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Palonosetron
Systematic (IUPAC) name
(3aR)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3 a,
4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
Identifiers
CAS number 135729-61-2
ATC code A04AA05
PubChem 148211
DrugBank APRD00351
Chemical data
Formula C 19H24N2O 
Mol. mass 296.407 g/mol
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%)
Therapeutic considerations
Licence data

US FDA:link

Pregnancy cat. B1(AU) B(US)
Legal status -only (US)
Routes Intravenous, oral

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, 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]

See also

  • 5-HT3 receptor antagonist: Drug discovery and development

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. ^ 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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