Ansensha Alectinib Hydrochloride Capsules

1. Indications and Usage
ALK-Positive NSCLC: Treatment of adult patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer (NSCLC).
Diagnostic Requirement: Use is restricted to patients whose tumors have been confirmed to be ALK-positive by a validated diagnostic test.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage: 600 mg (four 150 mg capsules) twice daily.
Critical Administration Instructions:
With Food: Must be taken with food to ensure adequate drug absorption.
Swallowing: Capsules must be swallowed whole; do not open, dissolve, or chew.
Missed Dose: If a dose is missed, do not take an extra dose. Resume with the next scheduled dose.
Vomiting: If vomiting occurs after administration, do not take an additional dose. Continue with the next scheduled dose.
3. Mechanism of Action
ALK Inhibition: Alectinib is a potent and selective inhibitor of the anaplastic lymphoma kinase (ALK) tyrosine kinase.
Signal Transduction Blockade: It inhibits ALK-mediated downstream signaling pathways (e.g., STAT3, AKT), thereby inhibiting tumor cell proliferation and promoting apoptosis.
CNS Penetration: Alectinib and its active metabolite possess high lipophilicity, allowing them to cross the blood-brain barrier and effectively target ALK-positive CNS metastases.
4. Safety and Warnings
Hepatotoxicity: Elevations in ALT, AST, and total bilirubin may occur. Liver function tests should be monitored every 2 weeks for the first 2 months, then monthly.
Interstitial Lung Disease (ILD)/Pneumonitis: Monitor for new or progressive respiratory symptoms. If confirmed, discontinue permanently.
QTc Prolongation: Can cause QT interval prolongation. Baseline and periodic ECG monitoring is recommended, particularly in patients with cardiovascular risk factors.
Severe Myalgia and CPK Elevation: Monitor creatine phosphokinase (CPK) levels every 2 weeks during the first month. Instruct patients to report unexplained muscle pain or weakness.
Bradyarrhythmia: Monitor heart rate and blood pressure. Withhold or reduce dose if symptomatic bradycardia occurs.
Embryo-Fetal Toxicity: May cause fetal harm. Effective contraception is required during and for at least 1 week after the final dose.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Constipation, edema, myalgia, nausea, fatigue, anemia, increased bilirubin, and rash.
Clinical Research Highlights: The phase III ALEXANDER trial demonstrated that alectinib significantly improved progression-free survival compared to crizotinib, with robust intracranial activity in patients with baseline CNS metastases.
6. Drug Interactions
CYP3A Inhibitors: Strong CYP3A inhibitors may increase alectinib exposure. Concomitant use should be avoided or managed with caution.
CYP3A Inducers: Strong CYP3A inducers may decrease alectinib exposure. Concomitant use should be avoided.
P-gp Substrates: Alectinib may inhibit P-glycoprotein (P-gp); caution is advised when co-administered with narrow therapeutic index P-gp substrates (e.g., digoxin, dabigatran).
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Alectinib (as hydrochloride).
Appearance: Hard gelatin capsules with a black and white body and cap, containing powder or granules.
Packaging: Available in 150 mg strengths.
Storage: Store at room temperature in the original container to protect from moisture.