Palonosetron
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| Systematic (IUPAC) name | |
| (3aR)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a, 4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one |
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| Clinical data | |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a610002 |
| Licence data | US FDA:link |
| Pregnancy cat. | B1 (AU) B (US) |
| Legal status | ℞-only (US) |
| Routes | Intravenous, oral |
| Pharmacokinetic data | |
| Bioavailability | 97% (oral) |
| Protein binding | 62% |
| Metabolism | Hepatic, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved) |
| Half-life | Approximately 40 hours |
| Excretion | Renal, 80% (of which 49% unchanged); fecal (5 to 8%) |
| Identifiers | |
| CAS number | 135729-61-2  |
| ATC code | A04AA05 |
| PubChem | CID 6337614 |
| DrugBank | APRD00351 |
| ChemSpider | 4892289  |
| UNII | 5D06587D6R |
| ChEMBL | CHEMBL1189679 |
| Chemical data | |
| Formula | C19H24N2O |
| Mol. mass | 296.407 g/mol |
| SMILES | eMolecules & PubChem |
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Palonosetron (INN, trade name Aloxi) is a 5-HT3 antagonist used in 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.[1] As of 2008[update], it is the most recent 5-HT3 antagonist to enter clinical use.
Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy,[1] or as a single oral capsule one hour before chemotherapy.[2] The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.[2]
[edit] See also
[edit] References
- ^ a b De Leon A (2006). "Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting". Proceedings (Baylor University. Medical Center) 19 (4): 413–6. PMC 1618755. PMID 17106506. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1618755. Full text at PMC: 1618755.
- ^ a b Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. http://www.medscape.com/viewarticle/580032. Retrieved 2008-09-04. Freely available with registration.
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