Akynzeo® (netupitant/palonosetron) has recently been approved by the Therapeutic Goods Administration (TGA) for the prevention of chemotherapy induced nausea and vomiting (CINV) in patients receiving moderately to highly emetogenic therapies. Despite advances in the medical management of CINV, nausea remains inadequately controlled in up to 84% of patients in the four days after treatment.

CINV can be difficult to manage as it involves multiple neurotransmitter pathways. Acute nausea is thought to primarily occur as a result of serotonin release from enterochromaffin cells in the small intestine. Delayed symptoms are largely attributed to neurokinin 1 (NK1) receptor activation in the central nervous system.

Akynzeo® is used to prevent acute and delayed nausea by targeting both of these critical pathways. Palonosetron, a serotonin subtype 3 (5-HT3) antagonist, effectively treats acute symptoms. It has a longer half-life than other available 5-HT3 antagonists (40 hours versus 4-8 hours), which provides an extended duration of effect. Netupitant, an NK1 antagonist, prevents both acute and delayed nausea with receptor occupancy studies showing significant blockade of NK1 receptors is maintained four days after administration of a single dose.

For maximum effectiveness, it is recommended to administer Akynzeo® with dexamethasone.

References:

  1. Akynzeo® (netupitant/palonosetron) Australian approved product information. Kew East: Specialised Therapeutics Australia Pty Ltd. Approved 6 May 2015.
  2. Frame DG. Best practice management of CINV in oncology patients: I. Physiology and treatment of CINV multiple neurotransmitters and receptors and the need for combination therapeutic approaches. J Support Oncol. 2010; 8(1): 5-9.
  3. Spinelli T, Calcagnile S, Giuliano C, Rossi G, Lanzarotti C, Mair S, et al. Netupitant PET imaging and ADME studies in humans. J Clin Pharmacol. 2014; 54(1): 97-108.

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