Fosaprepitant

Fosaprepitant is a prodrug of aprepitant and accordingly, its antiemetic effects are attributable to aprepitant. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1(NK 1 ) receptors.

• Fosaprepitant for injection, in combination with other antiemetic agents, is indicated in adults and pediatric patients 6 months of age and older for the prevention of: • acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin. • delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC).ICD-10: R11.2

• Fosaprepitant is contraindicated in patients: who are hypersensitive to any component of the product. Hypersensitivity reactions including anaphylactic reactions, flushing, erythema, and dyspnea have been reported [ see Warnings and Precautions (5.2), Adverse Reactions (6.2) ].contraindicated

Recommended Adult Dosage (2.1) Fosaprepitant for injection 150 mg on Day 1 as an intravenous infusion over 20 to 30 minutes. ( 2.1 ) Complete the infusion approximately 30 minutes prior to chemotherapy. Recommended Dosage for Pediatric Patients (6 months to 17 years) Weighing at Least 6 kg ( 2.2 ) See Full Prescribing Information for pediatric dosage regimens by age. For single dose chemotherapy regimens: single dose of fosaprepitant for injection on Day 1. For single or multi-day chemotherapy regimens: 3-day fosaprepitant for injection regimen of fosaprepitant for injection on Days 1, 2, and 3. Aprepitant capsules or fosaprepitant for oral suspension may be used as an alternative on Days 2 and 3. Administer fosaprepitant for injection through a central venous catheter as an intravenous infusion over 30 minutes (12 years to 17 years) or 60 minutes (6 months to less than 12 years). Complete the infusion approximately 30 minutes prior to chemotherapy. Concomitant Antiemetics See Full Prescribing Information for additional information. ( 2.1 , 2.2 ) 2.1 Prevention of Nausea and Vomiting Associated with HEC and MEC in Adult Patients The recommended dosage of fosaprepitant for injection, dexamethasone, and a 5-HT 3 antagonist for the prevention of nausea and vomiting associated with administration of HEC or MEC in adults is shown in Table 1 or Table 2, respectively. Administer fosaprepitant for injection as an intravenous infusion on Day 1 over 20 to 30 minutes, completing the infusion approximately 30 minutes prior to chemotherapy.

CYP3A4 Interactions: Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4; see Full Prescribing Information for recommendations regarding contraindications, risk of adverse reactions, and dosage adjustment of fosaprepitant and concomitant drugs. ( 4 , 5.1 , 7.1 , 7.2 ) Hypersensitivity Reactions (including anaphylaxis and anaphylactic shock) : May occur during or soon after infusion. If symptoms occur, discontinue the drug. Do not reinitiate fosaprepitant if symptoms occur with previous use. ( 4 , 5.2 ) Infusion Site Reactions (including thrombophlebitis, necrosis, and vasculitis): Majority of reactions reported in patients receiving vesicant chemotherapy. Avoid infusion into small veins. Discontinue infusion and administer treatment if a severe reaction develops. (5.3) Warfarin (a CYP2C9 substrate): Risk of decreased INR of prothrombin time; monitor INR in 2–week period, particularly at 7 to 10 days, following initiation of fosaprepitant. ( 5.4, 7.1 ) Hormonal Contraceptives: Efficacy of contraceptives may be reduced during and for 28 days following administration of fosaprepitant. Use effective alternative or back-up methods of contraception. ( 5.5 , 7.1 , 8.3 ) 5.1 Clinically Significant CYP3A4 Drug Interactions Fosaprepitant, a prodrug of aprepitant, is a weak inhibitor of CYP3A4, and aprepitant is a substrate, inhibitor, and inducer of CYP3A4. Use of fosaprepitant with other drugs that are CYP3A4 substrates, may result in increased plasma concentration of the concomitant drug.

The following clinically significant adverse reactions are described elsewhere in the labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.2)] Infusion Site Reactions [see Warnings and Precautions (5.3)] Most common adverse reactions in adults (≥2%) are: fatigue, diarrhea, neutropenia, asthenia, anemia, peripheral neuropathy, leukopenia, dyspepsia, urinary tract infection, pain in extremity. (6.1) Adverse reactions in pediatrics are similar to adults. To report SUSPECTED ADVERSE REACTIONS, contact Novadoz Pharmaceuticals Inc. at 1-855-668-2369 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. The overall safety of fosaprepitant for injection was evaluated in approximately 1800 adult and pediatric patients. Adverse Reactions in Adults for the Prevention of Nausea and Vomiting Associated with MEC In an active-controlled clinical trial in patients receiving MEC, safety was evaluated in 504 patients receiving a single dose of fosaprepitant for injection in combination with ondansetron and dexamethasone (fosaprepitant dimeglumine regimen) compared to 497 patients receiving ondansetron and dexamethasone alone (standard therapy). The most common adverse reactions are listed in Table 6.

8.1 Pregnancy Risk Summary There are insufficient data on use of fosaprepitant in pregnant women to inform a drug associated risk. In animal reproduction studies, no adverse developmental effects were observed in rats or rabbits exposed during the period of organogenesis to systemic drug levels (AUC) approximately equivalent to the exposure at the recommended human dose (RHD) of 150 mg [see Data] . The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Data Animal Data In embryofetal development studies in rats and rabbits, aprepitant was administered during the period of organogenesis at oral doses up to 1,000 mg/kg twice daily (rats) and up to the maximum tolerated dose of 25 mg/kg/day (rabbits). No embryofetal lethality or malformations were observed at any dose level in either species. The exposures (AUC) in pregnant rats at 1,000 mg/kg twice daily and in pregnant rabbits at 25 mg/kg/day were approximately equivalent to the exposure at the RHD of 150 mg. Aprepitant crosses the placenta in rats and rabbits.

Metabolism

Aprepitant after Fosaprepitant Administration Following administration of a single intravenous 150-mg dose of fosaprepitant, a prodrug of aprepitant administered as a 20-minute infusion to healthy subjects, the mean AUC 0-∞ of aprepitant was 37.4 (±14.8) mcg•hr/mL and the mean maximal aprepitant concentration (C max ) was 4.2 (±1.2) mcg/mL. Plasma concentrations of fosaprepitant are below the limits of quantification (10 ng/mL) within 30 minutes of the completion of infusion.

There is no specific information on the treatment of overdosage with fosaprepitant or aprepitant. In the event of overdose, fosaprepitant should be discontinued and general supportive treatment and monitoring should be provided. Because of the antiemetic activity of fosaprepitant, drug-induced emesis may not be effective in cases of fosaprepitant overdosage. Aprepitant is not removed by hemodialysis.

• Jan 25, 2008NDANDA022023Merck And Co Inc
• Jun 9, 2016ANDAANDA206197Fresenius Kabi Usa
• Sep 5, 2019NDANDA210064Teva Pharms Usa
• Sep 5, 2019ANDAANDA205020Apotex
• Sep 5, 2019ANDAANDA212309Be Pharms
• Sep 5, 2019ANDAANDA209965Msn
• Sep 5, 2019ANDAANDA204015Mylan Labs Ltd
• Aug 22, 2023NDANDA216686Steriscience

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

• Fosaprepitant Dimeglumine, Injection, 150 mg/5 mL (NDC 63323-972-10)To be discontinued
  Sponsor: Fresenius Kabi USA, LLC
  Updated Apr 8, 2026

1. 1Nausea1,45711%
2. 2Dyspnoea1,2399.2%
3. 3Pyrexia1,1038.2%
4. 4Diarrhoea1,0968.1%
5. 5Vomiting1,0647.9%
6. 6Fatigue1,0557.8%
7. 7Off Label Use8776.5%
8. 8Alopecia8626.4%
9. 9Rash8406.2%
10. 10Hypersensitivity8156.0%
11. 11Febrile Neutropenia8056.0%
12. 12Pruritus7215.3%
13. 13Infusion Related Reaction7155.3%
14. 14Stomatitis6574.9%
15. 15Pain6344.7%

The 10 most recently updated of 166 ClinicalTrials.gov registrations naming Fosaprepitant as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Study With IV NEPA (Fosnetupitant/Palonosetron) for the Prevention of Chemotherapy-induced Nausea and Vomiting in Paediatric Cancer Patients Undergoing Highly Emetogenic Chemotherapy (HEC)
  Recruiting · Phase 2 · Interventional · 95 enrolled · Helsinn Healthcare SA
  NCT06904235updated 2026-06-01
• Antiemetic Fosaprepitant To Remedy Nausea and Vomiting
  Recruiting · Phase 2 · Phase 3 · Interventional · 200 enrolled · Montefiore Medical Center
  NCT06382012updated 2026-05-18
• An Exploratory Study on Efficacy and Safety of Fosaprepitant and Palonosetron Hydrochloride for Injection in Preventing CINV From Multi-Agent HEC
  Recruiting · Phase 4 · Interventional · 200 enrolled · Shanghai 6th People's Hospital
  NCT07482891updated 2026-04-30
• A Prospective, Multicenter, Study of APF530 (Granisetron) SC for Prevention of CINV in Patients Receiving HEC
  Completed · Phase 3 · Interventional · 942 enrolled · Heron Therapeutics
  NCT02106494updated 2026-03-02
• Prevention of Delayed CINV After Autologous Transplant: Olanzapine-Containing Regimen vs. Dexamethasone-Containing Regimen
  Recruiting · Phase 3 · Interventional · 92 enrolled · The Affiliated People's Hospital of Ningbo University
  NCT07413809updated 2026-02-17
• Electroacupuncture for Chemotherapy-Induced GI Symptom Clusters in Breast Cancer
  Recruiting · Phase 3 · Interventional · 388 enrolled · Jiuda Zhao
  NCT06952920updated 2025-12-15
• To Evaluate the Efficacy and Safety of QLM2010 for Prevention of Chemotherapy-induced Nausea and Vomiting After Highly Emetogenic Chemotherapy.
  Completed · Phase 3 · Interventional · 665 enrolled · Qilu Pharmaceutical Co., Ltd.
  NCT07081256updated 2025-11-18
• Broadening Antiemetics Research by Comparing the Effectiveness of Fosaprepitant and Metoclopramide
  Not yet recruiting · Phase 4 · Interventional · 212 enrolled · Montefiore Medical Center
  NCT06740812updated 2025-09-08
• Nanocrystalline Megestrol for Managing Chemotherapy-Induced Nausea and Vomiting
  Not yet recruiting · Phase 3 · Interventional · 126 enrolled · The First Affiliated Hospital of Xinxiang Medical College
  NCT07124195updated 2025-08-15
• Olanzapine for the Prevention of Chemotherapy Induced Nausea and Vomiting in Gynecologic Oncology Patients
  Terminated · Phase 3 · Interventional · 62 enrolled · University of Michigan Rogel Cancer Center
  NCT04503668updated 2025-06-18

Frequently asked questions

How does Fosaprepitant work?

Fosaprepitant is a prodrug of aprepitant and accordingly, its antiemetic effects are attributable to aprepitant. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1(NK 1 ) receptors.

What is Fosaprepitant used for?

According to FDA labeling, Fosaprepitant carries indications including: Fosaprepitant for injection, in combination with other antiemetic agents, is indicated in adults and pediatric patients 6 months of age and older for the prevention of: • acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin. • delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Fosaprepitant?

Fosaprepitant is classified as Cytochrome P450 3A4 Inhibitors, Neurokinin 1 Antagonists, Emesis Suppression.

What are the brand names for Fosaprepitant?

Fosaprepitant is marketed under brand names including Emend Injection, Focinvez.

What are the contraindications for Fosaprepitant?

Fosaprepitant labeling lists contraindications including: Fosaprepitant is contraindicated in patients: who are hypersensitive to any component of the product. Hypersensitivity reactions including anaphylactic reactions, flushing, erythema, and dyspnea have been reported [ see Warnings and Precautions (5.2), Adverse Reactions (6.2) ].. Always consult the full prescribing information and a clinician.