Tanneng Fosaprepitant Dimeglumine for Injection

1. Indications and Usage
Highly Emetogenic Chemotherapy (HEC):
Prevention of acute and delayed nausea and vomiting (N&V) in adult patients (≥18 years) receiving highly emetogenic chemotherapy (HEC).
Moderately Emetogenic Chemotherapy (MEC):
Prevention of delayed N&V in adult patients receiving moderately emetogenic chemotherapy (MEC) (pediatric use approved for ≥12 years in some jurisdictions).
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Recommended Dosage:
Adult Dose: 150 mg (single dose).
Pediatric Dose (≥12 years): 150 mg (single dose).
Timing: Must be administered on Day 1 of the chemotherapy cycle, 30 minutes prior to chemotherapy.
Critical Administration Instructions:
Infusion Time: Administer over 20 to 30 minutes.
Dilution: Reconstitute with 5 mL of 0.9% Sodium Chloride. Then dilute into a compatible IV bag (e.g., total volume of 150 mL).
Compatibility: Do not mix with solutions containing divalent cations (e.g., Lactated Ringer’s or Hartmann’s Solution).
Combination Therapy: Must be used in conjunction with other antiemetics (e.g., dexamethasone and a 5-HT3 antagonist).
3. Mechanism of Action
Prodrug Conversion:
Fosaprepitant is a water-soluble prodrug that is rapidly converted to the active moiety, aprepitant, upon intravenous administration.
NK1 Receptor Antagonism:
Aprepitant is a selective, high-affinity antagonist at the neurokinin-1 (NK1) receptor. By blocking Substance P binding at central and peripheral nervous system sites, it inhibits the vomiting reflex arc triggered by chemotherapy.
4. Safety and Warnings
Hypersensitivity Reactions:
Serious hypersensitivity reactions, including anaphylaxis, have been reported. Discontinue immediately if signs of allergy appear.
Injection Site Reactions (ISRs):
Significant local reactions, including thrombophlebitis, extravasation, and necrosis (particularly when co-administered with vesicant chemotherapy), have been reported.
Hepatotoxicity:
As aprepitant affects hepatic metabolism, caution is required in patients with hepatic impairment.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions:
Injection site reactions (pain, erythema, induration), fatigue, constipation, cough, decreased appetite, and dizziness.
Clinical Research Highlights:
Phase 3 trials demonstrated that single-dose IV fosaprepitant provides comparable complete response rates in preventing CINV to the multi-day oral aprepitant regimen, with improved patient compliance.
6. Drug Interactions
CYP3A4 Substrates:
Aprepitant (the active metabolite) is a moderate CYP3A4 inhibitor and inducer. Dose adjustment of co-administered CYP3A4 substrates (e.g., dexamethasone, midazolam, etoposide, vincristine) is mandatory.
CYP2C9 Substrates:
May lower plasma concentrations of CYP2C9 substrates (e.g., warfarin). International Normalized Ratio (INR) must be monitored closely.
Contraindicated Drugs:
Concomitant use with drugs primarily metabolized by CYP3A4 that have narrow therapeutic indices (e.g., pimozide, quinidine, terfenadine) is contraindicated.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Fosaprepitant Dimeglumine.
Appearance: White to off-white lyophilized cake or powder.
Packaging: Single-use vial (150 mg).
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.