Zykadia (ceritinib)

Reviewed by: HU Medical Review Board | Last reviewed: July 2022 | Last updated: July 2022

Zykadia® is a targeted therapy that is used to treat some non-small cell lung cancers (NSCLC) that have a certain anaplastic lymphoma kinase (ALK) gene mutation. ALK mutation is determined by biomarker tests (molecular testing) conducted on a biopsy sample of the tumor. Ceritinib is an ALK inhibitor and is also classified as a kinase inhibitor. It is designed to block the activating sites (tyrosine kinases) of several proteins within the cancer cell. These proteins can stimulate cancer growth when the tumor has an ALK mutation. By blocking the proteins, ceritinib may shrink the cancer or slow the cancer’s progression.1,2

Ceritinib is used to treat patients with NSCLC that has a certain ALK gene mutation and has spread to other parts of the body (metastasized).1

About ALK mutations

An estimated 3-5 percent of lung tumors have mutations on the ALK gene, which stands for anaplastic lymphoma kinase. ALK mutations are more common in light smokers (may be defined as less than 10 pack years*) and/or never-smokers (patients may be considered “never smokers” if they have smoked less than 100 cigarettes in their lifetime). These mutations are also associated with younger patient age and adenocarcinomas.4,5

Receiving ceritinib

Ceritinib is available as a capsule or tablet taken by mouth. The dosage of ceritinib is determined by several factors, including the patient’s general health and ongoing response to treatment. Patients should not drink grapefruit juice or eat grapefruit during treatment with ceritinib, as it may increase the level of ceritinib in the blood to a harmful level. Patients should take their medication as prescribed by their doctor. Patients should talk to their doctor if they have any questions, or if they have questions regarding their ceritinib regimen.2

Side effects of ceritinib

Ceritinib may cause side effects, and in some cases, these side effects can be severe. Any side effects should be reported to a health care professional. Side effects experienced in greater than approximately 30 percent of patients taking ceritinib include diarrhea, decrease in hemoglobin (the protein responsible for carrying oxygen in the blood), increase in liver enzymes, nausea, vomiting, increase in creatinine in the blood (creatinine is used to monitor kidney function), abdominal pain, fatigue, increase in glucose, decrease in phosphate, and decreased appetite. Less common side effects experienced in approximately 10-29 percent of patients receiving Zykadia include constipation, increase in lipase (a pancreatic enzyme), heart burn or other esophageal disorders, rash, and an increase in total bilirubin (total bilirubin is used to monitor liver function). Less commonly, ceritinib can cause severe side effects, and patients taking ceritinib should seek medical care immediately if they experience difficulty breathing with a cough or fever, abnormal heartbeats (very fast or very slow), or dizziness. Additional side effects that are not an emergency but require medical attention include frequent diarrhea (4-6 episodes within 24 hours), nausea, vomiting (more than 4-5 times within 24 hours), signs of dehydration (tiredness, dry mouth, dark and decreased urine, or dizziness), yellowing of the skin or whites of the eyes (jaundice), dark or brown urine, decreased appetite, pain on the right side of the stomach region, bleeding or bruising more than normal, itching, increase in blood sugar, increased thirst, increased hunger, headaches, trouble thinking or concentrating, increased urination, blurred vision, tiredness, breath that smells like fruit, or coughing with or without mucus. This is not an exhaustive list of all potential side effects of ceritinib. Talk to your healthcare provider or pharmacist for further information.1,2


Patients receiving ceritinib should talk to their doctor about any other medications (prescription and over-the-counter), herbal remedies, and any supplements they are taking, as well as any other health conditions. Patients who have diabetes, a glucose intolerance, or those who take a corticosteroid medicine are at an increased risk of high blood sugar while taking ceritinib and should discuss blood sugar monitoring and management options with their doctor. If you are pregnant, plan to become pregnant, or are breastfeeding or plan to breastfeed, talk with your doctor. Ceritinib can cause harm to a developing fetus and should not be taken by women who are pregnant. While taking ceritinib, males with female partners who can become pregnant, and females who can become pregnant, should both use contraceptives during treatment and for a period of time after completing treatment (patients should discuss appropriate birth control methods, and how long they need to use them, with their doctor). Females should not breastfeed during ceritinib treatment and for a period of time following the final dose (patients should discuss breastfeeding considerations with their doctor).2*Pack years is a term used to help quantify the equivalent of how many years a patient has smoked.  It is calculated by multiplying the number of packs of cigarettes smoked per day by the number of years the person has smoked. For example, smoking one pack per day for one year equals 1 pack year, whereas smoking two packs per day for two years equals 4 pack years.

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