Netupitant/palonosetron

Netupitant/palonosetron, sold under the brand name Akynzeo, is a fixed-dose combination medication used for the prevention of acute and delayed chemotherapy-induced nausea and vomiting.^[7][9] It is marketed and distributed by Helsinn Therapeutics. Netupitant is an NK₁ receptor antagonist and palonosetron is a 5-HT₃ receptor antagonist.^[10]

Netupitant/palonosetron

Combination of
Netupitant	NK1 receptor antagonist
Palonosetron	5-HT3 receptor antagonist
Clinical data
Trade names	Akynzeo
AHFS/Drugs.com	Monograph
MedlinePlus	a614053
License data	US DailyMed: Netupitant
Pregnancy category	AU: B3[1]
Routes of administration	By mouth, intravenous
ATC code	A04AA55 (WHO)
Legal status
Legal status	AU: S4 (Prescription only)[2][3] CA: ℞-only[4][5] UK: POM (Prescription only)[6] US: ℞-only[7] EU: Rx-only[8] In general: ℞ (Prescription only)
Identifiers
CAS Number	2446322-17-2
KEGG	D10572 Y

The capsules contain netupitant and palonosetron hydrochloride. The intravenous version is a combination of fosnetupitant chloride hydrochloride and palonosetron hydrochloride.^[11][7][8]

Contraindications

Netupitant/palonosetron may be contraindicated during pregnancy.^[12][1][13]

Adverse effects

The most common side effects include headache, weakness, fatigue, upset stomach, constipation, and skin redness.^[7] The overall profile of adverse effects is comparable to that of palonosetron (see Palonosetron#Adverse effects); no common adverse effects can be attributed to netupitant.^[12]

Interactions

Further information: Netupitant § Interactions, and Palonosetron § Interactions

Pharmacology

Further information: Netupitant § Pharmacology, and Palonosetron § Pharmacology

History

Netupitant/palonosetron was approved for use in the United States in October 2014.^[14] It was approved for use in the European Union in May 2015.^[8] The intravenous version, which contains the prodrug fosnetupitant in place of netupitant, was approved in the United States in April 2018.^[15][11]

References

1. "Netupitant / palonosetron (Akynzeo) Use During Pregnancy". Drugs.com. 22 October 2018. Archived from the original on 19 December 2019. Retrieved 19 March 2020.
2. AusPAR: Netupitant / Palonosetron (as hydrochloride). Therapeutic Goods Administration (TGA) (Report). October 2020. Archived from the original on 9 September 2017. Retrieved 10 June 2022.
3. "Prescription medicines: registration of new chemical entities in Australia, 2015". Therapeutic Goods Administration (TGA). 21 June 2022. Archived from the original on 10 April 2023. Retrieved 10 April 2023.
4. "Archived copy" (PDF). Archived (PDF) from the original on 10 June 2022. Retrieved 10 June 2022.{{cite web}}: CS1 maint: archived copy as title (link)
5. "Cancer therapies". Health Canada. 8 May 2018. Archived from the original on 16 June 2024. Retrieved 13 April 2024.
6. "Akynzeo 300 mg/0.5 mg hard capsules - Summary of Product Characteristics (SmPC)". (emc). 11 February 2020. Archived from the original on 19 March 2020. Retrieved 19 March 2020.
7. "Akynzeo- netupitant and palonosetron capsule; Akynzeo- fosnetupitant and palonosetron injection". DailyMed. 28 May 2020. Archived from the original on 18 October 2020. Retrieved 18 July 2020.
8. "Akynzeo EPAR". European Medicines Agency (EMA). 19 March 2020. Archived from the original on 19 March 2020. Retrieved 19 March 2020.
9. "FDA approves Akynzeo for nausea and vomiting associated with cancer chemotherapy" (Press release). U.S. Food and Drug Administration (FDA). 10 October 2014. Archived from the original on 1 February 2017. Retrieved 16 December 2019.
10. "Akynzeo: Summary of Product Characteristics" (PDF). European Medicines Agency. Archived (PDF) from the original on 26 June 2016. Retrieved 12 July 2016.
11. "Drug Trials Snapshots: Akynzeo". U.S. Food and Drug Administration (FDA). 11 May 2018. Archived from the original on 24 January 2020. Retrieved 19 March 2020.
12. Haberfeld H, ed. (2015). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Akynzeo 300 mg / 0,5 mg Hartkapseln.
13. "Fosnetupitant / palonosetron (Akynzeo for Injection) Use During Pregnancy". Drugs.com. 22 October 2018. Archived from the original on 19 March 2020. Retrieved 19 March 2020.
14. "Drug Approval Package: Akynzeo (Netupitant and Palonosetron) Capsules NDA #205718". U.S. Food and Drug Administration (FDA). 7 November 2014. Archived from the original on 19 March 2020. Retrieved 19 March 2020.
15. "Drug Approval Package: Akynzeo (fosnetupitant and palonosetron) Injection". U.S. Food and Drug Administration (FDA). 31 May 2018. Archived from the original on 19 March 2020. Retrieved 19 March 2020.