Zykadia (ceritinib)

Zykadia® is a targeted therapy that is used to treat some non-small cell lung cancers (NSCLC) that have a certain abnormal lymphoma kinase (ALK) mutation. ALK mutation is determined by biomarker tests (molecular testing) conducted on a biopsy sample of the tumor. Zykadia is an ALK inhibitor and is also classified as a tyrosine kinase inhibitor (TKI). 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, Zykadia may shrink the cancer or slow the cancer’s progression.1,2

Zykadia 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 Zykadia 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

Taking Zykadia

Zykadia is a capsule that is taken by mouth. It is taken once daily with food. The dosage of Zykadia 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 Zykadia, as it may increase the level of Zykadia in the blood to a harmful level.2

Side Effects of Zykadia

Zykadia 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 Zykadia 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, Zykadia can cause severe side effects, and patients taking Zykadia 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 Zykadia 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 Zykadia 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 Zykadia 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 Zykadia, as it may be hazardous to the fetus. It is not recommended for men or women to conceive a child while taking Zykadia, and patients are advised to use barrier methods of contraception (i.e. condoms). It is not known whether Zykadia passes into breast milk, and patients should not breastfeed while taking Zykadia.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: October 2018.
View References
  1. Zykadia product website, Novartis Pharmaceuticals Corporation. Accessed online on 9/28/16 at http://www.us.zykadia.com/.
  2. Chemocare. Accessed online on 9/28/16 at http://chemocare.com/chemotherapy/drug-info/ceritinib.aspx.
  3. NCCN Clinical Practice Guideline in Oncology (NCCN Guidelines) Non-Small Cell Lung Cancer, Version 5.2017 - March 16, 2017. available at NCCN.org
  4. My Cancer Genome. Accessed online on 8/14/16 at https://www.mycancergenome.org/.
  5. Genetics Home Reference, National Institutes of Health. Accessed online on 8/2/16 at https://ghr.nlm.nih.gov/.