Cocaine.Approved, Illicit
CodeineThe therapeutic efficacy of Codeine can be decreased when used in combination with Eliglustat.Approved, Illicit
ConivaptanThe serum concentration of Eliglustat can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe serum concentration of Eliglustat can be increased when it is combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Eliglustat.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Eliglustat.Approved, Investigational
CyclosporineThe serum concentration of Eliglustat can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Eliglustat can be decreased when it is combined with Dabrafenib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Eliglustat.Approved
DarifenacinThe serum concentration of Eliglustat can be increased when it is combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Eliglustat can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Eliglustat.Approved
DasatinibThe serum concentration of Eliglustat can be increased when it is combined with Dasatinib.Approved, Investigational
DebrisoquinThe metabolism of Debrisoquin can be decreased when combined with Eliglustat.Approved
DeferasiroxThe serum concentration of Eliglustat can be decreased when it is combined with Deferasirox.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Eliglustat.Approved
DelavirdineThe serum concentration of Eliglustat can be increased when it is combined with Delavirdine.Approved
DesfluraneDesflurane may increase the QTc-prolonging activities of Eliglustat.Approved
DesipramineThe serum concentration of Eliglustat can be increased when it is combined with Desipramine.Approved
DexamethasoneThe serum concentration of Eliglustat can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexfenfluramineThe metabolism of Dexfenfluramine can be decreased when combined with Eliglustat.Approved, Illicit, Withdrawn
DexmethylphenidateThe metabolism of Dexmethylphenidate can be decreased when combined with Eliglustat.Approved
DextroamphetamineThe metabolism of Dextroamphetamine can be decreased when combined with Eliglustat.Approved, Illicit
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Eliglustat.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Eliglustat.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Eliglustat.Approved, Illicit
DihydroergotamineThe serum concentration of Eliglustat can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Eliglustat can be increased when it is combined with Diltiazem.Approved
DiphenhydramineThe serum concentration of Eliglustat can be increased when it is combined with Diphenhydramine.Approved
DisopyramideDisopyramide may increase the QTc-prolonging activities of Eliglustat.Approved
DofetilideDofetilide may increase the QTc-prolonging activities of Eliglustat.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Eliglustat.Approved
DomperidoneDomperidone may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Eliglustat.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Eliglustat.Approved
DoxazosinThe metabolism of Doxazosin can be decreased when combined with Eliglustat.Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Eliglustat.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Eliglustat.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Eliglustat.Approved, Investigational
DoxycyclineThe serum concentration of Eliglustat can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Eliglustat can be increased when it is combined with Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
DuloxetineThe serum concentration of Eliglustat can be increased when it is combined with Duloxetine.Approved
EfavirenzThe serum concentration of Eliglustat can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe metabolism of Eletriptan can be decreased when combined with Eliglustat.Approved, Investigational
EncainideThe metabolism of Encainide can be decreased when combined with Eliglustat.Approved, Withdrawn
EnclomipheneThe metabolism of Enclomiphene can be decreased when combined with Eliglustat.Investigational
EnzalutamideThe serum concentration of Eliglustat can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Eliglustat.Approved, Investigational
EribulinEribulin may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Eliglustat.Approved, Investigational
ErythromycinThe serum concentration of Eliglustat can be increased when it is combined with Erythromycin.Approved, Vet Approved
EscitalopramEscitalopram may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Eliglustat can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe metabolism of Esmirtazapine can be decreased when combined with Eliglustat.Investigational
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Eliglustat.Approved, Illicit
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Eliglustat.Approved, Investigational
EtravirineThe serum concentration of Eliglustat can be decreased when it is combined with Etravirine.Approved
EzogabineEzogabine may increase the QTc-prolonging activities of Eliglustat.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Eliglustat.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Eliglustat.Approved
FesoterodineThe metabolism of Fesoterodine can be decreased when combined with Eliglustat.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
FlecainideFlecainide may increase the QTc-prolonging activities of Eliglustat.Approved, Withdrawn
FluconazoleThe serum concentration of Eliglustat can be increased when it is combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Eliglustat.Approved
FluoxetineThe serum concentration of Eliglustat can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolFlupentixol may increase the QTc-prolonging activities of Eliglustat.Approved, Withdrawn
FluphenazineThe metabolism of Fluphenazine can be decreased when combined with Eliglustat.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Eliglustat.Approved
FluvoxamineThe serum concentration of Eliglustat can be increased when it is combined with Fluvoxamine.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
FosamprenavirThe serum concentration of Eliglustat can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Eliglustat can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the QTc-prolonging activities of Eliglustat.Approved
FosphenytoinThe serum concentration of Eliglustat can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Eliglustat can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Eliglustat.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Eliglustat.Approved
GefitinibThe metabolism of Gefitinib can be decreased when combined with Eliglustat.Approved, Investigational
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
GoserelinGoserelin may increase the QTc-prolonging activities of Eliglustat.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Eliglustat.Approved
HaloperidolThe serum concentration of Eliglustat can be increased when it is combined with Haloperidol.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Eliglustat.Approved, Vet Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Eliglustat.Approved
HydrocodoneThe metabolism of Hydrocodone can be decreased when combined with Eliglustat.Approved, Illicit
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Eliglustat.Approved, Illicit
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Eliglustat.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
IbrutinibThe metabolism of Ibrutinib can be decreased when combined with Eliglustat.Approved
IbutilideIbutilide may increase the QTc-prolonging activities of Eliglustat.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Eliglustat.Approved
IdelalisibThe serum concentration of Eliglustat can be increased when it is combined with Idelalisib.Approved
IloperidoneIloperidone may increase the QTc-prolonging activities of Eliglustat.Approved
ImatinibThe serum concentration of Eliglustat can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Eliglustat can be increased when it is combined with Imipramine.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Eliglustat.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Eliglustat.Approved
IndinavirThe serum concentration of Eliglustat can be increased when it is combined with Indinavir.Approved
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Eliglustat.Approved
IsavuconazoniumThe serum concentration of Eliglustat can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsofluraneIsoflurane may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
IsoniazidThe serum concentration of Eliglustat can be increased when it is combined with Isoniazid.Approved
IsradipineThe serum concentration of Eliglustat can be increased when it is combined with Isradipine.Approved
ItraconazoleThe serum concentration of Eliglustat can be increased when it is combined with Itraconazole.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Eliglustat.Approved
IvacaftorThe serum concentration of Eliglustat can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Eliglustat.Approved
KetoconazoleThe serum concentration of Eliglustat can be increased when it is combined with Ketoconazole.Approved, Investigational
LabetalolThe metabolism of Labetalol can be decreased when combined with Eliglustat.Approved
LapatinibLapatinib may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
LenvatinibLenvatinib may increase the QTc-prolonging activities of Eliglustat.Approved
LeuprolideLeuprolide may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
LevodopaThe metabolism of Levodopa can be decreased when combined with Eliglustat.Approved
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Eliglustat.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Eliglustat.Approved, Vet Approved
LisurideThe metabolism of Lisuride can be decreased when combined with Eliglustat.Approved
LithiumLithium may increase the QTc-prolonging activities of Eliglustat.Approved
LomustineThe metabolism of Lomustine can be decreased when combined with Eliglustat.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Eliglustat.Approved
LopinavirThe serum concentration of Eliglustat can be increased when it is combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Eliglustat.Approved
LorcaserinThe serum concentration of Eliglustat can be increased when it is combined with Lorcaserin.Approved
LovastatinThe serum concentration of Eliglustat can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Eliglustat can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Eliglustat can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe serum concentration of Eliglustat can be increased when it is combined with Lumefantrine.Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Eliglustat.Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Eliglustat.Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Eliglustat.Investigational, Withdrawn
MequitazineThe metabolism of Mequitazine can be decreased when combined with Eliglustat.Approved
MesoridazineThe metabolism of Mesoridazine can be decreased when combined with Eliglustat.Approved
MethadoneThe serum concentration of Eliglustat can be increased when it is combined with Methadone.Approved
MethamphetamineThe metabolism of Methamphetamine can be decreased when combined with Eliglustat.Approved, Illicit
MethotrimeprazineThe serum concentration of Eliglustat can be increased when it is combined with Methotrimeprazine.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Eliglustat.Approved, Vet Approved
MethylphenidateThe metabolism of Methylphenidate can be decreased when combined with Eliglustat.Approved, Investigational
MethyprylonThe metabolism of Methyprylon can be decreased when combined with Eliglustat.Approved, Illicit, Withdrawn
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
MetoprololThe serum concentration of Eliglustat can be increased when it is combined with Metoprolol.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Eliglustat.Approved
MexiletineThe metabolism of Mexiletine can be decreased when combined with Eliglustat.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Eliglustat.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
MinaprineThe metabolism of Minaprine can be decreased when combined with Eliglustat.Approved
MirabegronThe serum concentration of Eliglustat can be increased when it is combined with Mirabegron.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Eliglustat.Approved
MitotaneThe serum concentration of Eliglustat can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Eliglustat.Approved
ModafinilThe serum concentration of Eliglustat can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Eliglustat.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Eliglustat.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
NafcillinThe serum concentration of Eliglustat can be decreased when it is combined with Nafcillin.Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Eliglustat.Approved, Investigational
NebivololThe serum concentration of Nebivolol can be increased when it is combined with Eliglustat.Approved, Investigational
NefazodoneThe serum concentration of Eliglustat can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Eliglustat can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Eliglustat can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Eliglustat can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Eliglustat can be increased when it is combined with Nicardipine.Approved
NicergolineThe metabolism of Nicergoline can be decreased when combined with Eliglustat.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Eliglustat.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Eliglustat.Approved
NilotinibThe serum concentration of Eliglustat can be increased when it is combined with Nilotinib.Approved, Investigational
NitrofuralThe metabolism of Nitrofural can be decreased when combined with Eliglustat.Approved, Vet Approved
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Eliglustat.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Eliglustat.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
OfloxacinOfloxacin may increase the QTc-prolonging activities of Eliglustat.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
OlaparibThe serum concentration of Eliglustat can be increased when it is combined with Olaparib.Approved
OlodaterolOlodaterol may increase the QTc-prolonging activities of Eliglustat.Approved
OndansetronOndansetron may increase the QTc-prolonging activities of Eliglustat.Approved
OsimertinibThe serum concentration of Eliglustat can be increased when it is combined with Osimertinib.Approved
OxycodoneThe metabolism of Oxycodone can be decreased when combined with Eliglustat.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Eliglustat.Approved, Investigational, Vet Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
PalbociclibThe serum concentration of Eliglustat can be increased when it is combined with Palbociclib.Approved
PaliperidonePaliperidone may increase the QTc-prolonging activities of Eliglustat.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Eliglustat.Approved, Investigational
PanobinostatThe serum concentration of Eliglustat can be increased when it is combined with Panobinostat.Approved, Investigational
ParoxetineThe serum concentration of Eliglustat can be increased when it is combined with Paroxetine.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Eliglustat.Approved
PazopanibPazopanib may increase the QTc-prolonging activities of Eliglustat.Approved
Peginterferon alfa-2bThe serum concentration of Eliglustat can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidinePentamidine may increase the QTc-prolonging activities of Eliglustat.Approved
PentobarbitalThe serum concentration of Eliglustat can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerflutrenPerflutren may increase the QTc-prolonging activities of Eliglustat.Approved
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Eliglustat.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Eliglustat.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Eliglustat.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Eliglustat.Withdrawn
PhenforminThe metabolism of Phenformin can be decreased when combined with Eliglustat.Approved, Withdrawn
PhenobarbitalThe serum concentration of Eliglustat can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Eliglustat can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozidePimozide may increase the QTc-prolonging activities of Eliglustat.Approved
PindololThe metabolism of Pindolol can be decreased when combined with Eliglustat.Approved
PiperazineThe metabolism of Piperazine can be decreased when combined with Eliglustat.Approved, Vet Approved
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Eliglustat.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Eliglustat.Approved
PosaconazoleThe serum concentration of Eliglustat can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrimaquinePrimaquine may increase the QTc-prolonging activities of Eliglustat.Approved
PrimidoneThe serum concentration of Eliglustat can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcainamideProcainamide may increase the QTc-prolonging activities of Eliglustat.Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Eliglustat.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Eliglustat.Approved, Vet Approved
PromazineThe serum concentration of Eliglustat can be increased when it is combined with Promazine.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Eliglustat.Approved
PropafenoneThe serum concentration of Eliglustat can be increased when it is combined with Propafenone.Approved
PropofolPropofol may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational, Vet Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Eliglustat.Approved, Investigational
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Eliglustat.Approved
PseudoephedrineThe metabolism of Pseudoephedrine can be decreased when combined with Eliglustat.Approved
QuetiapineQuetiapine may increase the QTc-prolonging activities of Eliglustat.Approved
QuinidineThe serum concentration of Eliglustat can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Eliglustat can be increased when it is combined with Quinine.Approved
RanitidineThe metabolism of Ranitidine can be decreased when combined with Eliglustat.Approved
RanolazineThe serum concentration of Eliglustat can be increased when it is combined with Ranolazine.Approved, Investigational
RemoxiprideThe metabolism of Remoxipride can be decreased when combined with Eliglustat.Approved, Withdrawn
repinotanThe metabolism of repinotan can be decreased when combined with Eliglustat.Investigational
RifabutinThe serum concentration of Eliglustat can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Eliglustat can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Eliglustat can be decreased when it is combined with Rifapentine.Approved
RilpivirineRilpivirine may increase the QTc-prolonging activities of Eliglustat.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
RitonavirThe serum concentration of Eliglustat can be increased when it is combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Eliglustat can be increased when it is combined with Rolapitant.Approved
RopiniroleThe serum concentration of Eliglustat can be increased when it is combined with Ropinirole.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Eliglustat.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Eliglustat.Approved
SalbutamolSalbutamol may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Eliglustat.Approved
SaquinavirThe serum concentration of Eliglustat can be increased when it is combined with Saquinavir.Approved, Investigational
SertindoleThe metabolism of Sertindole can be decreased when combined with Eliglustat.Approved, Withdrawn
SertralineThe serum concentration of Eliglustat can be increased when it is combined with Sertraline.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
SildenafilThe serum concentration of Eliglustat can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Eliglustat can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Eliglustat can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Eliglustat.Approved
SolifenacinSolifenacin may increase the QTc-prolonging activities of Eliglustat.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
SotalolSotalol may increase the QTc-prolonging activities of Eliglustat.Approved
SparteineThe metabolism of Sparteine can be decreased when combined with Eliglustat.Experimental
St. John's WortThe serum concentration of Eliglustat can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Eliglustat can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Eliglustat.Approved
SulfisoxazoleThe serum concentration of Eliglustat can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SunitinibSunitinib may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
TamoxifenThe serum concentration of the active metabolites of Tamoxifen can be reduced when Tamoxifen is used in combination with Eliglustat resulting in a loss in efficacy.Approved
TamsulosinThe metabolism of Tamsulosin can be decreased when combined with Eliglustat.Approved, Investigational
TapentadolThe metabolism of Tapentadol can be decreased when combined with Eliglustat.Approved
TegaserodThe metabolism of Tegaserod can be decreased when combined with Eliglustat.Investigational, Withdrawn
TelaprevirThe serum concentration of Eliglustat can be increased when it is combined with Telaprevir.Approved
TelavancinTelavancin may increase the QTc-prolonging activities of Eliglustat.Approved
TelithromycinThe serum concentration of Eliglustat can be increased when it is combined with Telithromycin.Approved
TerbinafineThe serum concentration of Eliglustat can be increased when it is combined with Terbinafine.Approved, Investigational, Vet Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Eliglustat.Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Eliglustat.Withdrawn
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Eliglustat.Investigational
TetrabenazineTetrabenazine may increase the QTc-prolonging activities of Eliglustat.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Eliglustat.Approved
ThioridazineThe serum concentration of Eliglustat can be increased when it is combined with Thioridazine.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Eliglustat.Approved
TiclopidineThe serum concentration of Eliglustat can be increased when it is combined with Ticlopidine.Approved
TimololThe metabolism of Timolol can be decreased when combined with Eliglustat.Approved
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Eliglustat.Approved
TipranavirThe serum concentration of Eliglustat can be increased when it is combined with Tipranavir.Approved, Investigational
TizanidineTizanidine may increase the QTc-prolonging activities of Eliglustat.Approved
TocilizumabThe serum concentration of Eliglustat can be decreased when it is combined with Tocilizumab.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
ToremifeneToremifene may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Eliglustat.Approved, Investigational
TramadolThe therapeutic efficacy of Tramadol can be decreased when used in combination with Eliglustat.Approved, Investigational
TranylcypromineThe serum concentration of Eliglustat can be increased when it is combined with Tranylcypromine.Approved
TrazodoneTrazodone may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Eliglustat.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Eliglustat.Approved, Vet Approved
UmeclidiniumThe metabolism of Umeclidinium can be decreased when combined with Eliglustat.Approved
VandetanibVandetanib may increase the QTc-prolonging activities of Eliglustat.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Eliglustat.Approved
VemurafenibVemurafenib may increase the QTc-prolonging activities of Eliglustat.Approved
VenlafaxineThe serum concentration of Eliglustat can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Eliglustat can be increased when it is combined with Verapamil.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Eliglustat.Approved
VilazodoneThe metabolism of Vilazodone can be decreased when combined with Eliglustat.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Eliglustat.Approved
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Eliglustat.Approved, Investigational
VoriconazoleThe serum concentration of Eliglustat can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Eliglustat.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Eliglustat.Approved, Vet Approved
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Eliglustat.Approved
ZiprasidoneThe serum concentration of Eliglustat can be increased when it is combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Eliglustat.Approved
ZuclopenthixolZuclopenthixol may increase the QTc-prolonging activities of Eliglustat.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Poole RM: Eliglustat: first global approval. Drugs. 2014 Oct;74(15):1829-36. doi: 10.1007/s40265-014-0296-3. [PubMed:25239269 ]
External Links
ATC CodesA16AX10
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (376 KB)
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral84 mg/1
CapsuleOral84 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6916802 No2002-04-292022-04-29Us
US7196205 No2002-04-292022-04-29Us
US7615573 No2002-04-292022-04-29Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.038 mg/mLALOGPS
logP3.79ALOGPS
logP1.46ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)5.21ChemAxon
pKa (Strongest Basic)8.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area74.52 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity114.28 m3·mol-1ChemAxon
Polarizability46 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
ClassificationNot classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Ceramide glucosyltransferase activity
Specific Function:
Catalyzes the first glycosylation step in glycosphingolipid biosynthesis, the transfer of glucose to ceramide. May also serve as a "flippase".
Gene Name:
UGCG
Uniprot ID:
Q16739
Molecular Weight:
44853.255 Da
References
  1. Poole RM: Eliglustat: first global approval. Drugs. 2014 Oct;74(15):1829-36. doi: 10.1007/s40265-014-0296-3. [PubMed:25239269 ]

Enzymes

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
References
  1. Poole RM: Eliglustat: first global approval. Drugs. 2014 Oct;74(15):1829-36. doi: 10.1007/s40265-014-0296-3. [PubMed:25239269 ]
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
References
  1. Poole RM: Eliglustat: first global approval. Drugs. 2014 Oct;74(15):1829-36. doi: 10.1007/s40265-014-0296-3. [PubMed:25239269 ]
Comments
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Drug created on April 02, 2015 10:54 / Updated on December 07, 2016 02:39