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Ceritinib is a kinase inhibitor that primarily targets ALK but also inhibits other kinases, such as the insulin-like growth factor 1 receptor (IGF-1R), the insulin receptor (InsR), and ROS1. It blocks ALK autophosphorylation, downstream STAT3 phosphorylation, and proliferation of ALK-dependent cancer cells.
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✅ Description:
Ceritinib is prescribed for adult patients with metastatic non-small cell lung cancer (NSCLC) that is anaplastic lymphoma kinase (ALK)-positive, as determined by an FDA-approved test. Always follow the advice of a registered healthcare professional.
✔️ Pharmacokinetics
- Absorption: Peak plasma levels are reached 4–6 hours after oral administration. The drug exhibits dose-proportional increases in AUC and Cmax from 50 to 750 mg when taken on an empty stomach.
- Distribution: Ceritinib is 97% bound to plasma proteins and has a distribution volume of 4230 L. It favors distribution to red blood cells (blood-to-plasma ratio of 1.35).
- Elimination: It has a half-life of about 41 hours, with reduced clearance at steady-state dosing.
- Metabolism: Primarily metabolized by CYP3A enzymes. Ceritinib remains the main circulating compound in the plasma after administration.
- Excretion: Around 92.3% is excreted via feces (68% as an unchanged drug), while only 1.3% is excreted in urine.
✔️ Dosage & Administration of Cerinib 150
- The recommended dose is 450 mg orally once daily with food until the disease progresses or side effects become intolerable.
- Pediatric: Safety and efficacy are not established.
- Geriatric: No significant differences were observed in elderly patients.
- Hepatic Impairment: Dose reduction is required for severe hepatic impairment.
- If a dose is missed, it can be taken unless the next dose is due within 12 hours. Vomiting after a dose does not warrant an additional dose—continue with the next scheduled dose.
- Administration should always follow the instructions of a registered healthcare professional.
✔️ Side Effects of Cerinib 150
- Common: Gastrointestinal issues like nausea, vomiting, diarrhea, and abdominal pain.
- Serious: Hepatotoxicity, interstitial lung disease (ILD)/pneumonitis, QT prolongation, hyperglycemia, bradycardia, and pancreatitis.
✔️ Drug Interactions: Cerinib 150
- Strong CYP3A Inhibitors: Increase ceritinib levels. Avoid co-administration; if unavoidable, reduce the ceritinib dose by one-third.
- Strong CYP3A Inducers: Decrease ceritinib levels. Avoid concurrent use.
- CYP3A Substrates: Ceritinib raises the levels of sensitive CYP3A substrates like midazolam, requiring dose adjustments.
- CYP2C9 Substrates: Increases warfarin exposure; monitor INR frequently.
✔️ Contraindications
- Patients with known hypersensitivity to ceritinib or its components should not use the medication.
✔️ Warnings & Precautions
- Hepatotoxicity: Regular liver function monitoring is necessary. Adjust or discontinue doses based on severity.
- ILD/Pneumonitis: Monitor for pulmonary symptoms; discontinue if confirmed.
- QT Prolongation: Avoid in patients with long QT syndrome; monitor ECG and electrolytes.
- Hyperglycemia: Monitor fasting glucose levels and manage as needed.
- Bradycardia: Monitor heart rate and avoid combining with other bradycardia-inducing drugs.
- Pancreatitis: Check amylase and lipase levels periodically.
- Pregnancy: Can harm the fetus; contraception is advised for women during treatment and 6 months afterward. Men should use condoms during and for 3 months post-treatment.
✔️ Storage:
Store below 30°C in a cool, dry place away from sunlight and out of children’s reach.
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here information is for informational purposes only.
The information contained herein should NOT be used as a substitute
for the advice of a qualified physician. This may not cover
everything about particular health conditions,
lab tests, medicines, all possible side effects, drug interactions,
warnings, alerts, etc. Please consult your healthcare professional
and discuss all your queries related to any disease or medicine. We
intend to support, not replace, the doctor-patient relationship.
