Therapeutic Classification: antiemetics
Pharmacologic Classification: neurokinin antagonists
Absorption: Following IV administration, fosaprepitant is rapidly converted to aprepitant, the active component. IV administration results in complete bioavailability.
Distribution: Crosses the blood brain barrier; remainder of distribution unknown.
Protein Binding: 9599%.
Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A4 isoenzyme; not renally excreted.
Half-Life: Aprepitant: 913 hr.
Prevention of Acute and Delayed Nausea and Vomiting Associated with Highly Emetogenic Chemotherapy
- IV (Adults ): Emend or Focinvez: 150 mg given 30 min prior to chemotherapy on Day 1 only.
- IV (Children 1217 yr and ≥6 kg): Single-day chemotherapy regimen (Emend or Focinvez): 150 mg given 30 min prior to chemotherapy on Day 1 only; Multiday chemotherapy regimen (Emend): 115 mg given 30 min prior to chemotherapy on Day 1, then 80 mg once daily (as IV fosaprepitant or aprepitant oral capsules) for 2 days (Days 2 and 3); Multiday chemotherapy regimen (Focinvez): 115 mg given 30 min prior to chemotherapy on Day 1, then 80 mg once daily (as aprepitant oral capsules) for 2 days (Days 2 and 3).
- IV (Children 2<12 yr and ≥6 kg): Single-day chemotherapy regimen (Emend or Focinvez): 4 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 only; Multiday chemotherapy regimen (Emend): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as IV fosaprepitant or aprepitant oral suspension) once daily for 2 days (Days 2 and 3); Multiday chemotherapy regimen (Focinvez): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as aprepitant oral suspension) once daily for 2 days (Days 2 and 3).
- IV (Children 6 mo-<2 yr and ≥6 kg): Single-day chemotherapy regimen (Emend or Focinvez): 5 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 only; Multiday chemotherapy regimen (Emend): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as IV fosaprepitant or aprepitant oral suspension) once daily for 2 days (Days 2 and 3); Multiday chemotherapy regimen (Focinvez): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as aprepitant oral suspension) once daily for 2 days (Days 2 and 3).
Prevention of Delayed Nausea and Vomiting Associated with Moderately Emetogenic Chemotherapy
- IV (Adults ): Emend or Focinvez: 150 mg given 30 min prior to chemotherapy on Day 1 only.
- IV (Children 1217 yr and ≥6 kg): Single-day chemotherapy regimen (Emend or Focinvez): 150 mg given 30 min prior to chemotherapy on Day 1 only; Multiday chemotherapy regimen (Emend): 115 mg given 30 min prior to chemotherapy on Day 1, then 80 mg (as IV fosaprepitant or aprepitant oral capsules) once daily for 2 days (Days 2 and 3); Multiday chemotherapy regimen (Focinvez): 115 mg given 30 min prior to chemotherapy on Day 1, then 80 mg (as aprepitant oral capsules) once daily for 2 days (Days 2 and 3).
- IV (Children 2<12 yr and ≥6 kg): Single-day chemotherapy regimen (Emend or Focinvez): 4 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 only; Multiday chemotherapy regimen (Emend): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as IV fosaprepitant or aprepitant oral suspension) once daily for 2 days (Days 2 and 3); Multiday chemotherapy regimen (Focinvez): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as aprepitant oral suspension) once daily for 2 days (Days 2 and 3).
- IV (Children 6 mo-<2 yr and ≥6 kg): Single-day chemotherapy regimen (Emend or Focinvez): 5 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 only; Multiday chemotherapy regimen (Emend): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as IV fosaprepitant or aprepitant oral suspension) once daily for 2 days (Days 2 and 3); Multiday chemotherapy regimen (Focinvez): 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1, then 2 mg/kg (max dose = 80 mg) (as aprepitant oral suspension) once daily for 2 days (Days 2 and 3).