Ruitanning Fosrolapitant and Palonosetron Hydrochloride for Injection

1. Indications and Usage
Highly Emetogenic Chemotherapy (HEC):
Prevention of acute and delayed nausea and vomiting (N&V) in adult patients receiving highly emetogenic chemotherapy (HEC).
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Recommended Dosage:
Standard Dose: Fosrrolapitant 218 mg and Palonosetron Hydrochloride 0.25 mg (one vial).
Timing: Must be administered on Day 1 of each chemotherapy cycle, prior to the start of chemotherapy.
Infusion Time: The infusion duration must be at least 60 minutes.
Critical Administration Instructions:
Dilution: Must be diluted in 0.9% Sodium Chloride Injection.
Combination Therapy: Must be used in conjunction with other antiemetics (e.g., dexamethasone) to achieve optimal emetic control.
Frequency: The interval between two administrations must be no less than 2 weeks.
3. Mechanism of Action
Dual Blocking:
Fosrrolapitant: A long-acting Neurokinin-1 (NK1) receptor antagonist that prevents delayed N&V mediated by Substance P.
Palonosetron: A long-acting 5-HT3 receptor antagonist that effectively blocks acute N&V triggered by serotonin release from the gastrointestinal tract.
4. Safety and Warnings
Hypersensitivity:
Anaphylactic reactions have been reported. Appropriate medical support must be available in case of a hypersensitivity reaction.
QT Prolongation:
Exercise caution when co-administering with other drugs that are known to prolong the QT interval.
5-Hydroxytryptamine Syndrome (5-HTS):
May occur when administered with other serotonergic drugs (e.g., SSRIs, SNRIs).
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions:
Constipation, hiccups, abdominal distension, anorexia, injection site reactions, and transient elevations in liver enzymes.
Clinical Research Highlights:
In Phase 3 trials, the combination demonstrated superior complete response rates (no vomiting and no rescue medication) in both the acute and delayed phases compared to control arms.
6. Drug Interactions
CYP2D6 Substrates:
Concomitant use with narrow therapeutic index CYP2D6 substrates (e.g., thioridazine, pimozide) is contraindicated.
CYP3A4 Inducers:
Concomitant use with strong CYP3A4 inducers (e.g., rifampin) may significantly reduce fosrrolapitant plasma concentrations and efficacy.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredients: Fosrrolapitant and Palonosetron Hydrochloride.
Appearance: White to off-white lyophilized cake or loose body prior to reconstitution.
Packaging: Single-use vial.
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.