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Identification
NameGranisetron
Accession NumberDB00889  (APRD01002)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionA serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients. [PubChem]
Structure
Thumb
Synonyms
granisétron
granisetrón
granisetronum
External Identifiers
  • APF-530
  • APF530
  • BRL 43694
  • BRL-43694
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Granisetron Hydrochloride InjectionLiquid1 mgIntravenousSandoz Canada Incorporated2009-02-20Not applicableCanada
Granisetron Hydrochloride InjectionSolution1 mgIntravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Granisetron Hydrochloride InjectionLiquid1 mgIntravenousOmega Laboratories Ltd2009-05-14Not applicableCanada
Granisetron Hydrochloride Injection SdzSolution1 mgIntravenousSandoz Canada Incorporated2012-12-19Not applicableCanada
Kytril 1mg/1mlLiquid1 mgIntravenousHoffmann La Roche Limited1996-12-312012-01-06Canada
Kytril Tablets 1mgTablet1 mgOralHoffmann La Roche Limited1996-12-312015-11-06Canada
Nat-granisetronTablet1 mgOralNatco Pharma (Canada) Inc2016-03-01Not applicableCanada
SancusoPatch3.1 mg/24hTransdermalPro Strakan, Inc.2008-09-12Not applicableUs
SancusoPatch3.1 mg/24hTransdermalPhysicians Total Care, Inc.2009-02-16Not applicableUs
SancusoPatch3.1 mg/24hTransdermalKyowa Kirin Limited2012-04-20Not applicableEu
SustolInjection10 mg/.4mLSubcutaneousHeron Therapeutics2016-08-09Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-granisetronTablet1 mgOralApotex Inc2009-02-20Not applicableCanada
GranisetronInjection1 mg/mLIntravenousSandoz Inc2008-06-30Not applicableUs
GranisetronInjection, solution1 mg/mLIntravenousFresenius Kabi USA, LLC2009-11-20Not applicableUs
GranisetronInjection1 mg/mLIntravenousSandoz Inc2008-06-30Not applicableUs
GranisetronInjection, solution.1 mg/mLIntravenousFresenius Kabi USA, LLC2009-11-20Not applicableUs
GranisetronInjection, solution1 mg/mLIntravenousFresenius Kabi USA, LLC2009-11-20Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousWockhardt Limited2008-06-30Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralOrchid Pharma Inc2016-04-12Not applicableUs
Granisetron HydrochlorideTablet1 mg/1OralWest Ward Pharmaceuticals Corp.2007-12-31Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousWest ward Pharmaceutical Corp2009-12-23Not applicableUs
Granisetron HydrochlorideInjection, solution1 mg/mLIntravenousSagent Pharmaceuticals2010-12-01Not applicableUs
Granisetron HydrochlorideInjection.1 mg/mLIntravenousAkorn, Inc.2009-10-01Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousCipla USA Inc.2008-06-30Not applicableUs
Granisetron HydrochlorideInjection.1 mg/mLIntravenousWockhardt Limited2008-03-03Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousWest ward Pharmaceutical Corp2009-12-23Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousWOCKHARDT USA LLC2008-06-30Not applicableUs
Granisetron HydrochlorideInjection, solution1 mg/mLIntravenousSagent Pharmaceuticals2010-12-01Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralTaro Pharmaceuticals U.S.A., Inc.2010-05-28Not applicableUs
Granisetron HydrochlorideInjection4 mg/4mLIntravenousCipla USA Inc.2008-06-30Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralTeva Pharmaceuticals USA Inc2008-01-02Not applicableUs
Granisetron HydrochlorideTablet1 mg/1OralAscend Laboratories, LLC2010-01-01Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralNorthstar Rx LLC2008-04-29Not applicableUs
Granisetron HydrochlorideInjection.1 mg/mLIntravenousWOCKHARDT USA LLC2008-03-03Not applicableUs
Granisetron HydrochlorideInjection, solution1 mg/mLIntravenousAuro Medics Pharma Llc2016-07-06Not applicableUs
Granisetron HydrochlorideTablet1 mg/1OralBreckenridge Pharmaceutical, Inc.2009-06-22Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralAvera Mc Kennan Hospital2015-03-02Not applicableUs
Granisetron HydrochlorideInjection, solution.1 mg/mLIntravenousSagent Pharmaceuticals2010-12-01Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousAkorn, Inc.2009-10-01Not applicableUs
Granisetron HydrochlorideInjection.1 mg/mLIntravenousCipla Limited2007-12-31Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralCore Pharma, Llc2007-12-312016-03-15Us
Granisetron HydrochlorideInjection, solution4 mg/4mLIntravenousAuro Medics Pharma Llc2016-07-06Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
GranisolNot Available
KevatrilNot Available
KytrilNot Available
SustolNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Granisetron hydrochloride
107007-99-8
Thumb
  • InChI Key: QYZRTBKYBJRGJB-WQTKJZBYSA-N
  • Monoisotopic Mass: 348.1716891
  • Average Mass: 348.88
DBSALT000485
Categories
UNIIWZG3J2MCOL
CAS number109889-09-0
WeightAverage: 312.417
Monoisotopic: 312.195011409
Chemical FormulaC18H24N4O
InChI KeyMFWNKCLOYSRHCJ-BTTYYORXSA-N
InChI
InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12-,13+,14-
IUPAC Name
1-methyl-N-[(1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]-1H-indazole-3-carboxamide
SMILES
CN1N=C(C(=O)N[C@@H]2C[C@@H]3CCC[[email protected]](C2)N3C)C2=C1C=CC=C2
Pharmacology
IndicationFor the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy (including high dose cisplatin), postoperation, and radiation (including total body irradiation and daily fractionated abdominal radiation).
Structured Indications
PharmacodynamicsGranisetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptors. Granisetron has little or no affinity for other serotonin receptors, including 5-HT 1 , 5-HT 1A , 5-HT 1B/C , or 5-HT 2 ; for alpha 1 -, alpha 2 -, or beta-adrenoreceptors; for dopamine D 2 receptors; for histamine H 1 receptors; for benzodiazepine receptors; for picrotoxin receptors; or for opioid receptors. In most human studies, granisetron has had little effect on blood pressure, heart rate, or electrocardiogram (ECG). The drug is structurally and pharmacologically related to ondansetron, another selective inhibitor of 5-HT3 receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.
Mechanism of actionGranisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.
TargetKindPharmacological actionActionsOrganismUniProt ID
5-hydroxytryptamine receptor 3AProteinyes
antagonist
HumanP46098 details
Related Articles
AbsorptionAbsorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.
Volume of distributionNot Available
Protein binding65%
Metabolism

Primarily hepatic; undergoes N -demethylation and aromatic ring oxidation followed by conjugation. Animal studies suggest that some of the metabolites may have 5-HT 3 receptor antagonist activity.

SubstrateEnzymesProduct
Granisetron
9'-desmethylgranisetronDetails
Granisetron
7-hydroxygranisetronDetails
Route of eliminationThe remainder of the dose is excreted as metabolites, 48% in the urine and 38% in the feces.
Half life4-6 hours in healthy patients, 9-12 hours in cancer patients
Clearance
  • 0.52 L/h/kg [Cancer Patients with 1 mg bid for 7 days]
  • 0.41 L/h/kg [Healthy subject with a single 1 mg dose]
ToxicityLD50>2000 mg/kg (rat, oral)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Granisetron can be increased when it is combined with Abiraterone.Approved
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
AlmotriptanGranisetron may increase the serotonergic activities of Almotriptan.Approved, Investigational
AmantadineAmantadine may increase the QTc-prolonging activities of Granisetron.Approved
AmiodaroneGranisetron may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Granisetron.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Granisetron.Approved
AnagrelideGranisetron may increase the QTc-prolonging activities of Anagrelide.Approved
ApomorphineGranisetron may increase the hypotensive activities of Apomorphine.Approved, Investigational
AprepitantThe serum concentration of Granisetron can be increased when it is combined with Aprepitant.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
Arsenic trioxideGranisetron may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherGranisetron may increase the QTc-prolonging activities of Artemether.Approved
AsenapineGranisetron may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirThe metabolism of Granisetron can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Granisetron.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Granisetron.Approved
BedaquilineGranisetron may increase the QTc-prolonging activities of Bedaquiline.Approved
BetaxololThe metabolism of Granisetron can be decreased when combined with Betaxolol.Approved
BexaroteneThe serum concentration of Granisetron can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Granisetron can be decreased when combined with Boceprevir.Approved
BortezomibBortezomib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
BosentanThe serum concentration of Granisetron can be decreased when it is combined with Bosentan.Approved, Investigational
BromocriptineGranisetron may increase the serotonergic activities of Bromocriptine.Approved, Investigational
BupropionThe metabolism of Granisetron can be decreased when combined with Bupropion.Approved
BuserelinBuserelin may increase the QTc-prolonging activities of Granisetron.Approved
BuspironeGranisetron may increase the serotonergic activities of Buspirone.Approved, Investigational
CabergolineGranisetron may increase the serotonergic activities of Cabergoline.Approved
CarbamazepineThe metabolism of Granisetron can be increased when combined with Carbamazepine.Approved, Investigational
CelecoxibThe metabolism of Granisetron can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Granisetron can be increased when it is combined with Ceritinib.Approved
ChloroquineChloroquine may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
CholecalciferolThe metabolism of Granisetron can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Granisetron can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Granisetron can be decreased when combined with Cinacalcet.Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
CisaprideGranisetron may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramGranisetron may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinGranisetron may increase the QTc-prolonging activities of Clarithromycin.Approved
ClemastineThe metabolism of Granisetron can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Granisetron can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineClomipramine may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
ClotrimazoleThe metabolism of Granisetron can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineClozapine may increase the QTc-prolonging activities of Granisetron.Approved
CobicistatThe serum concentration of Granisetron can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Granisetron can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Granisetron can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibGranisetron may increase the QTc-prolonging activities of Crizotinib.Approved
CyclobenzaprineGranisetron may increase the serotonergic activities of Cyclobenzaprine.Approved
CyclosporineThe metabolism of Granisetron can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Granisetron can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe metabolism of Granisetron can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Granisetron can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Granisetron can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Granisetron can be decreased when it is combined with Deferasirox.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Granisetron.Approved
DelavirdineThe metabolism of Granisetron can be decreased when combined with Delavirdine.Approved
DesfluraneDesflurane may increase the QTc-prolonging activities of Granisetron.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Granisetron.Approved
DesvenlafaxineGranisetron may increase the serotonergic activities of Desvenlafaxine.Approved
DexamethasoneThe serum concentration of Granisetron can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanGranisetron may increase the serotonergic activities of Dextromethorphan.Approved
DihydroergotamineThe metabolism of Granisetron can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Granisetron can be decreased when combined with Diltiazem.Approved
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Granisetron.Approved
DisopyramideGranisetron may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilideGranisetron may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Granisetron.Approved
DomperidoneGranisetron may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Granisetron.Approved
DoxycyclineThe metabolism of Granisetron can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneGranisetron may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
DuloxetineGranisetron may increase the serotonergic activities of Duloxetine.Approved
EfavirenzThe serum concentration of Granisetron can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanGranisetron may increase the serotonergic activities of Eletriptan.Approved, Investigational
EliglustatGranisetron may increase the QTc-prolonging activities of Eliglustat.Approved
EnzalutamideThe serum concentration of Granisetron can be decreased when it is combined with Enzalutamide.Approved
Ergoloid mesylateGranisetron may increase the serotonergic activities of Ergoloid mesylate.Approved
ErgonovineGranisetron may increase the serotonergic activities of Ergonovine.Approved
ErgotamineGranisetron may increase the serotonergic activities of Ergotamine.Approved
EribulinEribulin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
ErythromycinErythromycin may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
EscitalopramGranisetron may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Granisetron can be decreased when it is combined with Eslicarbazepine acetate.Approved
EtravirineThe serum concentration of Granisetron can be decreased when it is combined with Etravirine.Approved
EzogabineEzogabine may increase the QTc-prolonging activities of Granisetron.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Granisetron.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Granisetron.Approved
FentanylGranisetron may increase the serotonergic activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Granisetron.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
FlecainideGranisetron may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluconazoleFluconazole may increase the QTc-prolonging activities of Granisetron.Approved
FluoxetineGranisetron may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolGranisetron may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvoxamineThe metabolism of Granisetron can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
FosamprenavirThe metabolism of Granisetron can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Granisetron can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the QTc-prolonging activities of Granisetron.Approved
FosphenytoinThe metabolism of Granisetron can be increased when combined with Fosphenytoin.Approved
FrovatriptanGranisetron may increase the serotonergic activities of Frovatriptan.Approved, Investigational
Fusidic AcidThe serum concentration of Granisetron can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Granisetron.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Granisetron.Approved
GemifloxacinGranisetron may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GoserelinGoserelin may increase the QTc-prolonging activities of Granisetron.Approved
HaloperidolHaloperidol may increase the QTc-prolonging activities of Granisetron.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Granisetron.Approved
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Granisetron.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
IbutilideGranisetron may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Granisetron can be increased when it is combined with Idelalisib.Approved
IloperidoneGranisetron may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Granisetron can be decreased when combined with Imatinib.Approved
ImipramineImipramine may increase the QTc-prolonging activities of Granisetron.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Granisetron.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Granisetron.Approved
IndinavirThe metabolism of Granisetron can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Granisetron can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidGranisetron may increase the serotonergic activities of Isocarboxazid.Approved
IsofluraneIsoflurane may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
IsoniazidThe metabolism of Granisetron can be decreased when combined with Isoniazid.Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Granisetron.Approved
ItraconazoleThe metabolism of Granisetron can be decreased when combined with Itraconazole.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Granisetron.Approved
IvacaftorThe serum concentration of Granisetron can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Granisetron can be decreased when combined with Ketoconazole.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
LenvatinibGranisetron may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideLeuprolide may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
LevofloxacinGranisetron may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranGranisetron may increase the serotonergic activities of Levomilnacipran.Approved
LinezolidGranisetron may increase the serotonergic activities of Linezolid.Approved, Investigational
LithiumLithium may increase the QTc-prolonging activities of Granisetron.Approved
LopinavirGranisetron may increase the QTc-prolonging activities of Lopinavir.Approved
LorcaserinGranisetron may increase the serotonergic activities of Lorcaserin.Approved
LovastatinThe metabolism of Granisetron can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Granisetron can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Granisetron can be increased when combined with Lumacaftor.Approved
LumefantrineGranisetron may increase the QTc-prolonging activities of Lumefantrine.Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Granisetron.Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Granisetron.Approved
MethadoneMethadone may increase the QTc-prolonging activities of Granisetron.Approved
MethotrimeprazineThe metabolism of Granisetron can be decreased when combined with Methotrimeprazine.Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Granisetron.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Granisetron.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
MilnacipranGranisetron may increase the serotonergic activities of Milnacipran.Approved
MirabegronMirabegron may increase the QTc-prolonging activities of Granisetron.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Granisetron.Approved
MitotaneThe serum concentration of Granisetron can be decreased when it is combined with Mitotane.Approved
MoclobemideGranisetron may increase the serotonergic activities of Moclobemide.Approved
ModafinilThe serum concentration of Granisetron can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Granisetron.Approved
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
NafcillinThe serum concentration of Granisetron can be decreased when it is combined with Nafcillin.Approved
NaratriptanGranisetron may increase the serotonergic activities of Naratriptan.Approved, Investigational
NefazodoneThe metabolism of Granisetron can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Granisetron can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Granisetron can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Granisetron can be increased when combined with Nevirapine.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Granisetron.Approved
NilotinibGranisetron may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Granisetron.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Granisetron.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
OfloxacinGranisetron may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
OlaparibThe metabolism of Granisetron can be decreased when combined with Olaparib.Approved
OlodaterolOlodaterol may increase the QTc-prolonging activities of Granisetron.Approved
OndansetronGranisetron may increase the QTc-prolonging activities of Ondansetron.Approved
OsimertinibThe serum concentration of Granisetron can be increased when it is combined with Osimertinib.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
PalbociclibThe serum concentration of Granisetron can be increased when it is combined with Palbociclib.Approved
PaliperidoneGranisetron may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatGranisetron may increase the arrhythmogenic activities of Panobinostat.Approved, Investigational
ParoxetineThe metabolism of Granisetron can be decreased when combined with Paroxetine.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Granisetron.Approved
PazopanibGranisetron may increase the QTc-prolonging activities of Pazopanib.Approved
Peginterferon alfa-2bThe serum concentration of Granisetron can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentamidinePentamidine may increase the QTc-prolonging activities of Granisetron.Approved
PentobarbitalThe metabolism of Granisetron can be increased when combined with Pentobarbital.Approved, Vet Approved
PerflutrenPerflutren may increase the QTc-prolonging activities of Granisetron.Approved
PethidineGranisetron may increase the serotonergic activities of Pethidine.Approved
PhenelzineGranisetron may increase the serotonergic activities of Phenelzine.Approved
PhenobarbitalThe metabolism of Granisetron can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Granisetron can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideGranisetron may increase the QTc-prolonging activities of Pimozide.Approved
PosaconazoleThe metabolism of Granisetron can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimaquineGranisetron may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe metabolism of Granisetron can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideGranisetron may increase the QTc-prolonging activities of Procainamide.Approved
ProcarbazineGranisetron may increase the serotonergic activities of Procarbazine.Approved
PromazinePromazine may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Granisetron.Approved
PropafenoneGranisetron may increase the QTc-prolonging activities of Propafenone.Approved
PropofolPropofol may increase the QTc-prolonging activities of Granisetron.Approved, Investigational, Vet Approved
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Granisetron.Approved
QuetiapineGranisetron may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineGranisetron may increase the QTc-prolonging activities of Quinidine.Approved
QuinineGranisetron may increase the QTc-prolonging activities of Quinine.Approved
RanolazineRanolazine may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
RasagilineGranisetron may increase the serotonergic activities of Rasagiline.Approved
RifabutinThe metabolism of Granisetron can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Granisetron can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Granisetron can be increased when combined with Rifapentine.Approved
RilpivirineRilpivirine may increase the QTc-prolonging activities of Granisetron.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
RitonavirThe metabolism of Granisetron can be decreased when combined with Ritonavir.Approved, Investigational
RizatriptanGranisetron may increase the serotonergic activities of Rizatriptan.Approved
RolapitantThe metabolism of Granisetron can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Granisetron can be decreased when combined with Ropinirole.Approved, Investigational
SalbutamolSalbutamol may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Granisetron.Approved
SaquinavirGranisetron may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SelegilineGranisetron may increase the serotonergic activities of Selegiline.Approved, Investigational, Vet Approved
SertralineSertraline may increase the QTc-prolonging activities of Granisetron.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
SildenafilThe metabolism of Granisetron can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Granisetron can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Granisetron can be increased when it is combined with Simeprevir.Approved
SolifenacinSolifenacin may increase the QTc-prolonging activities of Granisetron.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
SotalolGranisetron may increase the QTc-prolonging activities of Sotalol.Approved
St. John's WortThe serum concentration of Granisetron can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Granisetron can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Granisetron.Approved
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
SumatriptanGranisetron may increase the serotonergic activities of Sumatriptan.Approved, Investigational
SunitinibSunitinib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Granisetron.Approved
TapentadolGranisetron may decrease the analgesic activities of Tapentadol.Approved
Tedizolid PhosphateGranisetron may increase the serotonergic activities of Tedizolid Phosphate.Approved
TelaprevirThe metabolism of Granisetron can be decreased when combined with Telaprevir.Approved
TelavancinGranisetron may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinGranisetron may increase the QTc-prolonging activities of Telithromycin.Approved
TerbinafineThe metabolism of Granisetron can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Granisetron.Approved
TetrabenazineGranisetron may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Granisetron.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Granisetron.Approved
TiclopidineThe metabolism of Granisetron can be decreased when combined with Ticlopidine.Approved
TipranavirThe metabolism of Granisetron can be decreased when combined with Tipranavir.Approved, Investigational
TizanidineTizanidine may increase the QTc-prolonging activities of Granisetron.Approved
TocilizumabThe serum concentration of Granisetron can be decreased when it is combined with Tocilizumab.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
ToremifeneGranisetron may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TramadolGranisetron may decrease the analgesic activities of Tramadol.Approved, Investigational
TranylcypromineGranisetron may increase the serotonergic activities of Tranylcypromine.Approved
TrazodoneTrazodone may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Granisetron.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
VandetanibGranisetron may increase the QTc-prolonging activities of Vandetanib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Granisetron.Approved
VemurafenibGranisetron may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Granisetron.Approved
VerapamilThe metabolism of Granisetron can be decreased when combined with Verapamil.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Granisetron.Approved
VilazodoneGranisetron may increase the serotonergic activities of Vilazodone.Approved
VoriconazoleThe metabolism of Granisetron can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
VortioxetineGranisetron may increase the serotonergic activities of Vortioxetine.Approved
ZiprasidoneGranisetron may increase the QTc-prolonging activities of Ziprasidone.Approved
ZolmitriptanGranisetron may increase the serotonergic activities of Zolmitriptan.Approved, Investigational
ZuclopenthixolGranisetron may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food Interactions
  • Take without regard to meals.
References
Synthesis Reference

Neal Ward, David Alan Jones, Victor Witold Jacewicz, “Process for the preparation of granisetron.” U.S. Patent US6268498, issued April, 1986.

US6268498
General References
  1. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. [PubMed:15740177 ]
  2. Tan M: Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother. 2003 Sep;4(9):1563-71. [PubMed:12943486 ]
  3. Feyer P, Seegenschmiedt MH, Steingraeber M: Granisetron in the control of radiotherapy-induced nausea and vomiting: a comparison with other antiemetic therapies. Support Care Cancer. 2005 Sep;13(9):671-8. Epub 2005 Jul 26. [PubMed:16044252 ]
External Links
ATC CodesA04AA02
AHFS Codes
  • 56:22.20
PDB EntriesNot Available
FDA labelDownload (77.3 KB)
MSDSDownload (51.7 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9947
Blood Brain Barrier+0.9515
Caco-2 permeable+0.5231
P-glycoprotein substrateSubstrate0.5473
P-glycoprotein inhibitor IInhibitor0.6287
P-glycoprotein inhibitor IIInhibitor0.7243
Renal organic cation transporterNon-inhibitor0.5895
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6978
CYP450 1A2 substrateNon-inhibitor0.8546
CYP450 2C9 inhibitorNon-inhibitor0.9019
CYP450 2D6 inhibitorNon-inhibitor0.8841
CYP450 2C19 inhibitorNon-inhibitor0.9073
CYP450 3A4 inhibitorNon-inhibitor0.8355
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6016
Ames testNon AMES toxic0.5878
CarcinogenicityNon-carcinogens0.8464
BiodegradationNot ready biodegradable0.9868
Rat acute toxicity2.3943 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9083
hERG inhibition (predictor II)Inhibitor0.5458
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Strakan international ltd
  • Akorn inc
  • App pharmaceuticals llc
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories
  • Claris lifesciences ltd
  • Dr reddys laboratories inc
  • Ebewe pharma
  • Sagent strides llc
  • Sandoz canada inc
  • Teva parenteral medicines inc
  • Watson laboratories inc
  • Wockhardt usa inc
  • App pharmaceuticals
  • Hikma farmaceutica (portugal) sa
  • Hoffmann la roche inc
  • Cypress pharmaceutical inc
  • Apotex inc
  • Barr laboratories inc
  • Cipla ltd
  • Corepharma llc
  • Dr reddys laboratories ltd
  • Mylan pharmaceuticals inc
  • Natco pharma ltd
  • Orchid healthcare
  • Roxane laboratories inc
  • Taro pharmaceuticals usa inc
  • Teva pharmaceuticals usa
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntravenous.1 mg/mL
Injection, solutionIntravenous1 mg/mL
InjectionIntravenous.1 mg/mL
InjectionIntravenous1 mg/mL
InjectionIntravenous4 mg/4mL
Injection, solutionIntravenous4 mg/4mL
TabletOral1 mg/1
Tablet, film coatedOral1 mg/1
LiquidIntravenous1 mg
SolutionIntravenous1 mg
TabletOral1 mg
PatchTransdermal3.1 mg/24h
InjectionSubcutaneous10 mg/.4mL
Prices
Unit descriptionCostUnit
Sancuso 3.1 mg/24 hr patch372.0USD patch
Kytril 2 1 mg tablet Box131.98USD box
Kytril 1 mg tablet62.94USD tablet
Granisetron hcl 1 mg tablet60.19USD tablet
Granisetron hcl 4 mg/4 ml vial24.0USD ml
Kytril 1 mg Tablet20.27USD tablet
Apo-Granisetron 1 mg Tablet14.14USD tablet
Kytril 0.1 mg/ml vial11.54USD ml
Granisetron hcl 0.1 mg/ml vial7.2USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2100777 No2003-08-192012-01-16Canada
CA2158354 No2004-07-132014-03-15Canada
US5952340 No1996-09-142016-09-14Us
US7608282 No2004-10-222024-10-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point219 °C (HCl salt)Not Available
logP2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.434 mg/mLALOGPS
logP2.64ALOGPS
logP1.88ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)14.75ChemAxon
pKa (Strongest Basic)9ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area50.16 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity101.83 m3·mol-1ChemAxon
Polarizability35.57 Å3ChemAxon
Number of Rings4ChemAxon
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 indazole-3-carboxamides. These are aromatic compounds containing an indazole ring system that is substituted at the 3-position with a carboxamide group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzopyrazoles
Sub ClassIndazoles
Direct ParentIndazole-3-carboxamides
Alternative Parents
Substituents
  • Indazole-3-carboxamide
  • 2-heteroaryl carboxamide
  • Pyrazole-5-carboxamide
  • Piperidine
  • Benzenoid
  • Azole
  • Heteroaromatic compound
  • Pyrazole
  • Amino acid or derivatives
  • Carboxamide group
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxylic acid derivative
  • Azacycle
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Organic oxide
  • Organic oxygen compound
  • Hydrocarbon derivative
  • Organic nitrogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Voltage-gated potassium channel activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
Gene Name:
HTR3A
Uniprot ID:
P46098
Molecular Weight:
55279.835 Da
References
  1. Hillsley K, Grundy D: Plasticity in the mesenteric afferent response to cisplatin following vagotomy in the rat. J Auton Nerv Syst. 1999 May 28;76(2-3):93-8. [PubMed:10412832 ]
  2. Turvill JL, Connor P, Farthing MJ: The inhibition of cholera toxin-induced 5-HT release by the 5-HT(3) receptor antagonist, granisetron, in the rat. Br J Pharmacol. 2000 Jul;130(5):1031-6. [PubMed:10882387 ]
  3. Cappelli A, Anzini M, Vomero S, Mennuni L, Makovec F, Doucet E, Hamon M, Menziani MC, De Benedetti PG, Giorgi G, Ghelardini C, Collina S: Novel potent 5-HT(3) receptor ligands based on the pyrrolidone structure: synthesis, biological evaluation, and computational rationalization of the ligand-receptor interaction modalities. Bioorg Med Chem. 2002 Mar;10(3):779-801. [PubMed:11814868 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  5. Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38. [PubMed:15740177 ]
  6. Tan M: Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother. 2003 Sep;4(9):1563-71. [PubMed:12943486 ]
  7. Ho KY, Gan TJ: Pharmacology, pharmacogenetics, and clinical efficacy of 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting. Curr Opin Anaesthesiol. 2006 Dec;19(6):606-11. [PubMed:17093363 ]
  8. Abdelsayed GG: Management of radiation-induced nausea and vomiting. Exp Hematol. 2007 Apr;35(4 Suppl 1):34-6. [PubMed:17379085 ]
  9. Feyer P, Seegenschmiedt MH, Steingraeber M: Granisetron in the control of radiotherapy-induced nausea and vomiting: a comparison with other antiemetic therapies. Support Care Cancer. 2005 Sep;13(9):671-8. Epub 2005 Jul 26. [PubMed:16044252 ]

Enzymes

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. Tan M: Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother. 2003 Sep;4(9):1563-71. [PubMed:12943486 ]
  2. Janicki PK: Cytochrome P450 2D6 metabolism and 5-hydroxytryptamine type 3 receptor antagonists for postoperative nausea and vomiting. Med Sci Monit. 2005 Oct;11(10):RA322-8. Epub 2005 Sep 26. [PubMed:16192915 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Nakamura H, Ariyoshi N, Okada K, Nakasa H, Nakazawa K, Kitada M: CYP1A1 is a major enzyme responsible for the metabolism of granisetron in human liver microsomes. Curr Drug Metab. 2005 Oct;6(5):469-80. [PubMed:16248838 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 09, 2016 02:39