Fosaprepitant
Generic Name: fosaprepitant
Brand Names:
Fosaprepitant
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 ,3S)-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).
Overview
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 ,3S)-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).
Uses
1 INDICATIONS & 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.
Dosage
2 DOSAGE & 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. Aprepitant capsules or aprepitant for oral suspension may be used as an alternative on Days 2 and 3.
Side Effects
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 BE Pharmaceuticals Inc., at 1-877-648-9517 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
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 ) 7.1 Effect 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.
Warnings
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 for injection 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 for injection if symptoms occur with previous use. 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.
Pregnancy
8.1 Pregnancy Risk Summary There are insufficient data on use of fosaprepitant for injection 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.
Storage
16 HOW SUPPLIED/STORAGE AND HANDLING Single dose glass vial containing 150 mg of fosaprepitant as a white to off-white lyophilized cake or powder for reconstitution. Supplied as follows: NDC 71839-104-01 1 vial per carton. Storage Fosaprepitant for injection vials must be refrigerated, store at 2°C to 8°C (36°F to 46°F).
Frequently Asked Questions
What is Fosaprepitant used for?▼
1 INDICATIONS & 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.
What are the side effects of Fosaprepitant?▼
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 BE Pharmaceuticals Inc., at 1-877-648-9517 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Can I take Fosaprepitant during pregnancy?▼
8.1 Pregnancy Risk Summary There are insufficient data on use of fosaprepitant for injection 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.
What are the important warnings for Fosaprepitant?▼
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 for injection 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 for injection if symptoms occur with previous use. 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.
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Medical Disclaimer
This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.