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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Anaplastic lymphoma kinase (ALK) inhibitors
ceritinib
L01ED02
Adult Dosing
- Non-Small Cell Lung Cancer (NSCLC): 450 mg orally once daily with a low-fat meal until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of metastatic anaplastic lymphoma kinase (ALK)-positive non-small cell lung cancer (NSCLC) detected by an FDA-approved test
Mechanism of Action
- Selective, ATP-competitive inhibitor of anaplastic lymphoma kinase (ALK)
- Inhibits IGF-1R, ROS1, and InsR at higher concentrations
- Induces apoptosis and inhibits proliferation in ALK-dependent tumor cells
Contraindications
- Hypersensitivity to ceritinib or any of its excipients
Adverse Reactions
- Diarrhea, nausea, vomiting, and abdominal pain
- Fatigue and elevated transaminases
- Prolonged QT interval and bradycardia
- Interstitial lung disease (ILD) / pneumonitis
- Hyperglycemia and increased lipase/amylase
Drug Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole): increase ceritinib exposure, avoid or reduce dose
- Strong CYP3A inducers (e.g., rifampin): decrease ceritinib exposure, avoid concurrent use
- CYP3A and CYP2C9 substrates: ceritinib may alter their plasma concentrations
- Drugs known to prolong QT interval: monitor ECG closely
- Bradycardia-inducing drugs (e.g., beta-blockers): monitor heart rate
Curated Content: Needs Vetting Before Put to Clinical Use