Identification

Name
Palonosetron
Accession Number
DB00377
Description

Palonosetron (INN, trade name Aloxi) is an antagonist of 5-HT3 receptors that is indicated for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy and is the only drug of its class approved for this use by the U.S. Food and Drug Administration. As of 2008, it is the most recent 5-HT3 antagonist to enter clinical use.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 296.414
Monoisotopic: 296.188863401
Chemical Formula
C19H24N2O
Synonyms
  • (3aS)-2-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one
  • 2-(1-Azabicyclo(2.2.2)oct-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benz(de)isoquinolin-1-one
  • Palonosetron
  • Palonosétron
  • Palonosetrón
  • Palonosetronum
External IDs
  • 2-Qhbiqo
  • RS 25259
  • RS 25259-197

Pharmacology

Indication

For the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy, as well as prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy. Also used for the prevention of postoperative nausea and vomiting for up to 24 hours post operation.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Palonosetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Palonosetron is a highly specific and selective serotonin 5-HT3 receptor antagonist that is pharmacologically related to other 5-HT3 receptor antagonists, but differs structurally. Palonosetron has a high affinity for 5-HT3 receptors, but has little to no affinity for other 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. It is suggested 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

Palonosetron is a selective serotonin 5-HT3 receptor antagonist. 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. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT3 receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron's potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy.

TargetActionsOrganism
A5-hydroxytryptamine receptor 3A
antagonist
Humans
Absorption

Low oral bioavailability.

Volume of distribution
  • 8.3 ± 2.5 L/kg
Protein binding

62%

Metabolism

Hepatic (50%), primarily CYP2D6-mediated, although CYP3A4 and CYP1A2 are also involved.

Route of elimination

After a single intravenous dose of 10 mcg/kg [14C]-palonosetron, approximately 80% of the dose was recovered within 144 hours in the urine

Half-life

Approximately 40 hours

Clearance
  • 160 +/- 35 mL/h/kg
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

A single intravenous dose of palonosetron at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AbacavirPalonosetron may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbametapirThe serum concentration of Palonosetron can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Palonosetron can be increased when combined with Abatacept.
AbirateroneThe metabolism of Palonosetron can be decreased when combined with Abiraterone.
AcarboseAcarbose may decrease the excretion rate of Palonosetron which could result in a higher serum level.
AcebutololThe metabolism of Palonosetron can be decreased when combined with Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Palonosetron which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Palonosetron which could result in a higher serum level.
AcenocoumarolThe risk or severity of adverse effects can be increased when Palonosetron is combined with Acenocoumarol.
AcetaminophenAcetaminophen may decrease the excretion rate of Palonosetron which could result in a higher serum level.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
  • Take with or without food.

Products

Product Ingredients
IngredientUNIICASInChI Key
Palonosetron hydrochloride23310D4I19135729-62-3OLDRWYVIKMSFFB-SSPJITILSA-N
International/Other Brands
Jiouting (Jiuyuan Gene Engineering) / Onicit (Pfizer) / Palnox (Glenmark) / Paloxi (Kalbe) / Palzen (Dr. Reddy's) / Themiset (Themis Medicare) / Zhiruo (Chia Tai Tianqing)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AloxiInjection, solution250 μgIntravenousHelsinn Birex Pharmaceuticals Ltd.2005-03-22Not applicableEU flag
AloxiInjection0.075 mg/1.5mLIntravenousEisai Limited2014-05-28Not applicableUS flag
AloxiCapsule500 μgOralHelsinn Birex Pharmaceuticals Ltd.2005-03-22Not applicableEU flag
AloxiSolution0.25 mgIntravenousElvium Life Sciences2012-07-19Not applicableCanada flag
AloxiInjection0.25 mg/5mLIntravenousEisai Limited2014-05-28Not applicableUS flag
AloxiInjection0.05 mg/1mLIntravenousHelsinn Therapeutics (U.S.), Inc.2018-11-01Not applicableUS flag
AloxiCapsule500 μgOralHelsinn Birex Pharmaceuticals Ltd.2005-03-22Not applicableEU flag
AloxiCapsule, gelatin coated0.5 mg/1OralEisai Limited2008-08-222010-05-31US flag
AloxiCapsule0.5 mgOralElvium Life Sciences2012-08-07Not applicableCanada flag
AloxiInjection0.075 mg/1.5mLIntravenousMGI PHARMA2008-09-23Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PalonosetronInjection, solution0.25 mg/5mLIntravenousFresenius Kabi USA, LLC2018-09-19Not applicableUS flag
PalonosetronInjection, solution0.05 mg/1mLIntravenousDr.Reddy's Laboratories Limited2018-03-23Not applicableUS flag
PalonosetronInjection0.25 mg/5mLIntravenousQilu Pharmaceutical Co., Ltd.2018-09-19Not applicableUS flag
PalonosetronInjection, solution0.05 mg/1mLIntravenousNorthStar Rx LLC2018-05-29Not applicableUS flag
PalonosetronInjection, solution0.05 mg/1mLIntravenousBluePoint Laboratories2018-05-30Not applicableUS flag
PalonosetronInjection0.25 mg/5mLIntravenousApotex Corp.2018-09-19Not applicableUS flag
PalonosetronInjection0.075 mg/1.5mLIntravenousQilu Pharmaceutical Co., Ltd.2018-09-19Not applicableUS flag
Palonosetron HospiraInjection, solution250 μgIntravenousHospira, Inc.2016-04-08Not applicableEU flag
Palonosetron HydrochlorideInjection, solution0.075 mg/1.5mLIntravenousHospira, Inc.2018-11-142018-11-14US flag
Palonosetron HydrochlorideInjection0.25 mg/5mLIntravenousAccord Healthcare, Inc.2018-03-23Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AkynzeoPalonosetron (0.5 mg/1) + Netupitant (300 mg/1)CapsuleOralEisai Limited2014-10-132018-05-31US flag
AkynzeoPalonosetron hydrochloride (0.28 mg/1) + Fosnetupitant (260 mg/1)InjectionIntravenousHelsinn Therapeutics (U.S.), Inc.2018-04-20Not applicableUS flag
AkynzeoPalonosetron (0.5 mg) + Netupitant (300 mg)CapsuleOralElvium Life Sciences2017-11-20Not applicableCanada flag
AkynzeoPalonosetron (0.5 mg/1) + Netupitant (300 mg/1)CapsuleOralHelsinn Therapeutics (U.S.), Inc.2014-10-13Not applicableUS flag
AkynzeoPalonosetron hydrochloride (0.28 mg/20mL) + Fosnetupitant (260 mg/20mL)InjectionIntravenousHelsinn Therapeutics (U.S.), Inc.2020-06-15Not applicableUS flag

Categories

ATC Codes
A04AA55 — Palonosetron, combinationsA04AA05 — Palonosetron
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as isoquinolones and derivatives. These are aromatic polycyclic compounds containing a ketone bearing isoquinoline moiety.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Isoquinolines and derivatives
Sub Class
Isoquinolones and derivatives
Direct Parent
Isoquinolones and derivatives
Alternative Parents
Tetralins / Tetrahydroisoquinolines / Quinuclidines / Piperidines / Tertiary carboxylic acid amides / Trialkylamines / Lactams / Amino acids and derivatives / Azacyclic compounds / Organopnictogen compounds
show 3 more
Substituents
Amine / Amino acid or derivatives / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carboxamide group / Carboxylic acid derivative / Hydrocarbon derivative / Isoquinolone / Lactam
show 13 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
azabicycloalkane, organic heterotricyclic compound, delta-lactam (CHEBI:85161)

Chemical Identifiers

UNII
5D06587D6R
CAS number
135729-56-5
InChI Key
CPZBLNMUGSZIPR-NVXWUHKLSA-N
InChI
InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1
IUPAC Name
(5S)-3-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3-azatricyclo[7.3.1.0⁵,¹³]trideca-1(12),9(13),10-trien-2-one
SMILES
[H][[email protected]]12CCCC3=C1C(=CC=C3)C(=O)N(C2)[[email protected]@H]1CN2CCC1CC2

References

Synthesis Reference

Pierluigi Rossetto, Peter MacDonald, Ettore Bigatti, Gaia Banfi, Dario Tentorio, "Processes for preparing palonosetron salts." U.S. Patent US20080200681, issued August 21, 2008.

US20080200681
General References
  1. De Leon A: Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent). 2006 Oct;19(4):413-6. [PubMed:17106506]
  2. Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. [PubMed:15102873]
  3. Rubenstein EB: Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9. [PubMed:16163194]
  4. Yang LP, Scott LJ: Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000. [PubMed:19852528]
  5. Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. [PubMed:15139789]
  6. Eisenberg P, MacKintosh FR, Ritch P, Cornett PA, Macciocchi A: Efficacy, safety and pharmacokinetics of palonosetron in patients receiving highly emetogenic cisplatin-based chemotherapy: a dose-ranging clinical study. Ann Oncol. 2004 Feb;15(2):330-7. [PubMed:14760130]
  7. Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. [PubMed:15378559]
KEGG Drug
D07175
PubChem Compound
6337614
PubChem Substance
46508530
ChemSpider
4892289
BindingDB
50417287
RxNav
70561
ChEBI
85161
ChEMBL
CHEMBL1189679
ZINC
ZINC000003795819
Therapeutic Targets Database
DAP000367
PharmGKB
PA10352
PDBe Ligand
O7B
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Palonosetron
AHFS Codes
  • 56:22.00 — Antiemetics
PDB Entries
6y1z
FDA label
Download (185 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionAnaesthesia therapy / Palonosetron / Ponv1
4CompletedPreventionNausea / Neoplasms / Vomiting2
4CompletedPreventionPonv1
4CompletedPreventionPost Operative Nausea and Vomiting (PONV)4
4CompletedSupportive CareMalignancies / Tumors1
4CompletedSupportive CarePonv1
4CompletedTreatmentChemotherapy-Induced Nausea and Vomiting (CINV) / Neoplasms1
4CompletedTreatmentLeukemias / Malignant Lymphomas1
4CompletedTreatmentPain1
4Not Yet RecruitingTreatmentAntiemetic / Post Operative Nausea and Vomiting (PONV)1

Pharmacoeconomics

Manufacturers
  • Helsinn healthcare sa
Packagers
  • Cardinal Health
  • Catalent Pharma Solutions
  • Eisai Inc.
  • MGI Pharma
  • Oso Biopharmaceuticals Manufacturing LLC
  • Pierre Fabre
  • Sicor Pharmaceuticals
Dosage Forms
FormRouteStrength
Capsule300 mg
CapsuleOral
CapsuleOral300 MG
InjectionIntravenous
Injection, powder, for solutionIntravenous235 MG
CapsuleOral0.5 mg/0.5mg
CapsuleOral0.5 mg
CapsuleOral500 μg
Capsule, gelatin coatedOral0.5 mg/1
InjectionIntravenous0.05 mg/1mL
InjectionIntravenous0.075 mg/1.5mL
InjectionIntravenous0.25 mg/5mL
Injection, solutionIntravenous250 μg
Injection, solutionIntravenous; Parenteral250 MCG
Injection, solutionIntravenous250 mcg/5ml
CapsuleOral
Injection250 mcg/5ml
SolutionIntravenous250 mcg
SolutionIntravenous0.25 mg
Injection, solutionIntravenous; Parenteral250 MICROGRAMMI
Injection, solutionIntravenous250 MCG
Injection, solutionParenteral250 Mikrogramm
InjectionIntravenous.25 mg/2mL
Injection, solutionIntravenous0.05 mg/1mL
Injection, solutionIntravenous0.075 mg/1.5mL
Injection, solutionIntravenous0.25 mg/5mL
Injection, solutionParenteral250 MICROGRAMMI
Injection
Injection, solution250 mcg/5ml
Prices
Unit descriptionCostUnit
Aloxi 0.075 mg/1.5 ml vial52.8USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9125905Yes2015-09-082024-07-30US flag
US8518981Yes2013-08-272024-07-30US flag
US7947725Yes2011-05-242024-07-30US flag
US8598218Yes2013-12-032024-07-30US flag
US7960424Yes2011-06-142024-07-30US flag
US9173942Yes2015-11-032024-07-30US flag
US7947724Yes2011-05-242024-07-30US flag
US8598219Yes2013-12-032024-07-30US flag
US8729094Yes2014-05-202024-07-30US flag
US9066980Yes2015-06-302024-07-30US flag
US9186357No2015-11-172030-11-18US flag
US8623826No2014-01-072030-11-18US flag
US8951969No2015-02-102030-11-18US flag
US6297375No2001-10-022020-02-22US flag
US5202333Yes1993-04-132015-10-13US flag
US9457020Yes2016-10-042024-07-30US flag
US9439854Yes2016-09-132024-07-30US flag
US9457021Yes2016-10-042024-07-30US flag
US9271975No2016-03-012031-09-09US flag
US9943515No2018-04-172030-11-18US flag
US9403772No2016-08-022032-05-23US flag
US8895586No2014-11-252032-05-23US flag
US9908907No2018-03-062032-05-23US flag
US9951016No2018-04-242035-09-25US flag
US8426450No2013-04-232032-05-23US flag
US10208073No2019-02-192032-05-23US flag
US10233154No2019-03-192035-09-25US flag
US10624911No2017-06-022037-06-02US flag
US10676440No2015-09-252035-09-25US flag
US10717721No2012-05-232032-05-23US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.464 mg/mLALOGPS
logP2.72ALOGPS
logP2.55ChemAxon
logS-2.8ALOGPS
pKa (Strongest Basic)7.97ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area23.55 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity88.52 m3·mol-1ChemAxon
Polarizability33.9 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9899
Blood Brain Barrier+0.9953
Caco-2 permeable+0.5986
P-glycoprotein substrateSubstrate0.679
P-glycoprotein inhibitor IInhibitor0.8643
P-glycoprotein inhibitor IINon-inhibitor0.6745
Renal organic cation transporterInhibitor0.5763
CYP450 2C9 substrateNon-substrate0.83
CYP450 2D6 substrateSubstrate0.7618
CYP450 3A4 substrateSubstrate0.6446
CYP450 1A2 substrateInhibitor0.6626
CYP450 2C9 inhibitorNon-inhibitor0.541
CYP450 2D6 inhibitorNon-inhibitor0.7502
CYP450 2C19 inhibitorInhibitor0.9367
CYP450 3A4 inhibitorInhibitor0.6002
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7828
Ames testNon AMES toxic0.8664
CarcinogenicityNon-carcinogens0.9557
BiodegradationNot ready biodegradable0.9762
Rat acute toxicity2.7383 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.883
hERG inhibition (predictor II)Inhibitor0.6891
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 GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-0190000000-ae8443b987d38522ce30

Targets

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
  1. Hesketh PJ: New treatment options for chemotherapy-induced nausea and vomiting. Support Care Cancer. 2004 Aug;12(8):550-4. Epub 2004 Jun 30. [PubMed:15232725]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  3. Grunberg SM, Koeller JM: Palonosetron: a unique 5-HT3-receptor antagonist for the prevention of chemotherapy-induced emesis. Expert Opin Pharmacother. 2003 Dec;4(12):2297-303. [PubMed:14640928]
  4. Rubenstein EB: Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9. [PubMed:16163194]
  5. Eisenberg P, Figueroa-Vadillo J, Zamora R, Charu V, Hajdenberg J, Cartmell A, Macciocchi A, Grunberg S: Improved prevention of moderately emetogenic chemotherapy-induced nausea and vomiting with palonosetron, a pharmacologically novel 5-HT3 receptor antagonist: results of a phase III, single-dose trial versus dolasetron. Cancer. 2003 Dec 1;98(11):2473-82. [PubMed:14635083]
  6. Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. [PubMed:15102873]
  7. De Leon A: Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent). 2006 Oct;19(4):413-6. [PubMed:17106506]
  8. Yang LP, Scott LJ: Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000. [PubMed:19852528]
  9. Navari RM: Palonosetron: a second-generation 5-hydroxytryptamine receptor antagonist. Future Oncol. 2006 Oct;2(5):591-602. [PubMed:17026451]
  10. Gralla R, Lichinitser M, Van Der Vegt S, Sleeboom H, Mezger J, Peschel C, Tonini G, Labianca R, Macciocchi A, Aapro M: Palonosetron improves prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy: results of a double-blind randomized phase III trial comparing single doses of palonosetron with ondansetron. Ann Oncol. 2003 Oct;14(10):1570-7. [PubMed:14504060]
  11. Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. [PubMed:15139789]
  12. Eisenberg P, MacKintosh FR, Ritch P, Cornett PA, Macciocchi A: Efficacy, safety and pharmacokinetics of palonosetron in patients receiving highly emetogenic cisplatin-based chemotherapy: a dose-ranging clinical study. Ann Oncol. 2004 Feb;15(2):330-7. [PubMed:14760130]
  13. Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. [PubMed:15378559]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. [PubMed:15378559]
  2. Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. [PubMed:15102873]
  3. 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]
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
  1. Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. [PubMed:15378559]
  2. Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. [PubMed:15102873]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous [l4C]-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37. [PubMed:15378559]
  2. Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31. [PubMed:15102873]
  3. Palonosetron FDA label [File]

Drug created on June 13, 2005 07:24 / Updated on October 25, 2020 09:16

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