FOSAPREPITANT DIMEGLUMINE

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.

DistributionApre...

14.1 Prevention of Nausea and Vomiting Associated with HEC in Adults In a randomized, parallel, double-blind, active-controlled study, fosaprepitant for injection 150 mg as a single intravenous infusion (N = 1,147) was compared to a 3-day oral aprepitant regimen (N = 1,175) in patients receiving a HEC regimen that included cisplatin (≥70 mg/m 2 ). All patients in both groups received dexamethasone and ondansetron (see Table 12). Patient demographics were similar between the two treatment groups. Of the total 2,322 patients, 63% were men, 56% White, 26% Asian, 3% American Indian/Alaska Native, ...

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 ADV...

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) ]. taking pimozide. Inhibition of CYP3A4 by aprepitant, the active moiety, could result in elevated plasma concentrations of...

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...

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 f...