Aivida Trastuzumab Rezetecan for Injection

1. Indications and Usage
Non-Small Cell Lung Cancer (NSCLC):
Treatment of adult patients with unresectable locally advanced or metastatic NSCLC who have HER2(ERBB2) activating mutations and have received at least one prior systemic treatment.
Note: This indication was granted under conditional approval based on single-arm clinical trial results.
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Infusion ONLY.
Recommended Dosage:
Standard Dose: 4.8 mg/kg.
Weight Cap: If patient weight ≥85 kg, fixed dose is 408 mg.
Frequency: Administered once every 3 weeks (Q3W).
Critical Administration Instructions:
Pre-medication: Pre-medicate with antiemetics (e.g., dexamethasone, 5-HT3 receptor antagonists) prior to each administration due to emetogenic potential.
Infusion Time: Initial infusion over 90 minutes. If tolerated, subsequent infusions may be administered over 30 minutes.
Preparation: Reconstitute and dilute by qualified personnel. Do not shake. Do not use Sodium Chloride Injection; use 5% Glucose Injection only. Protect from light.
Filtration: Use only 0.20 or 0.22 μm polyethersulfone (PES) or polysulfone (PS) inline filters.
3. Mechanism of Action
Antibody-Drug Conjugate (ADC):
Composed of a humanized anti-HER2 monoclonal antibody linked to deruxtecan (a topoisomerase I inhibitor).
Targeted Delivery:
Binds to HER2 on tumor cells, internalized into the cell, and releases the cytotoxic payload, which then inhibits DNA replication and induces cell death. It also exhibits a bystander effect on neighboring HER2-low tumor cells.
4. Safety and Warnings
Interstitial Lung Disease (ILD)/Pneumonitis:
A serious and potentially fatal adverse reaction. Monitor for signs and symptoms (e.g., dyspnea, cough, fever). Initiate corticosteroids immediately if suspected. Permanently discontinue for Grade 3 or higher.
Cardiac Dysfunction:
Risk of congestive heart failure and left ventricular ejection fraction (LVEF) decline. Assess LVEF prior to initiation and periodically during treatment. Permanently discontinue for symptomatic CHF or significant LVEF drop.
Hematologic Toxicity:
Severe neutropenia, febrile neutropenia, and anemia are common. Monitor blood counts and adjust doses or interrupt treatment as necessary.
Embryo-Fetal Toxicity:
Can cause fetal death. Advise females of reproductive potential to use effective contraception.
5.Adverse Reactions and Clinical Research
Most Common Adverse Reactions:
Neutropenia, leukopenia, anemia, thrombocytopenia, nausea, fatigue, anorexia, vomiting, and alopecia.
Serious Adverse Events:
Platelet count decrease, anemia, ILD/pneumonitis, febrile neutropenia, and cardiac dysfunction.
6.Drug Interactions
CYP450 System:
As a large protein molecule (mAb), it is not expected to interact directly with CYP450 enzymes.
Live Vaccines:
Live or live-attenuated vaccines should be avoided during treatment.
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Trastuzumab Rezetecan.
Appearance: White to off-white blocky substance or powder.
Packaging: Single-use vial (100 mg).
Storage: Store in the original carton at 2°C to 8°C. Do not freeze.