Palonosetron

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Palonosetron
Clinical data
AHFS/Drugs.comMonograph
MedlinePlusa610002
[[Regulation of therapeutic goods |Template:Engvar data]]
Pregnancy
category
  • AU: B1
  • US: B (No risk in non-human studies)
Routes of
administration
Intravenous, oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability97% (oral)
Protein binding62%
MetabolismHepatic, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved)
Elimination half-lifeApproximately 40 hours
ExcretionRenal, 80% (of which 49% unchanged); fecal (5 to 8%)
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEBI
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC19H24N2O
Molar mass296.407 g/mol
3D model (JSmol)
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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. doi:10.1002/14651858.CD006272.pub2. PMID 20091591.
  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 1618755. 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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