Fosaprepitant 150 mg/5mL Injection, Powder, Lyophilized, For Solution
🆔 Identity & classification
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🏭 Manufacturer & labeler
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🩺 Clinical
Aprepitant injection and fosaprepitant injection are used along with other medications to prevent nausea and vomiting in adults that may occur within 24 hours or several days after receiving certain cancer chemotherapy treatments. Fosaprepitant injection can also be used in children 6 months of age and older. Aprepitant and fosaprepitant injections are not used to treat nausea and vomiting that you already have. Aprepitant and fosaprepitant injections are in a class of medications called antiemetics. They work by blocking the action of neurokinin, a natural substance in the brain that causes n...
Read the full MedlinePlus article ↗- Fosaprepitant is an anti-nausea medicine given by IV infusion before chemotherapy starts. Chemo can trigger powerful nausea signals in your brain — both right away and in the days...
- What exactly is this medication, and why am I getting it before chemo?
- Most people tolerate the infusion well. The most commonly reported side effects include fatigue, diarrhea, and weakness — though it's worth noting that the chemotherapy itself also...
- Will I feel anything during the infusion? What side effects should I expect?
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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375 mg / 5 mL
UNII 3SY5LH9PMK
Anhydrous lactose is a milk sugar with no water content. It acts as a filler and binder in tablets and capsules, adding bulk and helping ingredients stick together.
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5.4 mg / 5 mL
UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
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UNII QTT17582CB
A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
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75 mg / 5 mL
UNII 6OZP39ZG8H
Polysorbate 80 is a synthetic emulsifier derived from sorbitol and oleic acid. It helps mix oil and water-based ingredients together in medications and improves how the product disperses in the body.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
5 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $29.70 | $148.48 / 5 ml |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
| Medicare Part B allowsASP · J1453 | $0.123 / J1453 unit | — |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Emend 150 mg/5mL 00006-3061-00 | Merck | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant Dimeglumine 150 mg/5mL 00143-9384-01 | Hikma | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant Dimeglumine 150 mg/5mL 00143-9428-01 | Hikma | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 00338-0008-01 | Baxter | 1 vial | — | — | FDA listed | — |
| Fosaprepitant 150 mg 00591-4385-79 | Actavis | 1 injection | — | — | FDA listed | — |
| Fosaprepitant 150 mg/5mL 16714-0248-01 | NorthStar | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mLthis 31722-0165-31 | Camber | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg 43598-0671-11 | Dr. | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 43598-0859-11 | Dr. | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 43598-0948-11 | Dr. | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant Dimeglumine 150 mg/5mL 55150-0299-01 | Eugia | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 63323-0972-10 | Fresenius | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant Dimeglumine 150 mg/5mL 67184-0540-01 | Qilu | 1 vial | — | AP | FDA listed | — |
| fosaprepitant 150 mg/5mL 67457-0889-10 | Mylan | 1 vial | — | — | FDA listed | — |
| Fosaprepitant 150 mg/5mL 68001-0523-36 | BluePoint | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 68001-0675-25 | BluePoint | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 71731-5111-01 | Chia | 1 vial | — | AP | FDA listed | — |
| fosaprepitant 150 mg/5mL 71839-0104-01 | BE | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 72162-2636-02 | Bryant | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 72205-0054-01 | Novadoz | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 72205-0083-01 | Novadoz | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 72603-0450-01 | Northstar | 1 vial | — | AP | FDA listed | — |
| Fosaprepitant 150 mg/5mL 83634-0776-10 | Avenacy, | 1 vial | — | AP | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 31722-0165-31 You're viewing this | 1 VIAL, SINGLE-DOSE in 1 CARTON (31722-165-31) / 5 mL in 1 VIAL, SINGLE-DOSE | 2021-07-29 | Active |
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE 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). Limitations of Use • Fosaprepitant for injection has not been studied for the treatment of established nausea and vomiting.
Fosaprepitant for injection is a substance P/neurokinin-1 (NK 1 ) receptor antagonist, indicated in adults and pediatric patients 6 months of age and older, in combination with other antiemetic agents, for the prevention of ( 1 ): • 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). Limitations of Use ( 1 ) • Fosaprepitant for injection has not been studied for treatment of established nausea and vomiting.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION 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 regimen of fosaprepitant for injection on Days 1, 2, and 3.
Fosaprepitant 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 )
2.1Prevention 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. Table 1 Recommended Adult Dosing for the Prevention of Nausea and Vomiting Associated with HEC Day 1 Day 2 Day 3 Day 4 Fosaprepitant for injection 150 mg intravenously over 20 to 30 minutes none none none Dexamethasone* 12 mg orally 8 mg orally 8 mg orally twice daily 8 mg orally twice daily 5-HT 3 antagonist See selected 5-HT 3 antagonist prescribing information for the recommended dosage none none none *Administer dexamethasone 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 through 4.
Also administer dexamethasone in the evenings on Days 3 and 4. A 50% dosage reduction of dexamethasone on Days 1 and 2 is recommended to account for a drug interaction with fosaprepitant for injection [see Clinical Pharmacology ( 12.3 )]. Table 2 Recommended Adult Dosing for the Prevention of Nausea and Vomiting Associated with MEC Day 1 Fosaprepitant for injection 150 mg intravenously over 20 to 30 minutes Dexamethasone* 12 mg orally 5-HT 3 antagonist See selected 5-HT 3 antagonist prescribing information for the recommended dosage *Administer dexamethasone 30 minutes prior to chemotherapy treatment on Day 1.
A 50% dosage reduction of dexamethasone is recommended to account for a drug interaction with fosaprepitant for injection [see Clinical Pharmacology ( 12.3 )].
2.2Prevention of Nausea and Vomiting Associated with HEC and MEC in Pediatric Patients The recommended pediatric dosage regimens of fosaprepitant for injection, to be administered with a 5-HT 3 antagonist, with or without a corticosteroid, for the prevention of nausea and vomiting associated with administration of single or multi-day chemotherapy regimens of HEC or MEC, are shown in Tables 3 and 4. Single-day chemotherapy regimens include regimens in which HEC or MEC is administered for a single day only. Multi-day chemotherapy regimens include chemotherapy regimens in which HEC or MEC is administered for 2 or more days.
Fosaprepitant for Injection Dosage Regimens for Use with Single-Day Chemotherapy Regimens For pediatric patients weighing at least 6 kg receiving single-day HEC or MEC, fosaprepitant for injection may be administered as: • a single dose regimen of fosaprepitant for injection infused through a central venous catheter on Day 1, as shown in Table 3; or • as a 3-day fosaprepitant regimen consisting of fosaprepitant for injection as an intravenous infusion through a central ven…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Fosaprepitant for injection: 150 mg fosaprepitant, white to off-white lyophilized cake or powder in single dose glass vial for reconstitution Fosaprepitant for injection: 150 mg fosaprepitant, lyophilized powder in single dose vial for reconstitution. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS Fosaprepitant for injection 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 )]. • taking pimozide. Inhibition of CYP3A4 by aprepitant, the active moiety, could result in elevated plasma concentrations of this drug, which is a CYP3A4 substrate, potentially causing serious or life-threatening reactions, such as QT prolongation, a known adverse reaction of pimozide [see Warnings and Precautions ( 5.1 )]. • Known hypersensitivity to any component of this drug.
( 4 , 5.2 ) • Concurrent use with pimozide. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • 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)
5.1Clinically 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. o Use of pimozide with fosaprepitant is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, potentially resulting in prolongation of the QT interval, a known adverse reaction of pimozide [see Contraindications ( 4 )]. • Use of fosaprepitant with strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, diltiazem) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to fosaprepitant. • Use of fosaprepitant with strong CYP3A4 inducers (e.g., rifampin) may result in a reduction in aprepitant plasma concentrations and decreased efficacy of fosaprepitant.
See Table 7 and Table 8 for a listing of potentially significant drug interactions [see Drug Interactions ( 7.1 , 7.2 )].
5.2Hypersensitivity Reactions Serious hypersensitivity reactions, including anaphylaxis and anaphylactic shock, during or soon after infusion of fosaprepitant have occurred. Symptoms including flushing, erythema, dyspnea, hypotension and syncope have been reported [see Adverse Reactions ( 6.2 )]. Monitor patients during and after infusion.
If hypersensitivity reactions occur, discontinue the infusion and administer appropriate medical therapy. Do not reinitiate fosaprepitant in patients who experience these symptoms with previous use [see Contraindications ( 4 )].
5.3Infusion Site Reactions Infusion site reactions (ISRs) have been reported with the use of fosaprepitant for injection [see Adverse Reactions ( 6.1 )]. The majority of severe ISRs, including thrombophlebitis and vasculitis, were reported with concomitant vesicant (anthracycline-based) chemotherapy administration, particularly when associated with extravasation. Necrosis was also reported in some patients with concomitant vesicant chemotherapy.
Most ISRs occurred with the first, second or third exposure to single doses of fosaprepitant for injection and in some cases, reactions persisted for two weeks or longer. Treatment of severe ISRs consisted of medical, and in some cases surgical, intervention. Avoid infusion of fosaprepitant for injection into small veins or through a butterfly catheter.
If a severe ISR develops during infusion, discontinue the infusion and administer appropriate medical treatment.
5.4Decrease in INR with Concomitant Warfarin Coadministration of fosaprepitant with warfarin, a CYP2C9 substr…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS 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 Aspiro Pharma Limited at 1-866-495-1995 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical 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 regimen) compared to 497 patients receiving ondansetron and dexamethasone alone (standard therapy).
The most common adverse reactions are listed in Table 6. Table 6 Most Common Adverse Reactions in Patients Receiving MEC* Fosaprepitant for injection, ondansetron, and dexamethasone † (N=504) Ondansetron and dexamethasone ‡ (N=497) fatigue 15% 13% diarrhea 13% 11% neutropenia 8% 7% asthenia 4% 3% anemia 3% 2% peripheral neuropathy 3% 2% leukopenia 2% 1% dyspepsia 2% 1% urinary tract infection 2% 1% pain in extremity 2% 1% * Reported in ≥2% of patients treated with the fosaprepitant regimen and at a greater incidence than standard therapy. † Fosaprepitant regimen ‡ Standard therapy Infusion-site reactions were reported in 2.2% of patients treated with the fosaprepitant regimen compared to 0.6% of patients treated with standard therapy.
The infusion-site reactions included: infusion-site pain (1.2%, 0.4%), injection-site irritation (0.2%, 0.0%), vessel puncture-site pain (0.2%, 0.0%), and infusion-site thrombophlebitis (0.6%, 0.0%), reported in the fosaprepitant regimen compared to standard therapy, respectively. Adverse Reactions in Adults for the Prevention of Nausea and Vomiting Associated with HEC In an active-controlled clinical study in patients receiving HEC, safety was evaluated for 1143 patients receiving a single dose of fosaprepitant for injection compared to 1169 patients receiving the 3-day regimen of oral EMEND (aprepitant) [see Clinical Studies (14.1)].
The safety profile was generally similar to that seen in the MEC study with fosaprepitant and prior HEC studies with aprepitant. However, infusion-site reactions occurred at a higher incidence in patients in the fosaprepitant group (3.0%) compared to those in the aprepitant group (0.5%). The following additional infusion-site reactions occurred in the HEC study and were not reported in the MEC study described above: infusion-site erythema (0.5%, 0.1%), infusion-site pruritus (0.3%, 0.0%), and infusion-site induration (0.2%, 0.1%), reported in the fosaprepitant group compared to the aprepitant group, respectively.
Adverse Reactions in Pediatric Patients 6 Months to 17 Years of Age for the Prevention of Nausea and Vomiting Associated with HEC or MEC Single Dose Fosaprepitant for Injection Regimen The safety of a single dose of fosaprepitant for injection in pediatric patients (6 months to 17 years) was evaluated in two active-controlled and a single-arm clinical study in patients who received either HEC or MEC. Patients also received ondansetron with or without dexamethasone. The adverse reaction profile was similar to…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS See Full Prescribing Information for a list of clinically significant drug interactions. ( 4 , 5.1 , 5.4 , 5.5 , 7.1 , 7.2 )
7.1Effect of Fosaprepitant/Aprepitant on the Pharmacokinetics of Other Drugs When administered intravenously, fosaprepitant, a prodrug of aprepitant, is converted to aprepitant within 30 minutes. Therefore, drug interactions following administration of fosaprepitant for injection are likely to occur with drugs that interact with oral aprepitant. Fosaprepitant, given as a single 150-mg dose, is a weak inhibitor of CYP3A4, and the weak inhibition of CYP3A4 continues for 2 days after single dose administration.
Single dose fosaprepitant does not induce CYP3A4. Aprepitant is a substrate, an inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9 [see Clinical Pharmacology ( 12.3 )].
Some substrates of CYP3A4 are contraindicated with fosaprepitant [see Contraindications ( 4 )]. Dosage adjustment of some CYP3A4 and CYP2C9 substrates may be warranted, as shown in Table 7. Table 7 Effects of Fosaprepitant/Aprepitant on the Pharmacokinetics of Other Drugs CYP3A4 Substrates Pimozide Clinical Impact Increased pimozide exposure Intervention Fosaprepitant is contraindicated [see Contraindications ( 4 )].
Benzodiazepines Clinical Impact Increased exposure to midazolam or other benzodiazepines metabolized via CYP3A4 (alprazolam, triazolam) may increase the risk of adverse reactions [see Clinical Pharmacology ( 12.3 )]. Intervention Monitor for benzodiazepine-related adverse reactions. Dexamethasone Clinical Impact Increased dexamethasone exposure [see Clinical Pharmacology ( 12.3 )].
Intervention Reduce the dose of oral dexamethasone by approximately 50% [see Dosage and Administration ( 2.1 )]. Methylprednisolone Clinical Impact Increased methylprednisolone exposure [see Clinical Pharmacology ( 12.3 )]. Intervention Reduce the dose of oral methylprednisolone by approximately 50% on Days 1 and 2 for patients receiving HEC and on Day 1 for patients receiving MEC.
Reduce the dose of intravenous methylprednisolone by 25% on Days 1 and 2 for patients receiving HEC and on Day 1 for patients receiving MEC. Chemotherapeutic agents that are metabolized by CYP3A4 Clinical Impact Increased exposure of the chemotherapeutic agent may increase the risk of adverse reactions [see Clinical Pharmacology ( 12.3 )]. Intervention Vinblastine, vincristine, or ifosfamide or other chemotherapeutic agents • Monitor for chemotherapeutic-related adverse reactions.
Etoposide, vinorelbine, paclitaxel, and docetaxel • No dosage adjustment needed. Hormonal Contraceptives Clinical Impact Decreased hormonal exposure during administration of and for 28 days after administration of the last dose of fosaprepitant [see Warnings and Precautions ( 5.5 ), Use in Specific Populations ( 8.3 ), and Clinical Pharmacology ( 12.3 )]. Intervention Effective alternative or back-up methods of contraception (such as condoms and spermicides) should be used during treatment with fosaprepitant and for 1 month following administration of fosaprepitant.
Examples birth control pills, skin patches, implants, and certain IUDs CYP2C9 Substrates Warfarin Clinical Impact Decreased warfarin exposure and decreased prothrombin time (INR) [see Warnings and Precautions ( 5.4 ), Clinical Pharmacology ( 12.3 )]. Intervention In patients on chronic warfarin therapy, monitor the prothrombin time (INR) in the 2-week period, particularly at 7 to 10 days, following administration of fosaprepitant with each chemotherapy cycle. Other 5-HT 3 Antagonists Clinical Impact No change in the exposure of the 5-HT 3 antagonist [see Clinical Pharmacology ( 12.3 )].
Intervention No dosage adjustment needed Examples ondansetron, granisetron, dolasetron
7.2Effect of Other Drugs on the Pharmacokinetics of Fosaprepitant/Aprepitant Aprepitant is a CYP3A4 substrate [see Clinical Pharmacology ( 12.3 )]. Co-administration of fosaprepitant with drugs that are inhibitors…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy 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 1000 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 1000 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.
8.2Lactation Risk Summary Lactation studies have not been conducted to assess the presence of aprepitant in human milk, the effects on the breastfed infant, or the effects on milk production. Aprepitant is present in rat milk. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for fosaprepitant and any potential adverse effects on the breastfed infant from fosaprepitant or from the underlying maternal condition.
8.3Females and Males of Reproductive Potential Contraception Upon administration of fosaprepitant, the efficacy of hormonal contraceptives may be reduced. Advise females of reproductive potential using hormonal contraceptives to use an effective alternative or back-up non-hormonal contraceptive (such as condoms and spermicides) during treatment with fosaprepitant and for 1 month following the last dose [see Drug Interactions ( 7.1 ), Clinical Pharmacology ( 12.3 )].
8.4Pediatric Use The safety and effectiveness of a single dose and a 3-day regimen of fosaprepitant for injection have been established in pediatric patients 6 months to 17 years for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of HEC and MEC. Use of fosaprepitant in this age group is supported by evidence from adequate and well-controlled studies of fosaprepitant for injection in adults, with additional safety, efficacy and pharmacokinetic data in pediatric patients 6 months to 17 years.
Efficacy and safety were also supported by data from an adequate and well-controlled study of a 3-day oral aprepitant regimen in pediatric patients 6 months to 17 years. The safety of the 3-day fosaprepitant for injection regimen in pediatric patients 6 months to 17 years of age was supported by an open-label study in 100 patients receiving HEC or MEC. See the full prescribing information for fosaprepitant capsules for complete clinical information regarding studies performed with oral aprepitant.
Adverse reactions were similar to those reported in adult patients [see Dosage and Administration (2.2), Adverse Reactions (6.1), Clinical Pharmacology (12.3)]. The safety and effectiveness of fosaprepitant for injection for the prevention of nausea and vomiting associated with HEC or MEC have not been established in patients less than 6 months of age. Juvenile Animal Toxicity Data In juvenile dogs treated with fosaprepitant, changes in reproductive organs were observed.
In juvenile rats treated with aprepitant, slight changes in sexual maturation were observed without an effect on reproduction. No effects on neurobehavior, sensory and motor function, or learning and memory were observed in rats. In…
🤰 Pregnancy ▾
8.1Pregnancy 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 1000 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 1000 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.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of a single dose and a 3-day regimen of fosaprepitant for injection have been established in pediatric patients 6 months to 17 years for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of HEC and MEC. Use of fosaprepitant in this age group is supported by evidence from adequate and well-controlled studies of fosaprepitant for injection in adults, with additional safety, efficacy and pharmacokinetic data in pediatric patients 6 months to 17 years.
Efficacy and safety were also supported by data from an adequate and well-controlled study of a 3-day oral aprepitant regimen in pediatric patients 6 months to 17 years. The safety of the 3-day fosaprepitant for injection regimen in pediatric patients 6 months to 17 years of age was supported by an open-label study in 100 patients receiving HEC or MEC. See the full prescribing information for fosaprepitant capsules for complete clinical information regarding studies performed with oral aprepitant.
Adverse reactions were similar to those reported in adult patients [see Dosage and Administration (2.2), Adverse Reactions (6.1), Clinical Pharmacology (12.3)]. The safety and effectiveness of fosaprepitant for injection for the prevention of nausea and vomiting associated with HEC or MEC have not been established in patients less than 6 months of age. Juvenile Animal Toxicity Data In juvenile dogs treated with fosaprepitant, changes in reproductive organs were observed.
In juvenile rats treated with aprepitant, slight changes in sexual maturation were observed without an effect on reproduction. No effects on neurobehavior, sensory and motor function, or learning and memory were observed in rats. In a toxicity study in juvenile dogs treated with fosaprepitant from postnatal day 14 (equivalent to a newborn human) to day 42 (approximately equivalent to a 2 year old human), decreased testicular weight and Leydig cell size were seen in the males at 6 mg/kg/day and increased uterine weight, hypertrophy of the uterus and cervix, and edema of vaginal tissues were seen in females from 4 mg/kg/day.
A study was also conducted in young rats to evaluate the effects of aprepitant on growth and on neurobehavioral and sexual development. Rats were treated at oral doses up to the maximum feasible dose of 1000 mg/kg twice daily (providing exposure in male and female rats lower than the exposure at the recommended pediatric human dose) from the early postnatal period (Postnatal Day 10 (equivalent to a newborn human) through Postnatal Day 58 (approximately equivalent to a 15 year old human)). Slight changes in the onset of sexual maturation were observed in female and male rats; however, there were no effects on mating, fertility, embryonic-fetal survival, or histomorphology of the reproductive organs.
There were no effects in neurobehavioral tests of sensory function, motor function, and learning and memory.
🧓 Geriatric Use ▾
8.5Geriatric Use Of the 1649 adult cancer patients treated with intravenous fosaprepitant in HEC and MEC clinical studies, 27% were aged 65 and over, while 5% were aged 75 and over. Other reported clinical experience with fosaprepitant has not identified differences in responses between elderly and younger patients. In general, use caution when dosing elderly patients as they have a greater frequency of decreased hepatic, renal or cardiac function and concomitant disease or other drug therapy [see Clinical Pharmacology ( 12.3 )].
🆘 Overdosage ▾
10 OVERDOSAGE 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.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action 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. Aprepitant has little or no affinity for serotonin (5-HT 3 ), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV).
Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with aprepitant have shown that it crosses the blood brain barrier and occupies brain NK 1 receptors. Animal and human studies have shown that aprepitant augments the antiemetic activity of the 5-HT 3 -receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.
12.2Pharmacodynamics Cardiac Electrophysiology In a randomized, double-blind, positive-controlled, thorough QTc study, a single 200-mg dose of fosaprepitant (approximately 1.3 times the recommended dose) had no effect on the QTc interval.
12.3Pharmacokinetics 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 to ∞ 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. Distribution Aprepitant is greater than 95% bound to plasma proteins.
The mean apparent volume of distribution at steady state (Vd ss ) was approximately 70 L in humans. Aprepitant crosses the blood brain barrier in humans [see Clinical Pharmacology ( 12.1 )]. Elimination Metabolism Fosaprepitant is converted to aprepitant in in vitro incubations with human liver preparations and in S9 preparations from multiple other human tissues including kidney, lung and ileum.
Thus, it appears that the conversion of fosaprepitant to aprepitant can occur in multiple extrahepatic tissues in addition to the liver. Aprepitant undergoes extensive metabolism. In vitro studies using human liver microsomes indicate that aprepitant is metabolized primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19.
Metabolism is largely via oxidation at the morpholine ring and its side chains. No metabolism by CYP2D6, CYP2C9, or CYP2E1 was detected. In healthy young adults, aprepitant accounts for approximately 24% of the radioactivity in plasma over 72 hours following a single oral 300 mg dose of [ 14 C]-aprepitant, indicating a substantial presence of metabolites in the plasma.
Seven metabolites of aprepitant, which are only weakly active, have been identified in human plasma. Excretion Following administration of a single intravenous 100 mg dose of [ 14 C]-fosaprepitant to healthy subjects, 57% of the radioactivity was recovered in urine and 45% in feces. Aprepitant is eliminated primarily by metabolism; aprepitant is not renally excreted.
The apparent terminal half-life ranged from approximately 9 to 13 hours. Specific Populations Age: Geriatric Population Following oral administration of a single 125 mg dose of aprepitant on Day 1 and 80 mg once daily on Days 2 through 5, the AUC 0 to 24hr of aprepitant was 21% higher on Day 1 and 36% higher on Day 5 in elderly (65 years and older) relative to younger adults. The C max was 10% higher on Day 1 and 24% higher on Day 5 in elderly relative to younger adults.
These differences are not considered clinically meaningful [see Use in Specific Populations (8.5)]. Age: Pediatric Population Single Dose Fosaprepitant for Injection Regimen: Simulated systemic exposures of aprepitant in pa…
🧬 Mechanism of Action ▾
12.1Mechanism of Action 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. Aprepitant has little or no affinity for serotonin (5-HT 3 ), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV).
Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with aprepitant have shown that it crosses the blood brain barrier and occupies brain NK 1 receptors. Animal and human studies have shown that aprepitant augments the antiemetic activity of the 5-HT 3 -receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Fosaprepitant for injection: Single dose glass vial containing 150 mg of fosaprepitant as a white to off-white lyophilized powder for reconstitution. Supplied as follows: NDC 31722-165-31 1 vial per carton. Storage Fosaprepitant for injection vials must be refrigerated, store at 2°C to 8°C (36°F to 46°F).
The reconstituted final drug solution is stable for 24 hours at ambient room temperature [at or below 25°C (77°F)]. Discard unused portion.
📋 Description ▾
11 DESCRIPTION Fosaprepitant for injection is a sterile, lyophilized formulation containing fosaprepitant dimeglumine, a prodrug of aprepitant, a substance P/neurokinin-1 (NK 1 ) receptor antagonist, an antiemetic agent, chemically described as 1-Deoxy-1-(methylamino)-D-glucitol[3-[[(2 R ,3 S )-2-[(1 R )-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1 H -1,2,4-triazol-1-yl]phosphonate (2:1) (salt). Its molecular formula is C 23 H 22 F 7 N 4 O 6 P ⋅ 2(C 7 H 17 NO 5 ) and its structural formula is: Fosaprepitant dimeglumine is a white to light brown powder with a molecular weight of 1004.83.
It is soluble in water and methanol. Each vial of fosaprepitant for injection for administration as an intravenous infusion contains 150 mg of fosaprepitant (equivalent to 245.3 mg of fosaprepitant dimeglumine) and the following inactive ingredients: edetate disodium (5.4 mg), lactose anhydrous (375 mg), polysorbate 80 (75 mg), sodium hydroxide and/or hydrochloric acid (for pH adjustment). fosaprepitantstructure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Hypersensitivity Advise patients that hypersensitivity reactions, including anaphylaxis and anaphylactic shock, have been reported in patients taking fosaprepitant for injection. Advise patients to seek immediate medical attention if they experience signs or symptoms of a hypersensitivity reaction, such as hives, rash and itching, skin peeling or sores, flushing, difficulty in breathing or swallowing, or dizziness, rapid or weak heartbeat or feeling faint [see Warnings and Precautions ( 5.2 )].
Infusion Site Reactions Advise patients to seek medical attention if they experience new or worsening signs or symptoms of an infusion site reaction, such as erythema, edema, pain, necrosis, vasculitis, or thrombophlebitis at or near the infusion site [see Warnings and Precautions ( 5.3 )]. Drug Interactions Advise patients to discuss all medications they are taking, including other prescription, non-prescription medication or herbal products [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 )]. Warfarin: Instruct patients on chronic warfarin therapy to follow instructions from their healthcare provider regarding blood draws to monitor their INR during the 2-week period, particularly at 7 to 10 days, following initiation of fosaprepitant for injection with each chemotherapy cycle [see Warnings and Precautions ( 5.4 )].
Hormonal Contraceptives: Advise patients that administration of fosaprepitant for injection may reduce the efficacy of hormonal contraceptives. Instruct patients to use effective alternative or back-up methods of contraception (such as condoms and spermicides) during treatment with fosaprepitant for injection and for 1 month following administration of fosaprepitant for injection [see Warnings and Precautions ( 5.5 ), Use in Specific Populations ( 8.3 )]. Manufactured for: Camber Pharmaceuticals, Inc.
Piscataway, NJ 08854. Manufactured by: Aspiro Pharma Limited Survey No. 321, Biotech Park, Phase – III Karkapatla Village, Markook (Mandal) Siddipet, Telangana-502281, India.
Revised: 05/2026 fosaprepitantcamberlogo fosaprepitantaspirologo