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NK1 receptor antagonist

Aprepitant

Emendfosaprepitant

How it works

Blocks substance P at NK1 receptors in the chemoreceptor trigger zone. Adds to the 5-HT3 antagonist + dexamethasone backbone for highly emetogenic chemotherapy (HEC).

Strong CYP3A4 inhibitor on D1 (moderate D2–D3). Dose-adjust concurrent dexamethasone per guideline (usually 50% reduction when combined). Especially relevant for mFFX regimens.

Dosing

Typical doses

  • 125 mg PO 1 h before chemo, D1
  • 80 mg PO D2 + D3
  • Fosaprepitant 150 mg IV single dose D1 (alternative)

Schedule

  • D1–D3 of HEC cycle (mFFX); D1 only for MEC
    cycle_linked

Side Effects

  • Fatigue / asthenia
  • Constipation, diarrhoea
  • Headache, hiccups
  • CYP3A4 inhibition — interaction with dexamethasone, warfarin, midazolam, oral contraceptives
  • Rare hepatotoxicity — monitor LFTs

Monitoring

  • Review concurrent CYP3A4 substrates — may need dose adjustments