Ceritinib

Pronunciation: pronunciation varies by local usage.

Generic name: ceritinib
Brand names: Zykadia
Drug class: ALK kinase inhibitor
Form: Tablets
Route: Oral
Legal status: Prescription-only medicine

Availability and supply rules vary by country

Trade names by country: United States · Canada

What ceritinib is and how it works

Ceritinib is an oral ALK kinase inhibitor indicated for adults with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. (1)

Ceritinib is a prescription oral targeted therapy managed by an oncology specialist. It does not replace emergency treatment for severe adverse reactions. A specialist must confirm eligibility and the dosing plan.

Mechanism of action: how ceritinib works

Ceritinib is a selective inhibitor of anaplastic lymphoma kinase (ALK) and other kinases, blocking signaling pathways that promote cancer cell growth. (1)

What ceritinib is used for

ALK-positive metastatic non-small cell lung cancer

Ceritinib is indicated for adults with metastatic NSCLC whose tumors are ALK-positive as detected by an FDA-approved test. Treatment is initiated and managed by a specialist. (1)

Before taking ceritinib

Do not take / not appropriate for

No contraindications are listed in the US prescribing information. Treatment decisions are made by the oncology specialist. (all products) (1)

Tell your clinician about

Any new or worsening symptoms, particularly diarrhea, nausea, vomiting, abdominal pain, fatigue, cough, breathlessness, fever, chest pain, irregular heartbeat, dizziness, fainting, increased thirst, frequent urination, or blurred vision.
Pregnancy, plans for pregnancy, or breastfeeding (contraception and breastfeeding instructions apply).
History of liver or pancreas problems, heart disease, or diabetes.
All medicines, including other cancer treatments, over-the-counter products, herbals, and supplements.
Whether the patient can manage the oral dosing schedule and report symptoms promptly.

(1)

How to take ceritinib

Take ceritinib exactly as prescribed by the oncology specialist. The usual dose is 450 mg once daily with food.
Swallow tablets whole with a full glass of water. Do not crush or chew.
If you experience certain side effects, the specialist may lower the dose or pause treatment. Do not change the dose or stop taking ceritinib without the specialist's advice.

(1)

Procedures and treatment changes

Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1)

Missed dose

If a dose is missed, take the next dose at the regular time. Do not take an extra dose to make up for the missed one. Contact the oncology clinic if unsure.

Overdose

In case of suspected overdose, contact the poison control center or emergency services immediately. Overdose may worsen side effects such as severe gastrointestinal symptoms and heart rhythm changes. (1)

Side effects

Common side effects include gastrointestinal symptoms such as diarrhea, nausea, vomiting, and abdominal pain. Serious side effects can include liver problems, lung inflammation, heart rhythm changes, pancreatitis, high blood sugar, and slow heart rate. Contact the oncology team promptly for any concerning symptoms.

Diarrhea

What to notice: Frequent loose or watery stools.

What to do: Report diarrhea that is severe, persistent, or accompanied by blood or mucus. The specialist may recommend supportive medicines or dose adjustment. (1)

Nausea and vomiting

What to notice: Feeling sick or being sick after taking the medicine.

What to do: Take with food as directed to help reduce nausea. Persistent vomiting may require dose adjustment by the specialist. (1)

Abdominal pain

What to notice: Pain or discomfort in the stomach area.

What to do: Contact the team if pain is severe or persistent, as it may indicate pancreatitis or other serious conditions. (1)

Fatigue

What to notice: Unusual tiredness or weakness.

What to do: Discuss persistent fatigue with the specialist; it may be disease- or treatment-related. (1)

Liver problems (hepatotoxicity)

What to notice: Yellowing of skin or eyes (jaundice), dark urine, right upper abdominal pain, bleeding or bruising more easily.

What to do: Contact the oncology team immediately for blood tests. Do not stop ceritinib unless instructed. (1)

Lung inflammation (pneumonitis/interstitial lung disease)

What to notice: New or worsening cough, shortness of breath, chest pain, fever.

What to do: Seek urgent medical attention. Let the treating clinician decide whether to continue or stop ceritinib. (1)

Heart rhythm changes (QT prolongation)

What to notice: Chest pain, fast or irregular heartbeat, fainting, dizziness.

What to do: Seek immediate medical care. The emergency clinician will assess the need for ECG and management. (1)

High blood sugar (hyperglycemia)

What to notice: Increased thirst, frequent urination, blurred vision, tiredness, breath that smells fruity.

What to do: Contact the oncology team; they will check blood sugar and may adjust treatment. (1)

Pancreatitis

What to notice: Severe upper abdominal pain often radiating to the back, with nausea and vomiting.

What to do: Seek emergency medical attention. The clinician will evaluate and manage, including possible ceritinib discontinuation. (1)

Slow heart rate (bradycardia)

What to notice: Dizziness, fainting, extreme tiredness, feeling that the heart is beating slowly.

What to do: Contact the oncology team; they will check heart rate and blood pressure. (1)

Serious warnings

Interstitial lung disease/pneumonitis — emergency

Symptoms: New or worsening cough, shortness of breath, chest pain, fever.

Action: Seek immediate medical attention. The treating clinician will decide whether to continue or stop ceritinib. This condition can be life-threatening. (1)

Severe liver problems — urgent

Symptoms: Yellow skin or eyes, dark urine, severe upper right abdominal pain, confusion, or easy bleeding.

Action: Contact the oncology team immediately for assessment. The specialist will manage dosing based on liver tests. (1)

Pancreatitis — emergency

Symptoms: Severe upper abdominal pain often radiating to the back, with nausea and vomiting.

Action: Seek emergency medical attention. The emergency clinician will assess and manage, including the decision on ceritinib. (1)

Heart rhythm problems (QT prolongation) — emergency

Symptoms: Chest pain, fast or irregular heartbeat, fainting.

Action: Seek immediate medical care. The emergency clinician will check eCG and manage accordingly. (1)

Interactions

Medicine or test	Effect	Action
Strong CYP3A inhibitors (e.g., certain antifungals like ketoconazole, some antibiotics like clarithromycin)	May increase ceritinib blood levels and risk of side effects.	Avoid combination if possible. If unavoidable, the specialist will reduce the ceritinib dose by about one-third. (1)
Strong CYP3A inducers (e.g., rifampin, phenytoin, St. John's wort)	May decrease ceritinib effectiveness.	Avoid combination. (1)
Sensitive CYP3A substrates (e.g., certain statins like simvastatin, benzodiazepines like midazolam)	Ceritinib may increase their blood levels and side effects.	Avoid combination; discuss alternatives with the specialist. (1)
Narrow-therapeutic-index CYP2C9 substrates (e.g., warfarin)	Ceritinib may affect their levels, increasing risk of bleeding or clotting problems.	Avoid combination or monitor closely under specialist guidance. (1)

Pregnancy, breastfeeding, kidney/liver function, age

Pregnancy and breastfeeding

Ceritinib can cause fetal harm. Females of childbearing potential must use effective contraception during treatment and for 6 months after the last dose. Males with female partners of childbearing potential must use condoms during treatment and for 3 months after the last dose. Breastfeeding is not recommended during treatment and for 2 weeks after the last dose. (1)

Hepatic impairment

For severe hepatic impairment (Child-Pugh C), the specialist prescribes a dose about one-third lower. No dose adjustment is needed for mild to moderate impairment. (1)

Monitoring

Before starting

Confirm ALK-positive NSCLC with an FDA-approved test.
Obtain baseline liver function tests, fasting glucose, lipase/amylase, ECG, and electrolytes.
Assess for pregnancy in females of childbearing potential.
Review all medicines for potential interactions, especially CYP3A and CYP2C9 substrates.

During treatment

Monitor liver function tests at least monthly.
Monitor fasting glucose before and periodically during treatment.
Monitor lipase/amylase before and as indicated.
Perform periodic ECGs and electrolyte monitoring.
Regularly monitor heart rate and blood pressure.
Assess for adverse reactions and adjust dose as needed.

(1)

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Keep out of reach of children.

Professional information

Clinician-facing context only. Use the current local prescribing information and oncology guidelines.

All regions

Indication: ALK-positive metastatic NSCLC

Dose summary: Starting dose 450 mg once daily with food. Dose reductions: first to 300 mg, then 150 mg daily. The specialist ends treatment when 150 mg is not tolerated. Adjust for strong CYP3A inhibitors and hepatic impairment (Child-Pugh C).

Renal context: No renal dosing information is provided in the current label. (1)

Mechanism of action

Hepatic guidance

For severe hepatic impairment (Child-Pugh C), reduce dose by about one-third. No adjustment for mild to moderate impairment.

Overdose note

In case of overdose, provide supportive care with monitoring of cardiac function and electrolytes. Contact poison control. (1)

Frequently asked questions

How is ceritinib taken?

Ceritinib is taken by mouth, usually 450 mg once daily with food, as prescribed by the oncology specialist. Swallow tablets whole with water. (1)

What should I do if I miss a dose?

Take the next dose at the usual time. Do not take an extra dose. Contact your oncology team if you are unsure. (1)

Can ceritinib cause liver problems?

Yes, liver function abnormalities can occur. Your doctor will monitor your liver tests at least monthly. Report symptoms like yellowing skin/eyes, dark urine, or abdominal pain immediately. (1)

What medications should I avoid while taking ceritinib?

Avoid strong CYP3A inhibitors (e.g., certain antifungals, clarithromycin) and inducers (e.g., rifampin, St. John's wort), sensitive CYP3A substrates (e.g., simvastatin), and narrow-therapeutic-index CYP2C9 substrates (e.g., warfarin) unless specifically managed by your specialist. (1)

What is the mechanism of action of ceritinib?