Crizotinib
Cytostatic · Protein kinase inhibitor
Indications
Previously treated anaplastic lymphoma kinase (ALK)-positive advanced non-small cell lung cancer (NSCLC).
Dosage
Adults: 250 mg twice daily until disease progression or unacceptable toxicity. Adjust dose according to safety and tolerability. See literature. Children: Not recommended.
Adverse Effects
Blood dyscrasias, anorexia, hypophosphataemia, neuropathy, dizziness, dysgeusia, visual disorders, bradycardia, pneumonitis (discontinue), GI upset, rash, fatigue, oedema, raised LFTs, QT prolongation.
Risk Factor (Pregnancy/Lactation)
Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Severe hepatic impairment. Ensure adequate contraception during and for 90 days after end of treatment. Precautions: Non-adenocarcinoma NSCLC. Mild to moderate hepatic impairment, severe renal impairment. Risk factors for QT prolongation. Perform LFTs twice monthly for first two months and at least monthly thereafter. Elderly 65 years or above.
Interactions
Strong CYP3A4 inhibitors (e.g. azole antifungals, protease inhibitors) and inducers (e.g. carbamazepine, phenobarbital, phenytoin, rifamycin), CYP3A substrates with narrow therapeutic index (e.g. alfentanil, immunosuppressants, fentanyl, pimozide), P-gp substrates (e.g. digoxin, colchicine, pravastatin. UGT substrates (e.g. paracetamol, morphine), oral contraceptives. Substrates of CYP2B6, CYP2C8 or CYP2C9. Agents that prolong QT interval or cause bradycardia. St. John's Wort, grapefruit juice.
Advice to Patient
Take with or without meals. Swallow whole with a glass of water. If a dose is missed, inform prescriber. Do not take double dose. Contact prescriber if there is change in vision, severe headache, muscle pain, sore throat, cough, difficulty in urination, severe or prolonged diarrhoea (for more than 3 days), difficulty in breathing, feelings of cold and shiver. Take sufficient amount of fluids (2-3 litres per day) to maintain hydration, unless restricted by the prescriber. Avoid grapefruit and grapefruit juice during treatment. Avoid immunisation with live vaccines during treatment and for 6 months after completion of treatment.
Pharmacokinetics
Bioavailability: 43%. Metabolism: Hepatic. Half-life elimination: Terminal: 42 hrs. Time to peak, plasma: 4-6 hrs Excretion: Faeces (63%). Urine (22%).
Brands with this active ingredient
Compiled by Healify Pharmacy from published drug references. How we compile it →
Always consult a pharmacist or doctor.