Palonosetron
From Wikipedia, the free encyclopedia
 |
|
 |
|
|
Palonosetron
|
|
| 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 |
|
| Identifiers | |
| CAS number | |
| ATC code | A04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C19H24N2O |
| Mol. mass | 296.407 g/mol |
| Pharmacokinetic data | |
| Bioavailability | Low (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) |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Intravenous |
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 2007, 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] An oral formulation is currently under regulatory review, after the FDA accepted for review the supplemental New Drug Application (sNDA) for palonosetron capsules.[2][3]
[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. PMID 17106506. Full text at PMC: 1618755.
- ^ MGI Pharma press release - MGI PHARMA and HELSINN Announce sNDA for Aloxi Capsules Accepted for Review by U.S. FDA. MGI Pharma (2008). Retrieved on 2008-05-31.
- ^ Aloxi Oral Capsule. MGI Pharma (2007). Retrieved on 2007-05-16.
|
|||||||||||||||||||||||||||||
 |
This pharmacology-related article is a stub. You can help Wikipedia by expanding it. |
