Palonosetron

Palonosetron
Clinical data
Pronunciation/pæləˈnoʊsətrɒn/ pal-ə-NOH-sə-tron
Trade namesAloxi
AHFS/Drugs.comMonograph
MedlinePlusa610002
License data
Pregnancy
category
Routes of
administration		Intravenous, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability97% (oral)
Protein binding62%
MetabolismLiver, 50% (mostly CYP2D6-mediated, CYP3A4 and CYP1A2 also involved)
Elimination half-lifeApproximately 40–50 hours
ExcretionKidney, 80% (of which 49% unchanged); fecal (5 to 8%)
Identifiers
  • (3aS)-2-[(3S)-1-Azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC19H24N2O
Molar mass296.414 g·mol−1
3D model (JSmol)
Specific rotation[α]D −136°
[α]D –94.1° (HCl)
Melting point87 to 88 °C (189 to 190 °F)
  • O=C5N([C@H]2C1CCN(CC1)C2)C[C@@H]4c3c5cccc3CCC4
  • 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 checkY
  • Key:CPZBLNMUGSZIPR-NVXWUHKLSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Palonosetron, sold under the brand name Aloxi, is a medication used for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).[2][4][5] It is a 5-HT3 antagonist.[2][4][5]

Palonosetron is administered intravenously,[6] or as a single oral capsule.[7] It has a longer duration of action than other 5-HT3 antagonists. 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.[7] It is on the World Health Organization's List of Essential Medicines.[8]

The oral combination netupitant/palonosetron is approved for both acute and delayed CINV.[9][10][11][12]

  1. ^ a b https://www.tga.gov.au/resources/auspar/auspar-palonosetron-hydrochloride [bare URL]
  2. ^ a b c "Aloxi 250 micrograms solution for injection - Summary of Product Characteristics (SmPC)". (emc). 18 May 2018. Archived from the original on 24 January 2022. Retrieved 23 January 2022.
  3. ^ "Aloxi 500 micrograms soft capsules - Summary of Product Characteristics (SmPC)". (emc). 18 May 2018. Archived from the original on 24 January 2022. Retrieved 24 January 2022.
  4. ^ a b c "Aloxi- palonosetron hydrochloride injection". DailyMed. Archived from the original on 24 January 2022. Retrieved 23 January 2022.
  5. ^ a b c "Aloxi EPAR". European Medicines Agency. 13 March 2009. Archived from the original on 14 April 2021. Retrieved 23 January 2022.
  6. ^ De Leon A (October 2006). "Palonosetron (Aloxi): a second-generation 5-HT₃ receptor antagonist for chemotherapy-induced nausea and vomiting". Proceedings. 19 (4): 413–6. doi:10.1080/08998280.2006.11928210. PMC 1618755. PMID 17106506.
  7. ^ a b Waknine Y (September 4, 2008). "FDA Approvals: Nplate, Aloxi, Vidaza". Medscape. Archived from the original on 2008-12-02. Retrieved 2008-09-04. Freely available with registration.
  8. ^ World Health Organization (2021). World Health Organization model list of essential medicines: 22nd list (2021). Geneva: World Health Organization. hdl:10665/345533. WHO/MHP/HPS/EML/2021.02.
  9. ^ "Akynzeo EPAR". European Medicines Agency. 23 June 2015. Archived from the original on 19 March 2020. Retrieved 23 January 2022.
  10. ^ Cite error: The named reference EPAR was invoked but never defined (see the help page).
  11. ^ "Akynzeo 300 mg/0.5 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). 11 February 2020. Archived from the original on 24 January 2022. Retrieved 23 January 2022.
  12. ^ "Akynzeo- netupitant and palonosetron capsule Akynzeo- fosnetupitant and palonosetron injection". DailyMed. Archived from the original on 18 October 2020. Retrieved 24 January 2022.