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5-HT3 + NK1 antagonist combo

Palonosetron with netupitant

Brand names: Akynzeo

This is a fixed-dose oral combination of the 5-HT3 receptor antagonist palonosetron with the NK1 receptor antagonist netupitant, used to prevent acute and delayed chemotherapy-induced nausea and vomiting.

Dosing — being independently re-sourced

ClinCalc Pro is rebuilding its dose data from primary open sources — the manufacturer SmPC (eMC), the WHO Model Formulary and other official references — under clinician review. This drug's structured dose is not yet published here. Confirm all doses against the product SmPC and your local formulary before prescribing.

Clinical monograph

How it works

Palonosetron blocks serotonin 5-HT3 receptors that mediate the acute emetic response, while netupitant blocks substance P at central neurokinin-1 receptors involved in delayed emesis, giving complementary antiemetic cover.

Prescribing in practice

  • Netupitant is a CYP3A4 inhibitor, so doses of CYP3A4-substrate co-medications such as dexamethasone and certain chemotherapy agents must be adjusted and interacting drugs reviewed.
  • Both components can prolong the QT interval, so use with caution alongside other QT-prolonging drugs and in patients with electrolyte disturbance.
  • It is given as a single oral dose before the chemotherapy cycle rather than as ongoing daily therapy and is usually combined with a corticosteroid.

Monitoring

Monitor the adequacy of emetic control across the cycle and consider ECG and electrolytes where additional QT-prolonging risk factors are present.

Counselling the patient

  • Take the single dose about an hour before chemotherapy starts.
  • Constipation, headache and tiredness are common; report severe constipation.
  • Tell the team about all other medicines, as this drug can change how some are handled.

Evidence & guidelines

The combination's efficacy in preventing chemotherapy-induced nausea and vomiting is supported by registration trials and reflected in antiemetic guidelines.

Reference: NICE TA313; ESMO; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.