Adult: In patient with ALK-positive tumours: 750 mg once daily. Missed dose should be given if >12 hours before the next scheduled dose. Dose reduction, dosing interruption, or discontinuation may be required according to individual safety and tolerability (refer to detailed product guideline).
Special Patient Group
Patient taking CYP3A inhibitors: Reduce dose by approx 1/3, resume to usual dose upon discontinuation of treatment.
Severe: Not recommended.
Severe (Child-Pugh class C): Reduce by approx 1/3.
Should be taken with food. Take at the same time each day.
Congenital long QT syndrome. Concomitant use with β-blockers, non-dihydropyridine calcium channel blockers, clonidine, digoxin, strong CYP3A inducers.
Patient with cardiac diseases, bradycardia, predisposition for QTc prolongation, bradyarrhythmia, electrolyte abnormalities, diabetes mellitus. Severe renal and hepatic impairment. Pregnancy and lactation. Concomitant use with QT prolonging drugs (e.g. pimozide, thioridazine).
This drug may cause fatigue, dizziness or eye disorders, if affected, do not drive or operate machinery.
Establish ALK positivity and correct electrolyte abnormalities prior to initiation of treatment. Monitor renal function and LFT (including ALT, AST, total bilirubin) at baseline and monthly during therapy; fasting blood glucose, serum amylase and lipase levels, blood pressure, cardiac function (e.g. heart rate, QTc interval) periodically; signs and symptoms of pancreatitis, and gastrointestinal and pulmonary toxicities.
Increased risk of QTc prolongation with antiarrhythmics (e.g. quinidine). Enhanced hyperglycaemic effect with corticosteroids. Increased exposure with strong CYP3A inhibitors (e.g. ketoconazole, ritonavir, telithromycin, nefazodone). Decreased exposure with strong CYP3A inducer (e.g. carbamazepine, phenobarbital, rifampicin). May decrease bioavailability with proton pump inhibitors, H2-receptor antagonists, antacids. May increase serum concentration of CYP3A substrates (e.g. ciclosporin, ergotamine, fentanyl, pimozide), CYP2C9 substrates (e.g. phenytoin, warfarin). Potentially Fatal: Increased risk of bradycardia with β-blockers, non-dihydropyridine calcium channel blockers (e.g. diltiazem), clonidine, digoxin.
Food increases exposure. Increased exposure with grapefruit or grapefruit juice. Decreased exposure with St. John’s wort.
Description: Ceritinib is a selective and potent inhibitor of anaplastic lymphoma kinase (ALK), a tyrosine kinase involved in the pathogenesis of non-small cell lung carcinoma. It prevents autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signalling protein and decreases proliferation of ALK-dependent cancer cells. Pharmacokinetics: Absorption: Food increases exposure. Time to peak plasma concentration: Approx 4-6 hours. Distribution: Volume of distribution: 4,230 L. Plasma protein binding: Approx 97%. Metabolism: Metabolised in the liver by CYP3A via mono-oxygenation, O-dealkylation, N-formylation; further metabolised via glucuronidation and dehydrogenation. Excretion: Mainly via faeces (approx 92%; 68% as unchanged drug); urine (approx 1%). Elimination half-life: 31-41 hours.
Store at 25°C.
This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L01ED02 - ceritinib ; Belongs to the class of anaplastic lymphoma kinase (ALK) inhibitors. Used in the treatment of cancer.
Anon. Ceritinib. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/04/2018.Anon. Ceritinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/04/2018.Buckingham R (ed). Ceritinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2018.Joint Formulary Committee. Ceritinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/04/2018.Zykadia Capsule (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/04/2018.