Systematic (IUPAC) name
Clinical data
AHFS/ monograph
MedlinePlus a610002
Licence data US FDA:link
Pregnancy cat. B1(AU) B(US)
Legal status -only (US)
Routes Intravenous, oral
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%)
CAS number 135729-61-2 YesY
ATC code A04AA05
PubChem CID 6337614
DrugBank APRD00351
ChemSpider 4892289 YesY
UNII 5D06587D6R N
Chemical data
Formula C19H24N2O 
Mol. mass 296.407 g/mol
SMILES eMolecules & PubChem
 N(what is this?)  (verify)

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


  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. PMC 1618755. PMID 17106506.  Full text at PMC: 1618755.
  2. ^ a b Waknine, Yael (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. Retrieved 2008-09-04.  Freely available with registration.