Palonosetron

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Palonosetron
Systematic (IUPAC) name
(3aS)-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 135729-61-2
ATC code A04AA05
PubChem 148211
DrugBank DB00377
Chemical data
Formula C19H24N2O 
Mol. mass 296.407 g/mol
SMILES eMolecules & PubChem
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

Pregnancy cat.

B1(AU) B(US)

Legal status

-only(US)

Routes Intravenous, oral

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Overview

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 used for the control of delayed CINV—nausea and vomiting and there are tentative data to suggest that it may be better than granisetron.[1]

Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy,[2] or as a single oral capsule one hour before chemotherapy.[3] 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.[3]

See also

References

  1. Billio, A; Morello, E; Clarke, MJ (Jan 20, 2010). "Serotonin receptor antagonists for highly emetogenic chemotherapy in adults.". The Cochrane database of systematic reviews (1): CD006272. PMID 20091591. doi:10.1002/14651858.CD006272.pub2. 
  2. 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 1618755Freely accessible. PMID 17106506. 
  3. 3.0 3.1 Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. Retrieved 2008-09-04.  Freely available with registration.

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