The Full Wiki

More info on Palonosetron

Palonosetron: Wikis


Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.


From Wikipedia, the free encyclopedia

Systematic (IUPAC) name
(3aR)-2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3 a,
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


  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. Retrieved 2008-09-04.   Freely available with registration.


Got something to say? Make a comment.
Your name
Your email address