Palonosetron

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
Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a610002
Licence data	US FDA:link
Pregnancy category	AU: B1 US: B (No risk in non-human studies)
Legal status	US: ℞-only
Routes of administration	Intravenous, oral
Pharmacokinetic data
Bioavailability	97% (oral)
Protein binding	62%
Metabolism	Hepatic, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved)
Biological half-life	Approximately 40 hours
Excretion	Renal, 80% (of which 49% unchanged); fecal (5 to 8%)
Identifiers
CAS Number	135729-61-2 N
ATC code	A04AA05 (WHO)
PubChem	CID: 148211
IUPHAR/BPS	7486
DrugBank	DB00377 Y
ChemSpider	4892289 Y
UNII	5D06587D6R Y
ChEBI	CHEBI:85161 Y
ChEMBL	CHEMBL1189679 N
Chemical data
Formula	C19H24N2O
Molecular mass	296.407 g/mol
SMILES O=C5N([C@H]2C1CCN(CC1)C2)C[C@@H]4c3c5cccc3CCC4
InChI InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1 Y Key:CPZBLNMUGSZIPR-NVXWUHKLSA-N Y
NY (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 used for the control of delayed CINV—nausea and vomiting and there are tentative data to suggest that it may be better than granisetron.

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

See also

• 5-HT₃ receptor antagonist: Drug discovery and development