Ceritinib
ZYKADIA
What it isALK tyrosine kinase inhibitor; ALK-positive lung cancer after crizotinib.
Why this oneIt overcomes several crizotinib resistance mutations.
What limits itSevere GI toxicity — diarrhea, nausea, vomiting — in most patients, reduced by taking it with food. Hepatotoxicity; CYP3A4-dependent.
FDA-approved for
- ALK-positive non-small cell lung cancer (2014)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| ALK-positive metastatic NSCLC | Adult | 450 mg QD with food | 450 mg QD with food |
Renal Undefined
Hepatic Severe (Child-Pugh C): reduce dose ~1/3; no adjustment for mild/moderate
Instructions
- Take once daily with food
- If a dose is missed, make it up unless next dose is within 12 h
- If vomiting occurs, do not re-dose; continue next scheduled dose
- Dose reductions in 150 mg steps (450 -> 300 -> 150) for toxicity
- Unavoidable strong CYP3A inhibitor: reduce dose ~1/3
Cautions
- GI adverse reactions (diarrhea, nausea, vomiting)
- Hepatotoxicity (monitor LFTs at least monthly)
- Interstitial lung disease/pneumonitis
- QT interval prolongation
- Hyperglycemia
- Bradycardia
- Pancreatitis
- Embryo-fetal toxicity
Adverse reactions
- Diarrhea
- Nausea
- Abdominal pain
- Vomiting
- Fatigue
Pregnancy Can cause fetal harm (animal data and mechanism of action); avoid in pregnancy
Lactation No data; do not breastfeed during treatment and for 2 weeks after
NO BOXED WARNINGS
Principal riskSevere GI toxicity; take with food
Cost, est. cash$5,000–$30,000+/month or cycle
Generic entry2032 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryD
Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.
Mechanism of action: Ceritinib ballicule
