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Palonosetron



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 119904-90-4
ATC code A04AA05
PubChem 148211
DrugBank APRD00351
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.

B1(AU) B(US)

Legal status

-only(US)

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.

Additional recommended knowledge

Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy.[1] An oral formulation is in Phase III clinical trials.[2]

References

  1. ^ 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.
  2. ^ Aloxi® Oral Capsule. MGI Pharma (2007). Retrieved on 2007-05-16.


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Palonosetron". A list of authors is available in Wikipedia.
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