Furmonertinib Mesilate Tablets

Furmonertinib Mesilate ®） The English version of the instruction manual can be obtained through the US FDA and DailyMed platforms. The following is a summary of the core content based on the approval documents:

1. ‌Indications and Usage‌
Indications: Furmonertinib Mesilate is indicated for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) adult patients with EGFR exon 19 deletion or L858R mutation, as first-line therapy or after progression to other EGFR-TKI treatments.
The drug has been approved in China based on the results of the FURLONG study (a multicenter, randomized, double-blind, phase III clinical trial), which showed superior progression free survival (PFS) compared to gefitinib.
2. ‌Dosage and Administration‌
Recommended dosage: 110 mg orally, once daily, can be taken with meals or on an empty stomach.
Dosage form and specifications: Tablets containing 55 mg or 110 mg of furmonertinib.
Dose adjustment:
When a grade ≥ 3 adverse reaction occurs, medication can be suspended until it returns to grade ≤ 1, and then restarted once daily at 80 mg or 55 mg.
If the dose of 55 mg cannot be tolerated, the medication will be permanently discontinued.
3. ‌Mechanism of Action‌

Furmonertinib is a third-generation, irreversible EGFR tyrosine kinase inhibitor (TKI) with high selective inhibitory activity against EGFR sensitive mutations (such as ex19del, L858R) and drug-resistant mutations (T790M), while having weaker effects on wild-type EGFR, thereby reducing skin and gastrointestinal toxicity.

4. ‌Safety and Warnings‌
Interstitial lung disease (ILD)/pneumonia: About 1-2% of patients experience it, requiring immediate discontinuation of medication and treatment with corticosteroids.
QT interval prolongation: can increase the risk of arrhythmia. It is recommended to monitor electrocardiogram before and during treatment, especially in patients with underlying heart disease or those taking other QT prolonging drugs.
Hepatotoxicity: Some patients may experience elevated ALT/AST levels, and it is recommended to regularly monitor liver function. If transaminase>3 × ULN and bilirubin>2 × ULN, the medication should be permanently discontinued.
Embryo fetal toxicity: Animal studies have shown that it can cause fetal damage. It is recommended that women with fertility potential take effective contraceptive measures during treatment and for at least 6 months after the last dose.
5. ‌Adverse Reactions‌
Common adverse reactions (≥ 20%):
Rash, diarrhea, dry skin, itching, decreased appetite, nausea, and elevated AST/ALT.
≥ Grade 3 adverse reactions:
AST/ALT elevation (about 10%), rash (about 3%), and diarrhea (about 2%).
Laboratory abnormality:
Elevated liver enzymes, hypoalbuminemia, and dyslipidemia are common.
6. ‌Drug Interactions‌
Strong CYP3A4 inhibitors (such as ketoconazole): may increase the blood concentration of furmonertinib, it is recommended to avoid co administration; If combined use is necessary, toxic reactions should be closely monitored.
Strong CYP3A4 inducers (such as rifampicin): may significantly reduce blood drug concentration and should be avoided in combination.
P-gp substrate drugs: Furmonertinib may inhibit P-glycoprotein and increase exposure to drugs such as digoxin, and should be used with caution.
7. ‌Pharmaceutical Information‌
Product Name: Amele ® （Ameile ®）
Common name: Furmonertinib Mesilane
R&D company: Hansoh Pharma, Jiangsu
NMPA approval date: Approved in December 2021, expanded indications in 2024
FDA status: Currently in the international multicenter Phase III clinical trial phase, not yet approved in the United States
Storage conditions: Room temperature (15-30 ° C), away from light and moisture, sealed for storage