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Zykadia (ceritinib)

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) 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 NSCLC patients with a certain ALK gene mutation that has spread to other parts of the body (metastasized).1 In March, 2017, the National Comprehensive Cancer Network (NCCN) added ceritinib as a first-line treatment option for people with ALK gene mutation.3

About ALK mutations

An estimated 3-5% of lung tumors have mutations on the ALK gene, which stands for anaplastic lymphoma kinase. ALK mutations are more common in light smokers (defined as less than 10 pack years*) and/or never-smokers (patients are 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 a capsule that is taken by mouth. It is taken once daily with food. 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 30% 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 10-29% 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). Rarely, ceritinib can cause severe side effects, and patients taking ceritinib should seek medical care immediately if they experience difficulty breathing with a cough or low-grade 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 a complete list of side effects.1,2


Patients receiving ceritinib should talk to their doctor about other medications, herbal remedies, and any supplements they are taking, as well as any other health conditions. Patients should talk to their doctor before receiving immunizations or vaccinations while taking ceritinib to make sure they are appropriate. 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. Patients who are pregnant or may become pregnant during treatment should discuss their condition with their doctor prior to starting ceritinib, as it may be hazardous to the fetus. It is not recommended for men or women to conceive a child while taking ceritinib. Females who can become pregnant should utilize effective birth control (patients should discuss appropriate birth control methods with their doctor) throughout ceritinib treatment and for six months following the last dose of ceritinib. Males with female partners who can become pregnant should utilize condoms throughout ceritinib treatment and for three months following the last dose of ceritinib. It is not known whether ceritinib passes into breast milk, and patients should not breastfeed while taking ceritinib and for two weeks following the last dose of ceritinib.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.

Written by: Emily Downward | Last reviewed: January 2020.
  1. Zykadia product website, Novartis Pharmaceuticals Corporation. Accessed online on 9/28/16 at
  2. Chemocare. Accessed online on 9/28/16 at
  3. NCCN Clinical Practice Guideline in Oncology (NCCN Guidelines) Non-Small Cell Lung Cancer, Version 5.2017 - March 16, 2017. available at
  4. My Cancer Genome. Accessed online on 8/14/16 at
  5. Genetics Home Reference, National Institutes of Health. Accessed online on 8/2/16 at