Identification
- Summary
Granisetron is a 5HT3 antagonist used to treat nausea and vomiting in cancer therapy and postoperatively.
- Brand Names
- Sancuso, Sustol
- Generic Name
- Granisetron
- DrugBank Accession Number
- DB00889
- Background
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Granisetron (DB00889)
- Weight
- Average: 312.417
Monoisotopic: 312.195011409 - Chemical Formula
- C18H24N4O
- Synonyms
- Granisétron
- Granisetrón
- Granisetron
- Granisetronum
- External IDs
- APF-530
- APF530
- BRL 43694
- BRL-43694
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).
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prevention of Nausea and vomiting •••••••••••• Treatment of Nausea and vomiting ••• ••••• Prevention of Nausea and vomiting ••• ••••• Prevention of Nausea and vomiting •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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.
Target Actions Organism A5-hydroxytryptamine receptor 3A antagonistHumans - 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.
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- 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]
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
LD50>2000 mg/kg (rat, oral)
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Granisetron is combined with 1,2-Benzodiazepine. Abametapir The serum concentration of Granisetron can be increased when it is combined with Abametapir. Acenocoumarol The risk or severity of adverse effects can be increased when Granisetron is combined with Acenocoumarol. Acetazolamide The risk or severity of CNS depression can be increased when Acetazolamide is combined with Granisetron. Acetophenazine The risk or severity of CNS depression can be increased when Granisetron is combined with Acetophenazine. - Food Interactions
- Take with or without food. The absorption is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Granisetron hydrochloride 318F6L70J8 107007-99-8 QYZRTBKYBJRGJB-WQTKJZBYSA-N - Product Images
- International/Other Brands
- Kevatril / Sancuso / Sustol
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Granisetron Hydrochloride Injection Liquid 1 mg / mL Intravenous Sandoz Canada Incorporated 2009-02-20 2019-08-01 Canada 
Granisetron Hydrochloride Injection Solution 1 mg / mL Intravenous Strides Pharma Canada Inc Not applicable Not applicable Canada Granisetron Hydrochloride Injection Liquid 1 mg / mL Intravenous Omega Laboratories Ltd 2009-05-14 Not applicable Canada Granisetron Hydrochloride Injection Sdz Solution 1 mg / mL Intravenous Sandoz Canada Incorporated 2012-12-19 2019-08-01 Canada Kytril Injection, solution 1 mg/1mL Intravenous Genentech, Inc. 1993-12-29 2010-07-31 US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-granisetron Tablet 1 mg Oral Apotex Corporation 2009-02-20 Not applicable Canada Granisetron Injection, solution 1 mg/1mL Intravenous Fresenius Kabi USA, LLC 2009-11-20 Not applicable US Granisetron Injection 1 mg/1mL Intravenous Sandoz Inc. 2008-06-30 2020-05-19 US Granisetron Injection, solution 1 mg/1mL Intravenous Fresenius Kabi USA, LLC 2009-11-20 2024-05-31 US Granisetron Injection 1 mg/1mL Intravenous Sandoz Inc. 2008-06-30 2020-05-19 US
Categories
- ATC Codes
- A04AA02 — Granisetron
- Drug Categories
- Alimentary Tract and Metabolism
- Antidepressive Agents
- Antiemetic Serotonin 5-HT3 Receptor Antagonists
- Antiemetics
- Antiemetics and Antinauseants
- Autonomic Agents
- Aza Compounds
- Azabicyclo Compounds
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Gastrointestinal Agents
- Heterocyclic Compounds, Fused-Ring
- Indazoles
- Moderate Risk QTc-Prolonging Agents
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Pyrazoles
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin 3 Receptor Antagonists
- Serotonin 5-HT3 Receptor Antagonists
- Serotonin Agents
- Serotonin Receptor Antagonists
- Chemical TaxonomyProvided by Classyfire
- 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
- 2-heteroaryl carboxamide / Amine / Amino acid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzenoid / Carboxamide group / Carboxylic acid derivative / Heteroaromatic compound show 14 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- tertiary amino compound, monocarboxylic acid amide, indazoles (CHEBI:5537)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- WZG3J2MCOL
- CAS number
- 109889-09-0
- 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[C@@H]2C[C@@H]3CCC[C@H](C2)N3C)C2=C1C=CC=C2
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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- External Links
- KEGG Drug
- D04370
- KEGG Compound
- C07023
- PubChem Compound
- 5284566
- PubChem Substance
- 46505137
- ChemSpider
- 10482033
- BindingDB
- 50443668
- 26237
- ChEBI
- 5537
- ChEMBL
- CHEMBL1290003
- ZINC
- ZINC000100018854
- Therapeutic Targets Database
- DAP000295
- PharmGKB
- PA449809
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- CWB
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Granisetron
- PDB Entries
- 2yme / 6np0
- FDA label
- Download (77.3 KB)
- MSDS
- Download (51.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Prevention Chemotherapy-Induced Nausea and Vomiting 1 4 Completed Prevention Gallstones 1 4 Completed Prevention Post Operative Nausea and Vomiting (PONV) 1 4 Completed Treatment Chemotherapy-Induced Nausea and Vomiting 1 4 Completed Treatment Leukemias / Lymphoma 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
- Akorn Inc.
- Amerigen Pharmaceuticals Inc.
- Apotex Inc.
- APP Pharmaceuticals
- Ascend Laboratories LLC
- Aveva Drug Delivery Systems Inc.
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Cipla Ltd.
- Corepharma LLC
- Cura Pharmaceutical Co. Inc.
- DAVA Pharmaceuticals
- Doctor Reddys Laboratories Ltd.
- Ebewe Pharma
- F Hoffmann La Roche Ltd.
- F Hoffmann-La Roche Ltd.
- GlaxoSmithKline Inc.
- Hawthorn Pharmaceuticals
- Hikma Pharmaceuticals
- Mylan
- Neuman Distributors Inc.
- Northstar Rx LLC
- Orchid Healthcare
- Physicians Total Care Inc.
- Prostrakan Inc.
- Roxane Labs
- Taro Pharmaceuticals USA
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- West-Ward Pharmaceuticals
- Wockhardt Ltd.
- Dosage Forms
Form Route Strength Injection Parenteral 1 MG/ML Tablet Oral 1 mg Tablet Oral 1.0 mg Injection Parenteral 3 mg/3ml Injection Solution Intravenous 1 mg Injection, solution 3 mg/3ml Injection, solution Tablet, film coated Oral Injection, solution Intravenous bolus; Intravenous drip 1 MG/ML Solution Parenteral 1 MG/1ML Solution Parenteral 3 MG/3ML Tablet, film coated Oral 1 MG Injection, solution 1 MG/ML Injection, solution, concentrate Intravenous; Parenteral 1 MG/ML Solution Parenteral 1 MG/ML Injection Intravenous Injection Intravenous 0.1 mg/1mL Injection Intravenous 1 mg/1mL Injection Intravenous 4 mg/4mL Injection, solution Intravenous 1.12 mg/1mL Injection, solution Intravenous 4 mg/4mL Solution Intravenous 1 mg/1mL Solution Intravenous 4 mg/4mL Tablet Oral 1 mg/1 Liquid Intravenous 1 mg / mL Solution Intravenous 1 mg / mL Solution, concentrate Parenteral 1 MG/ML Injection, solution Parenteral 1 MG/1ML Solution Intravenous Injection 3 mg/3ml Injection, solution Parenteral 3 MG/3ML Solution Intravenous 1 mg/ml Injection, solution Intramuscular; Intravenous 1 mg/ml Solution Oral 2 mg/10mL Injection, solution Intravenous 3 mg/3ml Solution 1 mg/ml Solution Parenteral 1 mg Injection, solution Intramuscular; Parenteral 3 MG/1ML Injection, solution Intravenous 0.1 mg/1mL Injection, solution Intravenous 1 mg/1mL Injection, solution Intravenous 1 mg/4mL Injection, solution Intravenous; Parenteral 1 MG/1ML Injection, solution Intravenous; Parenteral 3 MG/3ML Injection, solution Intravenous; Parenteral 3 MG/5ML Solution Oral 0.2 MG/ML Tablet, film coated Oral 1 mg/1 Injection, solution Parenteral 3 mg Solution Intravenous 3 mg/3ml Injection Intravenous 1 mg/ml Injection Intravenous 3 mg/3ml Solution Parenteral 300000 mg Tablet, film coated Oral 2 mg Solution, concentrate Parenteral Solution Parenteral 3 MG Patch Transdermal 3.1 mg/24h Patch Transdermal 3.1 MG Patch, extended release Transdermal 34.3 mg Solution Intravenous 1.12 mg Solution Intravenous 3.000 mg Injection Subcutaneous 10 mg/0.4mL Injection, solution Intramuscular Injection, solution Intravenous Solution Oral Tablet Oral Solution Parenteral Solution Intravenous 1.00 mg Injection Parenteral Solution Tablet Oral 1.000 mg - Prices
Unit description Cost Unit Sancuso 3.1 mg/24 hr patch 372.0USD patch Kytril 2 1 mg tablet Box 131.98USD box Kytril 1 mg tablet 62.94USD tablet Granisetron hcl 1 mg tablet 60.19USD tablet Granisetron hcl 4 mg/4 ml vial 24.0USD ml Kytril 1 mg Tablet 20.27USD tablet Apo-Granisetron 1 mg Tablet 14.14USD tablet Kytril 0.1 mg/ml vial 11.54USD ml Granisetron hcl 0.1 mg/ml vial 7.2USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2158354 No 2004-07-13 2014-03-15 Canada CA2100777 No 2003-08-19 2012-01-16 Canada US7608282 No 2009-10-27 2024-10-22 US US5952340 No 1999-09-14 2016-09-14 US US6613355 No 2003-09-02 2021-06-28 US US6790458 No 2004-09-14 2021-05-11 US US8715710 No 2014-05-06 2024-09-28 US US8252304 No 2012-08-28 2024-09-28 US US8252305 No 2012-08-28 2024-09-28 US US9913910 No 2018-03-13 2024-09-28 US US10357570 No 2019-07-23 2024-09-28 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 219 °C (HCl salt) Not Available logP 2.6 Not Available - Predicted Properties
Property Value Source Water Solubility 0.434 mg/mL ALOGPS logP 2.64 ALOGPS logP 1.88 Chemaxon logS -2.9 ALOGPS pKa (Strongest Acidic) 14.75 Chemaxon pKa (Strongest Basic) 9 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 50.16 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 101.83 m3·mol-1 Chemaxon Polarizability 35.57 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9947 Blood Brain Barrier + 0.9515 Caco-2 permeable + 0.5231 P-glycoprotein substrate Substrate 0.5473 P-glycoprotein inhibitor I Inhibitor 0.6287 P-glycoprotein inhibitor II Inhibitor 0.7243 Renal organic cation transporter Non-inhibitor 0.5895 CYP450 2C9 substrate Non-substrate 0.7898 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.6978 CYP450 1A2 substrate Non-inhibitor 0.8546 CYP450 2C9 inhibitor Non-inhibitor 0.9019 CYP450 2D6 inhibitor Non-inhibitor 0.8841 CYP450 2C19 inhibitor Non-inhibitor 0.9073 CYP450 3A4 inhibitor Non-inhibitor 0.8355 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.6016 Ames test Non AMES toxic 0.5878 Carcinogenicity Non-carcinogens 0.8464 Biodegradation Not ready biodegradable 0.9868 Rat acute toxicity 2.3943 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9083 hERG inhibition (predictor II) Inhibitor 0.5458
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0009000000-775096476371af54ef72 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0209000000-7e27a19ff60407e27c5f Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0029000000-8ce3b7b737db8386d04c Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-3009000000-ee8fa73e1d03d45f3da7 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0n2c-1920000000-241b3671c602cba62b06 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0f6x-9720000000-4d7f3f6dd26fb5714ede Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 185.0252882 predictedDarkChem Lite v0.1.0 [M-H]- 175.57648 predictedDeepCCS 1.0 (2019) [M+H]+ 184.7835882 predictedDarkChem Lite v0.1.0 [M+H]+ 177.93448 predictedDeepCCS 1.0 (2019) [M+Na]+ 184.6659882 predictedDarkChem Lite v0.1.0 [M+Na]+ 184.76445 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Abdelsayed GG: Management of radiation-induced nausea and vomiting. Exp Hematol. 2007 Apr;35(4 Suppl 1):34-6. [Article]
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Bustos ML, Zhao Y, Chen H, Caritis SN, Venkataramanan R: Polymorphisms in CYP1A1 and CYP3A5 Genes Contribute to the Variability in Granisetron Clearance and Exposure in Pregnant Women with Nausea and Vomiting. Pharmacotherapy. 2016 Dec;36(12):1238-1244. doi: 10.1002/phar.1860. Epub 2016 Dec 5. [Article]
- Lang D, Radtke M, Bairlein M: Highly Variable Expression of CYP1A1 in Human Liver and Impact on Pharmacokinetics of Riociguat and Granisetron in Humans. Chem Res Toxicol. 2019 Jun 17;32(6):1115-1122. doi: 10.1021/acs.chemrestox.8b00413. Epub 2019 Apr 16. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55