Xalkori (crizotinib)

Xalkori® is a targeted therapy that is used to treat some non-small cell lung cancers (NSCLC) that have a certain anaplastic lymphoma kinase (ALK) or ROS1 mutation. ALK or ROS1 mutation is determined by biomarker tests (molecular testing) conducted on a biopsy sample of the tumor. Crizotinib 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 or ROS1 mutation. By blocking the proteins, crizotinib may shrink the cancer or slow the cancer’s progression.1,2

Crizotinib is used to treat patients with NSCLC that has a certain ALK or ROS1 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 crizotinib

Crizotinib is a capsule taken by mouth. The dosage is determined by several factors, including the patient’s general health, liver and kidney function, and ongoing response to treatment. Patients should not drink grapefruit juice or eat grapefruit during treatment with crizotinib, as it may increase the level of crizotinib 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 crizotinib regimen.2

Side effects of crizotinib

Crizotinib 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 crizotinib include vision problems (such as blurred vision, double vision, or increased sensitivity to light), nausea, diarrhea, and vomiting. Less common side effects experienced in approximately 10-29 percent of patients receiving Xalkori include swelling (edema), constipation, fatigue, decreased appetite, dizziness, increased liver enzymes, numbness or tingling in hands and feet, taste changes, heartburn, and rash. Rarely, crizotinib can cause severe side effects, and patients taking crizotinib should seek medical care immediately if they experience difficulty breathing with a cough or fever, slow or fast heartbeat, 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), eye irritation, 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, or coughing with or without mucus. This is not an exhaustive list of all potential side effects of crizotinib. Talk to your healthcare provider or pharmacist for further information.1,2


Patients receiving crizotinib 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 are pregnant or may become pregnant during treatment should discuss their condition with their doctor prior to starting crizotinib, as it may be hazardous to the fetus. It is not recommended for men or women to conceive a child while taking crizotinib. Females who can become pregnant should utilize effective birth control (patients should discuss appropriate birth control methods with their doctor) throughout crizotinib treatment and for at least 45 days following the last dose of crizotinib. Males with female partners who can become pregnant should utilize condoms throughout crizotinib treatment and for at least 90 days following the last dose of crizotinib (patients should discuss appropriate birth control methods with their doctor). It is not known whether crizotinib passes into breast milk, and patients should not breastfeed while taking crizotinib and for 45 days following the last dose of crizotinib.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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Written by: Emily Downward | Last reviewed: January 2021.