Palonosetron

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Palonosetron
Systematic (IUPAC) name
(3aR)-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	119904-90-4
ATC code	A04AA05
PubChem	148211
DrugBank	APRD00351
Chemical data
Formula	C19H24N2O
Mol. mass	296.407 g/mol
Pharmacokinetic data
Bioavailability	Low (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)
Therapeutic considerations
Pregnancy cat.	B1(AU) B(US)
Legal status	℞-only(US)
Routes	Intravenous

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. As of 2007, it is the most recent 5-HT₃ antagonist to enter clinical use.

Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy. An oral formulation is in Phase III clinical trials.