Identification

Name
Granisetron
Accession Number
DB00889  (APRD01002)
Type
Small Molecule
Groups
Approved, Investigational
Description

A 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 IDs
APF-530 / APF530 / BRL 43694 / BRL-43694
Product Ingredients
IngredientUNIICASInChI Key
Granisetron hydrochloride318F6L70J8107007-99-8QYZRTBKYBJRGJB-WQTKJZBYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Granisetron Hydrochloride InjectionLiquid1 mgIntravenousOmega Laboratories Ltd2009-05-14Not applicableCanada
Granisetron Hydrochloride InjectionSolution1 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Granisetron Hydrochloride InjectionLiquid1 mgIntravenousSandoz Canada Incorporated2009-02-20Not applicableCanada
Granisetron Hydrochloride Injection SdzSolution1 mgIntravenousSandoz Canada Incorporated2012-12-19Not applicableCanada
Kytril 1mg/1mlLiquid1 mgIntravenousHoffmann La Roche1996-12-312012-01-06Canada
Kytril Tablets 1mgTablet1 mgOralHoffmann La Roche1996-12-312015-11-06Canada
Nat-granisetronTablet1 mgOralNatco Pharma Limited2016-03-01Not applicableCanada
SancusoPatch3.1 mg/24hTransdermalPhysicians Total Care, Inc.2009-02-16Not applicableUs
SancusoPatch3.1 mg/24hTransdermalKyowa Kirin, Inc.2008-09-12Not applicableUs
SancusoPatch3.1 mg/24hTransdermalKyowa Kirin Limited2012-04-20Not applicableEu
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-granisetronTablet1 mgOralApotex Corporation2009-02-20Not applicableCanada
GranisetronInjection1 mg/mLIntravenousSandoz2008-06-30Not applicableUs
GranisetronInjection, solution.1 mg/mLIntravenousFresenius Kabi2009-11-20Not applicableUs
GranisetronInjection1 mg/mLIntravenousSandoz2008-06-30Not applicableUs
GranisetronInjection, solution1 mg/mLIntravenousFresenius Kabi2009-11-20Not applicableUs
GranisetronInjection, solution1 mg/mLIntravenousFresenius Kabi2009-11-20Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousCipla Limited2008-06-30Not applicableUs
Granisetron HydrochlorideTablet, film coated1 mg/1OralTaro Pharmaceuticals U.S.A., Inc.2010-05-28Not applicableUs
Granisetron HydrochlorideInjection, solution1 mg/mLIntravenousAuro Medics Pharma Llc2016-07-06Not applicableUs
Granisetron HydrochlorideInjection1 mg/mLIntravenousWest Ward Pharmaceutical2009-12-23Not applicableUs
International/Other Brands
Granisol / Kevatril / Kytril / Sustol
Categories
UNII
WZG3J2MCOL
CAS number
109889-09-0
Weight
Average: 312.417
Monoisotopic: 312.195011409
Chemical Formula
C18H24N4O
InChI Key
MFWNKCLOYSRHCJ-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[[email protected]@H]2C[[email protected]@H]3CCC[[email protected]](C2)N3C)C2=C1C=CC=C2

Pharmacology

Indication

For 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
Pharmacodynamics

Granisetron 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 action

Granisetron 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.

TargetActionsOrganism
A5-hydroxytryptamine receptor 3A
antagonist
Human
Absorption

Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.

Volume of distribution
Not Available
Protein binding

65%

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.

Route of elimination

The remainder of the dose is excreted as metabolites, 48% in the urine and 38% in the feces.

Half life

4-6 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]
Toxicity

LD50>2000 mg/kg (rat, oral)

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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
AmiodaroneThe metabolism of Granisetron can be decreased when combined with 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
ArtemetherThe metabolism of Granisetron can be decreased when combined with 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
BoceprevirThe metabolism of Granisetron can be decreased when combined with Boceprevir.Approved, Withdrawn
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 serotonergic 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
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
DosulepinThe metabolism of Granisetron can be decreased when combined with Dosulepin.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
DronedaroneThe metabolism of Granisetron can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Granisetron.Approved, Vet Approved
DuloxetineGranisetron may increase the serotonergic activities of Duloxetine.Approved
EletriptanGranisetron may increase the serotonergic activities of Eletriptan.Approved, Investigational
EliglustatThe metabolism of Granisetron can be decreased when combined with 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 serotonergic activities of Escitalopram.Approved, Investigational
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
FluoxetineThe metabolism of Granisetron can be decreased when combined with 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
LopinavirThe metabolism of Granisetron can be decreased when combined with 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
LumefantrineThe metabolism of Granisetron can be decreased when combined with Lumefantrine.Approved
ManidipineThe metabolism of Granisetron can be decreased when combined with Manidipine.Approved, Investigational
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
MidostaurinThe metabolism of Granisetron can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Granisetron can be increased when it is combined with Mifepristone.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
MoexiprilMoexipril may increase the QTc-prolonging activities of Granisetron.Approved
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
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
NilotinibThe metabolism of Granisetron can be decreased when combined with 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
QuinidineThe metabolism of Granisetron can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Granisetron can be decreased when combined with 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.Investigational, 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, Withdrawn
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, Withdrawn
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
ZiprasidoneThe metabolism of Granisetron can be decreased when combined with 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
KEGG Drug
D04370
KEGG Compound
C07023
PubChem Compound
5284566
PubChem Substance
46505137
ChemSpider
10482033
BindingDB
50443668
ChEBI
5537
ChEMBL
CHEMBL1290003
Therapeutic Targets Database
DAP000295
PharmGKB
PA449809
IUPHAR
2300
Guide to Pharmacology
GtP Drug Page
HET
CWB
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Granisetron
ATC Codes
A04AA02 — Granisetron
AHFS Codes
  • 56:22.20 — 5-HT3 Receptor Antagonists
PDB Entries
2yme
FDA label
Download (77.3 KB)
MSDS
Download (51.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers4
1CompletedNot AvailablePharmacokinetics1
1CompletedTreatmentCancers1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentProphylaxis against postoperative nausea and vomiting / Prophylaxis of acute chemotherapy induced nausea and vomiting1
1CompletedTreatmentProphylaxis of acute chemotherapy induced nausea and vomiting1
1Not Yet RecruitingTreatmentTumors, Solid1
1Not Yet RecruitingTreatmentProphylaxis of acute chemotherapy induced nausea and vomiting2
1TerminatedSupportive CareCancer, Breast / Nausea / Vomiting1
2CompletedPreventionCancers1
2CompletedPreventionSpinal Induced Shivering1
2CompletedPreventionProphylaxis of acute chemotherapy induced nausea and vomiting1
2CompletedSupportive CareNausea and Vomiting / Unspecified Adult Solid Tumor, Protocol Specific1
2CompletedSupportive CareCancer treatment / Nausea / Vomiting1
2CompletedSupportive CareVomiting1
2CompletedSupportive CareProphylaxis of acute chemotherapy induced nausea and vomiting1
2CompletedTreatmentMalignant Lymphomas1
2RecruitingTreatmentProphylaxis against postoperative nausea and vomiting1
2TerminatedPreventionNausea / Vomiting1
2WithdrawnSupportive CareMalignant Gliomas1
3Active Not RecruitingTreatmentCancer of the Cervix1
3CompletedPreventionProphylaxis of acute chemotherapy induced nausea and vomiting4
3CompletedSupportive CareNausea1
3CompletedSupportive CareNausea and Vomiting / Unspecified Adult Solid Tumor, Protocol Specific3
3CompletedTreatmentNausea / Vomiting1
3CompletedTreatmentProphylaxis of acute chemotherapy induced nausea and vomiting4
3RecruitingDiagnosticGastroparesis1
3Unknown StatusSupportive CareNausea and Vomiting / Testicular germ cell tumour1
3Unknown StatusSupportive CareUnspecified Adult Solid Tumor, Protocol Specific1
4CompletedTreatmentChemotherapy-induced Acute or Delayed Nausea and Vomiting (CINV)1
4CompletedTreatmentLeukemias / Malignant Lymphomas1
4CompletedTreatmentMyofascial Pain Syndrome / Temporomandibular Disorders1
4CompletedTreatmentProlonged QTc Interval1
4CompletedTreatmentProphylaxis against postoperative nausea and vomiting1
4Not Yet RecruitingPreventionSpinal-induced Hypotension1
4Not Yet RecruitingTreatmentCancers / Nausea / Vomiting1
4RecruitingPreventionGallstone formation1
4Unknown StatusTreatmentChemotherapy-induced Acute or Delayed Nausea and Vomiting (CINV)1
Not AvailableCompletedSupportive CareCancer, Breast / Cancer, Ovarian / Chronic Myeloproliferative Disorders / Gestational Trophoblastic Disease / Leukemias / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasms / Nausea and Vomiting / Neuroblastomas / Testicular germ cell tumour1
Not AvailableCompletedTreatmentNausea / Vomiting2
Not AvailableRecruitingNot AvailableArterial Hypotension / Cesarean Section Complications1
Not AvailableRecruitingPreventionProphylaxis against postoperative nausea and vomiting1
Not AvailableSuspendedSupportive CareMalignant Ovarian Mixed Epithelial Tumor / Nausea and Vomiting / Ovarian Brenner Tumor / Ovarian Clear Cell Cystadenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mucinous Cystadenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Cystadenocarcinoma / Stage II Ovarian Cancer / Stage IIA Fallopian Tube Cancer / Stage IIA Ovarian Cancer / Stage IIB Fallopian Tube Cancer / Stage IIB Ovarian Cancer / Stage IIC Fallopian Tube Cancer / Stage IIC Ovarian Cancer / Stage IIIA Fallopian Tube Cancer / Stage IIIA Ovarian Cancer / Stage IIIA Primary Peritoneal Cancer / Stage IIIB Fallopian Tube Cancer / Stage IIIB Ovarian Cancer / Stage IIIB Primary Peritoneal Cancer / Stage IIIC Fallopian Tube Cancer / Stage IIIC Ovarian Cancer / Stage IIIC Primary Peritoneal Cancer / Stage IV Fallopian Tube Cancer / Stage IV Ovarian Cancer / Stage IV Primary Peritoneal Cancer / Undifferentiated Ovarian Carcinoma1
Not AvailableUnknown StatusNot AvailableAntiemetic / Antiggaging Effect / Dental Situations / Gag Reflex / Granisetron1
Not AvailableUnknown StatusSupportive CareNon-Hodgkin's Lymphoma (NHL)1

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
InjectionIntravenous1 mg/mL
Injection, solutionIntravenous.1 mg/mL
Injection, solutionIntravenous1 mg/mL
InjectionIntravenous.1 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)
CA2158354No2004-07-132014-03-15Canada
CA2100777No2003-08-192012-01-16Canada
US7608282No2004-10-222024-10-22Us
US5952340No1996-09-142016-09-14Us
US6613355No2001-06-282021-06-28Us
US6790458No2001-05-112021-05-11Us
US8715710No2004-09-282024-09-28Us
US8252304No2004-09-282024-09-28Us
US8252305No2004-09-282024-09-28Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)219 °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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

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

Taxonomy

Description
This compound belongs to the class of organic compounds known as indazole-3-carboxamides. These are aromatic compounds containing an indazole ring system that is substituted at the 3-position with a carboxamide group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzopyrazoles
Sub Class
Indazoles
Direct Parent
Indazole-3-carboxamides
Alternative Parents
Pyrazole-5-carboxamides / 2-heteroaryl carboxamides / Piperidines / Benzenoids / Heteroaromatic compounds / Trialkylamines / Secondary carboxylic acid amides / Amino acids and derivatives / Azacyclic compounds / Organopnictogen compounds
show 3 more
Substituents
Indazole-3-carboxamide / 2-heteroaryl carboxamide / Pyrazole-5-carboxamide / Piperidine / Benzenoid / Azole / Heteroaromatic compound / Pyrazole / Amino acid or derivatives / Carboxamide group
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tertiary amino compound, monocarboxylic acid amide, indazoles (CHEBI:5537)

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-gate...
Gene Name
HTR3A
Uniprot ID
P46098
Uniprot Name
5-hydroxytryptamine receptor 3A
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
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
Substrate
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
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]

Drug created on June 13, 2005 07:24 / Updated on November 22, 2017 12:32