Netupitant or fosnetupitant and palonosetron

(Akynzeo®)

Akynzeo®

Drug updated on 4/16/2024

Dosage FormFor Injection (intravenous; 235 mg fosnetupitant/0.25 mg palonosetron ); Injection (intravenous; 235 mg fosnetupitant/0.25 mg palonosetron); Capsule (oral; 300 mg netupitant/0.5 mg palonosetron)
Drug ClassSerotonin-3 (5-HT3) receptor antagonists and substance P/neurokinin-1 (NK-1) receptor antagonists
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Akynzeo capsule is indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, including, but not limited to, highly emetogenic chemotherapy.
  • Akynzeo for injection and Akynzeo injection are indicated in combination with dexamethasone in adults for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy.
  • Akynzeo is a combination of palonosetron, a serotonin-3 (5-HT3) receptor antagonist, and netupitant or fosnetupitant, substance P/neurokinin-1 (NK-1) receptor antagonists: palonosetron prevents nausea and vomiting during the acute phase and netupitant/fosnetupitant prevents nausea and vomiting during both the acute and delayed phase after cancer chemotherapy.

Summary
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  • Netupitant or fosnetupitant and palonosetron (Akynzeo) is indicated in combination with dexamethasone for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of cancer chemotherapy, including highly emetogenic chemotherapy.
  • Akynzeo works by combining the effects of palonosetron, a serotonin-3 (5-HT3) receptor antagonist, which prevents nausea during the acute phase; netupitant/fosnetupitant are substance P/neurokinin-1 (NK-1) receptor antagonists that prevent nausea during both the acute and delayed phases after cancer chemotherapy.
  • Clinical trials have shown high complete response rates in patients receiving highly or moderately emetogenic chemotherapy when treated with Akynzeo plus dexamethasone; its efficacy was maintained over multiple cycles making it superior to other treatments such as aprepitant plus granisetron.
  • The drug has been found to be well tolerated in both oral and intravenous formulations providing a simple option for prophylaxis against acute and delayed CINV in adult patients undergoing cancer treatment.
  • A total of 5 systematic reviews/meta-analyses were reviewed which provided evidence supporting use of Akynzeo as an effective antiemetic regimen compared to others like aprepitant-based regimens especially for those unsuited for oral administration due to safety considerations related to injection site toxicity or hypersensitivity reactions.
  • In terms cost-effectiveness from a United States perspective, one study suggested that using single dose NEPA could result not only higher quality-adjusted life-days but also significant per-patient cost reduction mainly due lower medical costs related CINV-related events along with lower study drug costs compared APR + GRAN regimen used commonly today.

Product Monograph / Prescribing Information

Document TitleYearSource
Akynzeo (netupitant/fosnetupitant and palonosetron) Prescribing Information2023Helsinn Therapeutics (U.S.), Inc., Iselin, NJ

Systematic Reviews / Meta-Analyses

Clinical Practice Guidelines