Cerinib 150mg Capsule

✔️ 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.