Generic
Alectinib
1 brands available in the market
At a glance
ALK and RET tyrosine kinase inhibitor indicated for ALK-positive advanced non-small cell lung cancer (NSCLC).
Description
Alectinib is a highly selective and potent ALK and RET tyrosine kinase inhibitor designed for treating ALK-positive advanced non-small cell lung cancer, including cases with central nervous system metastasis.
Indications
Indicated as monotherapy for first-line treatment or for patients with ALK-positive advanced NSCLC previously treated with crizotinib.
Therapeutic class
Anti neoplastic preparations, Protein kinase inhibitor
Pharmacological class
Tyrosine Kinase Inhibitor (TKI)
Pharmacology
Alectinib blocks ALK tyrosine kinase activity and downstream STAT3 and PI3K/AKT pathways, triggering apoptosis in tumor cells. It crosses the blood-brain barrier to target CNS metastases.
Mechanism of action
Inhibits ALK and RET kinase phosphorylation, inhibiting downstream signal transduction and causing tumor cell death.
Dosage
Recommended Dose: 600 mg (four 150 mg capsules) twice daily with food. Severe hepatic impairment (Child-Pugh C): 450 mg twice daily with food. Dose reductions in steps of 150 mg BD for toxicity.
Administration
Oral use. Must be taken with food. Capsules must be swallowed whole without opening or dissolving.
Missed dose
Take if missed, unless next dose is due within 6 hours. Do not take double doses. If vomiting occurs after taking, take next dose at scheduled time.
Side effects
Constipation, edema, myalgia, nausea, increased bilirubin, anemia, and rash.
Precautions & warnings
Monitor for Interstitial Lung Disease (ILD)/pneumonitis, hepatotoxicity, symptomatic bradycardia, and photosensitivity (use SPF >50 sunscreen). Avoid during pregnancy.
Contraindications
Known hypersensitivity to alectinib or any of its excipients.
Drug interactions
Co-administration with strong CYP3A inducers or inhibitors does not require dose adjustment based on combined exposure, but appropriate monitoring is advised.
Food interactions
Must be taken with food to ensure adequate bioavailability.
Use in pregnancy
May cause fetal harm. Effective contraception required during treatment and for at least 3 months after the last dose.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Use in lactation
Breast-feeding is not recommended during treatment with Alectinib.
Pediatric use
Safety and effectiveness in patients under 18 years of age have not been established.
Geriatric use
No dose adjustment required in patients aged 65 years and older.
Renal / hepatic impairment
No dose adjustment for renal impairment. Severe hepatic impairment (Child-Pugh C) starting dose is 450 mg twice daily.
Overdose effects
No specific antidote. Provide general supportive care and monitoring.
Storage conditions
Store below 30°C in a dry place away from light and moisture. Keep out of reach of children.
Chemical structure
Alectinib (C30H34N4O2)