Zeruini Zorifertinib Hydrochloride Tablets

1. Indications and Usage
Non-Small Cell Lung Cancer: Treatment of adult patients with locally advanced or metastatic NSCLC who have EGFR exon 19 deletion or exon 21 (L858R) substitution mutations, and who have concurrent central nervous system (CNS) metastases.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage: 240 mg once daily.
Critical Administration Instructions:
Timing: Can be taken fasting or with food, but should be taken at approximately the same time each day.
Swallowing: Tablets must be swallowed whole; do not crush or chew.
Missed Dose: If a dose is missed, take it as soon as possible on the same day. Resume the regular schedule the next day. Do not take two doses to make up for the missed one.
Vomiting: If vomiting occurs after taking a dose, do not take an extra dose on the same day; resume the next day at the regular time.
3. Mechanism of Action
EGFR Inhibition: Zorifertinib is a potent and selective inhibitor of EGFR tyrosine kinase.
CNS Penetration: It is designed as a non-substrate of blood-brain barrier (BBB) efflux transporters, allowing it to fully penetrate the BBB and target tumor cells in the central nervous system.
4. Safety and Warnings
Hypersensitivity: Contraindicated in patients with known hypersensitivity to zorifertinib or any excipients.
Hepatotoxicity: Interstitial lung disease (ILD)/pneumonitis may occur and requires vigilant monitoring.
Dermatologic Toxicity: Rash and diarrhea are common; early intervention is necessary to manage severity.
Pregnancy and Lactation: Can cause fetal harm. Women of reproductive potential must use effective contraception during treatment and for at least 30 days after the last dose.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Rash, diarrhea, fatigue, decreased appetite, and liver function abnormalities (elevated ALT, AST).
Clinical Research Highlights: As the first EGFR-TKI specifically designed for NSCLC with CNS metastases, clinical data demonstrate its robust ability to penetrate the blood-brain barrier and control intracranial tumors.
6. Drug Interactions
CYP3A4 Modulators: Zorifertinib is primarily metabolized by CYP3A4.
Strong Inhibitors (e.g., ketoconazole, clarithromycin): May increase zorifertinib plasma concentrations; dose adjustment may be necessary.
Strong Inducers (e.g., rifampicin, carbamazepine): May decrease zorifertinib plasma concentrations and reduce efficacy.
P-gp/BCRP Substrates: Caution is advised when co-administering with substrates of P-gp or BCRP.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Zorifertinib (as hydrochloride).
Appearance: Tablets (available in 50 mg and 100 mg strengths).
Packaging: Blister packaging.
Storage: Store at room temperature; protect from moisture.