FOSAPREPITANT

Other

Brand names: Fosaprepitant

Intravenous

Mechanism of Action

12.1 Mechanism 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.

Indications

1 INDICATIONS AND USAGE Fosaprepitant for injection

in combination with other antiemetic agents

indicated in adults and pediatric patients 6 months of age and older

in combination with other antiemetic agents

Contraindications

• 4 CONTRAINDICATIONS 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

FDA 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 and concomitant drugs
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
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) ]
, ketoconazole, diltiazem) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to fosaprepitant

Known Side Effects

9 documented side effects by frequency

Nausea

>10%

Shortness of Breath

1-10%

Fever

1-10%

Diarrhea

1-10%

Vomiting

1-10%

Fatigue

1-10%

Hair Loss

1-10%

Rash

1-10%

Itching

1-10%

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Formulations

Dosage Forms

Tablet

Route

Intravenous