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Identification
NameGranisetron
Accession NumberDB00889  (APRD01002)
TypeSmall Molecule
GroupsApproved, 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 Identifiers
  • APF-530
  • APF530
  • BRL 43694
  • BRL-43694
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Granisetrontablet1 mgoralAa Pharma Inc2009-02-20Not applicableCanada
Granisetron Hydrochloride Injectionsolution1 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Granisetron Hydrochloride Injectionliquid1 mgintravenousOmega Laboratories Ltd2009-05-14Not 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 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
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Granisetroninjection, solution1 mg/mLintravenousFresenius Kabi USA, LLC2009-11-20Not applicableUs
Granisetroninjection, solution1 mg/mLintravenousFresenius Kabi USA, LLC2009-11-20Not applicableUs
Granisetroninjection, solution.1 mg/mLintravenousFresenius Kabi USA, LLC2009-11-20Not applicableUs
Granisetroninjection1 mg/mLintravenousSandoz Inc2008-06-30Not applicableUs
Granisetroninjection1 mg/mLintravenousSandoz Inc2008-06-30Not applicableUs
Granisetron Hydrochlorideinjection, solution1 mg/mLintravenousSagent Pharmaceuticals2010-12-01Not applicableUs
Granisetron Hydrochloridetablet1 mg/1oralRoxane Laboratories, Inc2008-05-16Not applicableUs
Granisetron Hydrochlorideinjection4 mg/4mLintravenousCipla USA Inc.2008-06-30Not applicableUs
Granisetron Hydrochlorideinjection1 mg/mLintravenousWOCKHARDT USA LLC2008-06-30Not applicableUs
Granisetron Hydrochlorideinjection1 mg/mLintravenousCipla USA Inc.2008-06-30Not applicableUs
Granisetron Hydrochlorideinjection, solution.1 mg/mLintravenousSagent Pharmaceuticals2010-12-01Not applicableUs
Granisetron Hydrochlorideinjection.1 mg/mLintravenousCipla Limited2007-12-31Not applicableUs
Granisetron Hydrochlorideinjection.1 mg/mLintravenousAkorn, Inc.2009-10-01Not applicableUs
Granisetron Hydrochloridetablet1 mg/1oralAscend Laboratories, LLC2010-01-01Not applicableUs
Granisetron Hydrochlorideinjection.1 mg/mLintravenousWockhardt Limited2008-03-03Not applicableUs
Granisetron Hydrochlorideinjection1 mg/mLintravenousAkorn, Inc.2009-10-01Not applicableUs
Granisetron Hydrochlorideinjection1 mg/mLintravenousWockhardt Limited2008-06-30Not applicableUs
Granisetron Hydrochloridetablet, film coated1 mg/1oralNorthstar Rx LLC2008-04-29Not applicableUs
Granisetron Hydrochloridetablet1 mg/1oralBreckenridge Pharmaceutical, Inc.2009-06-22Not applicableUs
Granisetron Hydrochlorideinjection1 mg/mLintravenousWest ward Pharmaceutical Corp2009-12-23Not applicableUs
Granisetron Hydrochloridetablet, film coated1 mg/1oralOrchid Pharma Inc2016-04-12Not applicableUs
Granisetron Hydrochloridetablet, film coated1 mg/1oralCore Pharma, Llc2007-12-312016-03-15Us
Granisetron Hydrochloridetablet, film coated1 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2010-05-28Not applicableUs
Granisetron Hydrochlorideinjection1 mg/mLintravenousWest ward Pharmaceutical Corp2009-12-23Not applicableUs
Granisetron Hydrochloridetablet, film coated1 mg/1oralAvera Mc Kennan Hospital2015-03-02Not applicableUs
Granisetron Hydrochlorideinjection.1 mg/mLintravenousWOCKHARDT USA LLC2008-03-03Not applicableUs
Granisetron Hydrochlorideinjection, solution1 mg/mLintravenousSagent Pharmaceuticals2010-12-01Not applicableUs
Granisetron Hydrochloridetablet, film coated1 mg/1oralTeva Pharmaceuticals USA Inc2008-01-02Not 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
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
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).
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.
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
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
Tabletoral1 mg
Injectionintravenous.1 mg/mL
Injectionintravenous1 mg/mL
Injectionintravenous4 mg/4mL
Injection, solutionintravenous.1 mg/mL
Injection, solutionintravenous1 mg/mL
Tabletoral1 mg/1
Tablet, film coatedoral1 mg/1
Liquidintravenous1 mg
Solutionintravenous1 mg
Patchtransdermal3.1 mg/24h
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
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)
Interactions
Drug Interactions
Drug
AlmotriptanGranisetron may increase the serotonergic activities of Almotriptan.
AmitriptylineGranisetron may increase the serotonergic activities of Amitriptyline.
AmoxapineGranisetron may increase the serotonergic activities of Amoxapine.
ApomorphineGranisetron may increase the hypotensive activities of Apomorphine.
BromocriptineGranisetron may increase the serotonergic activities of Bromocriptine.
BuspironeGranisetron may increase the serotonergic activities of Buspirone.
CabergolineGranisetron may increase the serotonergic activities of Cabergoline.
CitalopramGranisetron may increase the QTc-prolonging activities of Citalopram.
ClomipramineGranisetron may increase the serotonergic activities of Clomipramine.
CyclobenzaprineGranisetron may increase the serotonergic activities of Cyclobenzaprine.
DesipramineGranisetron may increase the serotonergic activities of Desipramine.
DesvenlafaxineGranisetron may increase the serotonergic activities of Desvenlafaxine.
DextromethorphanGranisetron may increase the serotonergic activities of Dextromethorphan.
DihydroergotamineGranisetron may increase the serotonergic activities of Dihydroergotamine.
DofetilideGranisetron may increase the QTc-prolonging activities of Dofetilide.
DoxepinGranisetron may increase the serotonergic activities of Doxepin.
DuloxetineGranisetron may increase the serotonergic activities of Duloxetine.
EletriptanGranisetron may increase the serotonergic activities of Eletriptan.
Ergoloid mesylateGranisetron may increase the serotonergic activities of Ergoloid mesylate.
ErgonovineGranisetron may increase the serotonergic activities of Ergonovine.
ErgotamineGranisetron may increase the serotonergic activities of Ergotamine.
EscitalopramGranisetron may increase the serotonergic activities of Escitalopram.
FentanylGranisetron may increase the serotonergic activities of Fentanyl.
FluoxetineGranisetron may increase the serotonergic activities of Fluoxetine.
FluvoxamineGranisetron may increase the serotonergic activities of Fluvoxamine.
FrovatriptanGranisetron may increase the serotonergic activities of Frovatriptan.
GoserelinGoserelin may increase the QTc-prolonging activities of Granisetron.
ImipramineGranisetron may increase the serotonergic activities of Imipramine.
IsocarboxazidGranisetron may increase the serotonergic activities of Isocarboxazid.
IvabradineIvabradine may increase the QTc-prolonging activities of Granisetron.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Granisetron.
LevomilnacipranGranisetron may increase the serotonergic activities of Levomilnacipran.
LinezolidGranisetron may increase the serotonergic activities of Linezolid.
LithiumGranisetron may increase the serotonergic activities of Lithium.
LorcaserinGranisetron may increase the serotonergic activities of Lorcaserin.
MaprotilineGranisetron may increase the serotonergic activities of Maprotiline.
MethadoneGranisetron may increase the serotonergic activities of Methadone.
MifepristoneMifepristone may increase the QTc-prolonging activities of Granisetron.
MilnacipranGranisetron may increase the serotonergic activities of Milnacipran.
MirtazapineGranisetron may increase the serotonergic activities of Mirtazapine.
MoclobemideGranisetron may increase the serotonergic activities of Moclobemide.
NaratriptanGranisetron may increase the serotonergic activities of Naratriptan.
NefazodoneGranisetron may increase the serotonergic activities of Nefazodone.
NortriptylineGranisetron may increase the serotonergic activities of Nortriptyline.
OctreotideOctreotide may increase the QTc-prolonging activities of Granisetron.
PanobinostatGranisetron may increase the arrhythmogenic activities of Panobinostat.
ParoxetineGranisetron may increase the serotonergic activities of Paroxetine.
PethidineGranisetron may increase the serotonergic activities of Pethidine.
PhenelzineGranisetron may increase the serotonergic activities of Phenelzine.
ProcarbazineGranisetron may increase the serotonergic activities of Procarbazine.
PromethazineGranisetron may increase the serotonergic activities of Promethazine.
ProtriptylineGranisetron may increase the serotonergic activities of Protriptyline.
RasagilineGranisetron may increase the serotonergic activities of Rasagiline.
RizatriptanGranisetron may increase the serotonergic activities of Rizatriptan.
SelegilineGranisetron may increase the serotonergic activities of Selegiline.
SertralineGranisetron may increase the serotonergic activities of Sertraline.
SumatriptanGranisetron may increase the serotonergic activities of Sumatriptan.
TapentadolGranisetron may decrease the analgesic activities of Tapentadol.
Tedizolid PhosphateGranisetron may increase the serotonergic activities of Tedizolid Phosphate.
TramadolGranisetron may decrease the analgesic activities of Tramadol.
TranylcypromineGranisetron may increase the serotonergic activities of Tranylcypromine.
TrazodoneGranisetron may increase the serotonergic activities of Trazodone.
TrimipramineGranisetron may increase the serotonergic activities of Trimipramine.
VenlafaxineGranisetron may increase the serotonergic activities of Venlafaxine.
VilazodoneGranisetron may increase the serotonergic activities of Vilazodone.
VortioxetineGranisetron may increase the serotonergic activities of Vortioxetine.
ZolmitriptanGranisetron may increase the serotonergic activities of Zolmitriptan.
Food Interactions
  • Take without regard to meals.

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 ]
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Drug created on June 13, 2005 07:24 / Updated on June 27, 2016 01:53