Netupitant and palonosetron (Akynzeo)

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General information

Class/mechanism: Neurokinin 1 (NK1) antagonist and serotonin 5-HT3 antagonist combination pill. Netupitant is selective human substance P/neurokinin 1 (NK1) receptor antagonist. Netupitant blocks substance P activation of tachykinin family neurokinin 1 (NK1) receptors, which reduces the incidence of delayed emesis. Chemotherapy medications can cause nausea and vomiting by stimulating release of serotonin from the enterochromaffin cells of the small intestine, and serotonin triggers the vomiting reflex by binding to and activating 5-HT3 receptors. Palonosetron (Aloxi) prevents nausea and vomiting by binding with high affinity to 5-HT3 receptors and blocking their activation by serotonin.[1][2][3]
Route: PO
Extravasation: n/a

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Patient drug information

History of changes in FDA indication

  • 2014-10-10: FDA approved 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.

History of changes in EMA indication

  • 2015-05-27: Initial authorization

Also known as

  • Generic name: NEPA
  • Brand name: Akynzeo