Netupitant

Netupitant
Clinical data
License data
Drug classNK1 receptor antagonists, antiemetics
ATC code
  • None
Pharmacokinetic data
Bioavailability>60% (estimated)
Protein binding>99%
Metabolismmainly CYP3A4; also CYP2D6 and CYP2C9
Elimination half-life88 hours
Excretion71% (faeces)
Identifiers
  • 2-[3,5-Bis(trifluoromethyl)phenyl]-N,2-dimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]propanamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC30H32F6N4O
Molar mass578.603 g·mol−1
3D model (JSmol)
  • Cc1ccccc1c2cc(ncc2N(C)C(=O)C(C)(C)c3cc(cc(c3)C(F)(F)F)C(F)(F)F)N4CCN(CC4)C
  • InChI=1S/C30H32F6N4O/c1-19-8-6-7-9-23(19)24-17-26(40-12-10-38(4)11-13-40)37-18-25(24)39(5)27(41)28(2,3)20-14-21(29(31,32)33)16-22(15-20)30(34,35)36/h6-9,14-18H,10-13H2,1-5H3
  • Key:WAXQNWCZJDTGBU-UHFFFAOYSA-N

Netupitant is an antiemetic medication. In the United States, the combinations of netupitant/palonosetron and the prodrug fosnetupitant/palonosetron (both brand name Akynzeo) are approved by the Food and Drug Administration for the prevention of acute and delayed chemotherapy-induced nausea and vomiting, including highly emetogenic chemotherapy such as with cisplatin.[1][2] In the European Union, the combinations are approved by the European Medicines Agency (EMA) for the same indication.[3][4]

  1. ^ "Akynzeo- netupitant and palonosetron capsule Akynzeo- fosnetupitant and palonosetron injection". DailyMed. U.S. National Library of Medicine. 30 April 2018. Archived from the original on 18 October 2020. Retrieved 19 March 2020.
  2. ^ "FDA approves Akynzeo for nausea and vomiting associated with cancer chemotherapy" (Press release). Food and Drug Administration. October 10, 2014. Archived from the original on February 1, 2017. Retrieved December 16, 2019.
  3. ^ "Akynzeo: Summary of Product Characteristics" (PDF). European Medicines Agency. Archived (PDF) from the original on 26 June 2016. Retrieved 12 July 2016.
  4. ^ "Akynzeo EPAR". European Medicines Agency (EMA). 19 March 2020. Archived from the original on 19 March 2020. Retrieved 19 March 2020.