Saimeina Befotertinib Mesylate Capsules

1. Indications and Usage
Befotertinib is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have progressed on or after EGFR-TKI therapy and have confirmed EGFR T790M mutation-positive disease.
2. Dosage and Administration
Recommended Dosage: The recommended starting dosage is 75 mg orally once daily for the first 21 days.
Dose Escalation: If no severe adverse reactions or Grade ≥2 thrombocytopenia or headache occur, the dosage may be escalated to 100 mg once daily thereafter. Treatment continues until disease progression or intolerable toxicity.
Administration: The capsules can be taken with or without food. Swallow the capsules whole with water; do not chew or crush.
Missed Dose: If a dose is missed and the delay is more than 12 hours, take the missed dose. If less than 12 hours, skip the missed dose and take the next dose at the scheduled time.
Dose Modification: Dosage interruptions or reductions are required based on the severity of adverse reactions.
3. Mechanism of Action
Befotertinib is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). It irreversibly binds to and inhibits both sensitizing EGFR mutations (such as Exon 19 deletion and L858R) and the resistant T790M mutation, thereby blocking downstream signaling pathways and inhibiting tumor cell growth.
4. Safety and Warnings
Interstitial Lung Disease: Monitor for respiratory symptoms. Permanent discontinuation is required for any grade of interstitial lung disease.
Thromboembolism: Venous thromboembolism and pulmonary embolism have been reported. Evaluate risks and consider prophylactic anticoagulation for high-risk patients.
Hepatotoxicity: Monitor liver function regularly. Dose interruption, reduction, or discontinuation may be necessary for Grade ≥3 elevations in liver enzymes.
QTc Prolongation: Monitor ECG, especially in patients with risk factors for arrhythmia. Suspend treatment if QTc interval exceeds 500 ms.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: The most common adverse reactions include thrombocytopenia, rash, anemia, venous thromboembolism, headache, fatigue, and musculoskeletal pain.
Clinical Research: In clinical trials, serious adverse reactions included pulmonary embolism, other venous thromboembolism events, and thrombocytopenia.
6. Drug Interactions
CYP3A4 Inhibitors: Strong CYP3A4 inhibitors may increase plasma concentrations of befotertinib.
CYP3A4 Inducers: Strong CYP3A4 inducers may decrease plasma concentrations of befotertinib.
QTc-Prolonging Drugs: Concomitant use may increase the risk of QTc interval prolongation.
7. Pharmaceutical Information
Composition: The active ingredient is Befotertinib. Excipients include mannitol, microcrystalline cellulose, croscarmellose sodium, colloidal silicon dioxide, and sodium stearyl fumarate.
Appearance: The contents of the capsules are white or off-white powder.
Storage: Store at a temperature not exceeding 25°C in the original packaging.