Identification
- Summary
Palonosetron is a serotonin antagonist used in the prophylaxis or management of vomiting that results from emetogenic chemotherapy, and for the management of postoperative nausea and vomiting.
- Brand Names
- Akynzeo, Aloxi
- Generic Name
- Palonosetron
- DrugBank Accession Number
- DB00377
- Background
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
Structure for Palonosetron (DB00377)
- 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.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for prophylaxis of Nausea post chemotherapy Regimen in combination with: Netupitant (DB09048) •••••••••••• Prophylaxis of Postoperative nausea and vomiting •••••••••••• ••••• •••••••••• •••••••••• •••••••• Prophylaxis of Acute chemotherapy induced nausea and vomiting •••••••••••• •••••• ••••••••• •••••••••• •••••••••• •••••••• Prophylaxis of Acute chemotherapy induced nausea and vomiting •••••••••••• ••••• Prophylaxis of Acute chemotherapy induced nausea and vomiting •••••••••••• •••••• ••••••••• •••••••••• •••••••••• •••••••• - Contraindications & Blackbox Warnings
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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.
Target Actions Organism A5-hydroxytryptamine receptor 3A antagonistHumans - 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
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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.
- 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 Palonosetron is combined with 1,2-Benzodiazepine. Abacavir Palonosetron may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Palonosetron can be increased when it is combined with Abametapir. Abatacept The metabolism of Palonosetron can be increased when combined with Abatacept. Abiraterone The metabolism of Palonosetron can be decreased when combined with Abiraterone. - Food Interactions
- Take with or without 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 Palonosetron hydrochloride 23310D4I19 135729-62-3 OLDRWYVIKMSFFB-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
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Aloxi Capsule 500 μg Oral Helsinn Birex Pharmaceuticals Ltd. 2016-09-08 Not applicable EU 
Aloxi Injection 0.25 mg/5mL Intravenous Eisai Inc. 2014-05-28 2022-10-31 US 
Aloxi Capsule 500 μg Oral Helsinn Birex Pharmaceuticals Ltd. 2016-09-08 Not applicable EU Aloxi Solution 0.25 mg / 5 mL Intravenous Knight Therapeutics Inc. 2012-07-19 Not applicable Canada 
Aloxi Injection 0.05 mg/1mL Intravenous Helsinn Therapeutics (U.S.), Inc. 2018-11-01 2022-11-01 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Palonosetron Injection, solution 0.05 mg/1mL Intravenous NorthStar Rx LLC 2018-05-29 Not applicable US Palonosetron Injection 0.25 mg/5mL Intravenous Apotex Corp. 2018-09-19 Not applicable US Palonosetron Injection 0.25 mg/5mL Intravenous BluePoint Laboratories 2021-01-25 2023-07-31 US Palonosetron Injection 0.25 mg/5mL Intravenous Qilu Pharmaceutical Co., Ltd. 2018-09-19 Not applicable US Palonosetron Injection, solution 0.05 mg/1mL Intravenous BluePoint Laboratories 2018-05-30 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Akynzeo Palonosetron hydrochloride (0.50 mg) + Netupitant (300 mg) Capsule Oral Helsinn Birex Pharmaceuticals Ltd 2020-12-22 Not applicable EU AKYNZEO Palonosetron (0.5 MG) + Netupitant (300 MG) Capsule Oral Helsinn Birex Pharmaceuticals Ltd 2019-03-01 Not applicable Italy 
Akynzeo Palonosetron (0.5 mg/1) + Netupitant (300 mg/1) Capsule Oral Helsinn Therapeutics (U.S.), Inc. 2014-10-13 Not applicable US Akynzeo Palonosetron hydrochloride (0.25 mg) + Netupitant (235 mg) Injection, solution, concentrate Intravenous Helsinn Birex Pharmaceuticals Ltd 2022-05-04 Not applicable EU Akynzeo Palonosetron hydrochloride (0.50 mg) + Netupitant (300 mg) Capsule Oral Helsinn Birex Pharmaceuticals Ltd 2016-09-08 Not applicable EU - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image PALOXITRON 250 MCG/5 ML IV ENJEKSIYON ICIN COZELTI ICEREN 1 AMPUL Palonosetron (250 mcg/5ml) Injection, solution Intravenous PHARMADA İLAÇ SAN. VE TİC. A.Ş. 2018-02-20 2024-01-23 Turkey 
VOTRON 250 MCG/5 ML ENJEKSIYONLUK COZELTI ICEREN FLAKON Palonosetron (250 mcg/5ml) Injection, solution BİEM İLAÇ SAN. VE TİC. A.Ş. 2013-01-29 Not applicable Turkey
Categories
- ATC Codes
- A04AA55 — Palonosetron, combinations
- A04AA — Serotonin (5HT3) antagonists
- A04A — ANTIEMETICS AND ANTINAUSEANTS
- A04 — ANTIEMETICS AND ANTINAUSEANTS
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Alimentary Tract and Metabolism
- Antidepressive Agents
- Antiemetic Serotonin 5-HT3 Receptor Antagonists
- Antiemetics
- Antiemetics and Antinauseants
- Autonomic Agents
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Gastrointestinal Agents
- Heterocyclic Compounds, Fused-Ring
- Isoquinolines
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Quinuclidines
- 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 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)
- Affected organisms
- Humans and other mammals
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][C@]12CCCC3=C1C(=CC=C3)C(=O)N(C2)[C@@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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. [Article]
- 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. [Article]
- 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. [Article]
- External Links
- KEGG Drug
- D07175
- PubChem Compound
- 6337614
- PubChem Substance
- 46508530
- ChemSpider
- 4892289
- BindingDB
- 50417287
- 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
- PDB Entries
- 6w1y / 6y1z
- FDA label
- Download (185 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 Completed Other Chemotherapy-induced Nausea and Vomiting, Prophylaxis 1 4 Completed Prevention Anesthesia therapy / Palonosetron / Post Operative Nausea and Vomiting (PONV) 1 4 Completed Prevention Nausea / Neoplasm / Vomiting 2 4 Completed Prevention Post Operative Nausea and Vomiting (PONV) 6 4 Completed Supportive Care Cancer / Tumor 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
Form Route Strength Capsule Oral Injection Intravenous Injection, powder, for solution Intravenous Injection, solution, concentrate Intravenous Capsule, gelatin coated Oral Capsule Oral 0.5 mg Capsule Oral 0.5 mg/0.5mg Capsule Oral 500 μg Capsule, gelatin coated Oral 0.5 mg/1 Injection Intravenous 0.05 mg/1mL Injection Intravenous 0.075 mg/1.5mL Injection Intravenous 0.25 mg/5mL Injection, solution Intravenous 250 μg Injection, solution Intravenous; Parenteral 250 MCG Solution Intravenous 0.25 mg / 5 mL Capsule Oral 500 mcg Solution Intravenous 50 µg/ml Capsule, liquid filled Oral 0.50 mg Injection, solution Intravenous 50 mcg/ml Injection, solution Intravenous Solution Intravenous 0.250 mg Solution Parenteral 0.280 mg Injection, solution Intravenous 250 mcg/5ml Solution Intravenous 0.25 mg Solution Intravenous 0.0561 mg Solution Intravenous 250 mcg Injection, solution 250 mcg/5ml Solution Intravenous 0.28 mg Injection, solution Intravenous 250 micrograms/5ml Injection, solution Intravenous; Parenteral 250 MICROGRAMMI Injection, solution 250 MICROGRAMMI Injection, solution Intravenous 250 MCG Injection, solution Parenteral Injection Intravenous .25 mg/2mL Injection, solution Intravenous 0.05 mg/1mL Injection, solution Intravenous 0.075 mg/1.5mL Injection, solution Intravenous 0.25 mg/5mL Injection, solution Parenteral 250 Mikrogramm Injection, solution Parenteral 250 MICROGRAMMI Injection, solution 0.05 mg/1ml Solution Intravenous 0.05 mg/ml Injection Intravenous Solution Parenteral Solution Intravenous 0.280 mg - Prices
Unit description Cost Unit Aloxi 0.075 mg/1.5 ml vial 52.8USD 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 US9125905 Yes 2015-09-08 2024-07-30 US US8518981 Yes 2013-08-27 2024-07-30 US US7947725 Yes 2011-05-24 2024-07-30 US US8598218 Yes 2013-12-03 2024-07-30 US US7960424 Yes 2011-06-14 2024-07-30 US US9173942 Yes 2015-11-03 2024-07-30 US US7947724 Yes 2011-05-24 2024-07-30 US US8598219 Yes 2013-12-03 2024-07-30 US US8729094 Yes 2014-05-20 2024-07-30 US US9066980 Yes 2015-06-30 2024-07-30 US US9186357 No 2015-11-17 2030-11-18 US US8623826 No 2014-01-07 2030-11-18 US US8951969 No 2015-02-10 2030-11-18 US US6297375 No 2001-10-02 2020-02-22 US US5202333 Yes 1993-04-13 2015-10-13 US US9457020 Yes 2016-10-04 2024-07-30 US US9439854 Yes 2016-09-13 2024-07-30 US US9457021 Yes 2016-10-04 2024-07-30 US US9271975 No 2016-03-01 2031-09-09 US US9943515 No 2018-04-17 2030-11-18 US US9403772 No 2016-08-02 2032-05-23 US US8895586 No 2014-11-25 2032-05-23 US US9908907 No 2018-03-06 2032-05-23 US US9951016 No 2018-04-24 2035-09-25 US US8426450 No 2013-04-23 2032-05-23 US US10208073 No 2019-02-19 2032-05-23 US US10233154 No 2019-03-19 2035-09-25 US US10624911 No 2020-04-21 2037-06-02 US US10676440 No 2020-06-09 2035-09-25 US US10717721 No 2020-07-21 2032-05-23 US US10828297 No 2020-11-10 2030-12-17 US US10961195 No 2021-03-30 2035-09-25 US US11312698 No 2012-05-23 2032-05-23 US US11529362 No 2017-06-02 2037-06-02 US US11559523 No 2010-11-18 2030-11-18 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 2.7 Not Available - Predicted Properties
Property Value Source Water Solubility 0.464 mg/mL ALOGPS logP 2.72 ALOGPS logP 2.55 Chemaxon logS -2.8 ALOGPS pKa (Strongest Basic) 7.97 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 23.55 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 88.52 m3·mol-1 Chemaxon Polarizability 33.9 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9899 Blood Brain Barrier + 0.9953 Caco-2 permeable + 0.5986 P-glycoprotein substrate Substrate 0.679 P-glycoprotein inhibitor I Inhibitor 0.8643 P-glycoprotein inhibitor II Non-inhibitor 0.6745 Renal organic cation transporter Inhibitor 0.5763 CYP450 2C9 substrate Non-substrate 0.83 CYP450 2D6 substrate Substrate 0.7618 CYP450 3A4 substrate Substrate 0.6446 CYP450 1A2 substrate Inhibitor 0.6626 CYP450 2C9 inhibitor Non-inhibitor 0.541 CYP450 2D6 inhibitor Non-inhibitor 0.7502 CYP450 2C19 inhibitor Inhibitor 0.9367 CYP450 3A4 inhibitor Inhibitor 0.6002 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7828 Ames test Non AMES toxic 0.8664 Carcinogenicity Non-carcinogens 0.9557 Biodegradation Not ready biodegradable 0.9762 Rat acute toxicity 2.7383 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.883 hERG inhibition (predictor II) Inhibitor 0.6891
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 179.1814763 predictedDarkChem Lite v0.1.0 [M-H]- 174.91325 predictedDeepCCS 1.0 (2019) [M+H]+ 179.9106763 predictedDarkChem Lite v0.1.0 [M+H]+ 177.27124 predictedDeepCCS 1.0 (2019) [M+Na]+ 179.4181763 predictedDarkChem Lite v0.1.0 [M+Na]+ 184.20525 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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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
- Hesketh PJ: New treatment options for chemotherapy-induced nausea and vomiting. Support Care Cancer. 2004 Aug;12(8):550-4. Epub 2004 Jun 30. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Navari RM: Palonosetron: a second-generation 5-hydroxytryptamine receptor antagonist. Future Oncol. 2006 Oct;2(5):591-602. [Article]
- 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. [Article]
- Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4. [Article]
- 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. [Article]
- 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. [Article]
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
- 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. [Article]
- 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. [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]
- 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
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
- Palonosetron FDA label [File]
Drug created at June 13, 2005 13:24 / Updated at December 02, 2023 07:00