Both AKYNZEO® formulations target 2 pathways of CINV

The correlation between these pharmacological data and clinical efficacy has not been established.

Netupitant is a selective antagonist of substance P/NK1 receptors. As shown in in vitro and in vivo studies, netupitant inhibits substance P-mediated response1

  • Netupitant has a mean plasma half-life of approximately 80 hours
  • Netupitant demonstrated 92.5% NK1 receptor occupancy at 6 hours, with 76% occupancy at 96 hours

Fosnetupitant is a soluble prodrug of netupitant that is used in AKYNZEO for injection2

  • Fosnetupitant is rapidly converted to netupitant after IV administration
  • An IV fosnetupitant dose of 235 mg achieved a similar netupitant area under the curve (AUC) as 300 mg oral netupitant

Palonosetron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor1

  • Oral palonosetron has a mean plasma half-life of approximately 48 hours

CINV
=chemotherapy-induced nausea and vomiting.