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 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

Pregnancy cat.

B1(AU) B(US)

Legal status

â„ž-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]

[edit] References

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