Xalkori (Crizotinib) - Oral

What Is Xalkori?

Xalkori (crizotinib) is an oral medication used to treat non-small cell lung cancer (NSCLC) that has spread in adults. It can also be used for a specific type of lymphoma in children and young adults.

To be eligible for this treatment, your lung cancer must be positive for the anaplastic lymphoma kinase (ALK) or ROS-1 mutation, and the lymphoma must be positive for ALK mutation.

Xalkori is a tyrosine kinase inhibitor that suppresses tumor cell growth or survival by blocking the activity of certain receptors, such as ALK and ROS-1. It's available in capsule form to be taken by mouth.

Drug Facts

Generic Name: Crizotinib

Brand Name(s): Xalkori

Drug Availability: Prescription

Administration Route:  Oral

Therapeutic Classification: Kinase inhibitor

Available Generically: No

Controlled Substance: N/A

Active Ingredient: Crizotinib

Dosage Form(s): Capsules

What Is Xalkori Used For?

Xalkori is a targeted therapy used to treat:

  • Metastatic NSCLC or NSCLC that has spread to other body parts and has either an ALK or ROS-1 mutation
  • Anaplastic large cell lymphoma (ALCL) with an ALK mutation that is relapsed and refractory (meaning the lymphoma has returned following initial treatment) in young adults and children one year and older
  • ALK-positive unresectable, recurrent, or refractory inflammatory myofibroblastic tumor in adults and children 1 and older

Special tests called genomic testing are performed on the cancer cells to find these mutations. Specialized laboratories do this testing.

How to Take Xalkori

Before starting treatment, read the prescription label and patient information leaflet provided to you with your medication. Talk to your healthcare provider or pharmacist if you have any questions.

Xalkori is dispensed in capsule forms meant to be swallowed whole. You can take them with or without food. However, do not consume grapefruit or grapefruit products when taking them, including supplements that contain grapefruit extract. Grapefruit can increase the amount of drug in the body, potentially causing side effects.

Children should only take Xalkori under adult supervision.

Storage 

Keep Xalkori at room temperature (between 68 F and 77 F) and in its original packaging. Do not store it in the bathroom. It should also be kept out of reach of children and pets to prevent accidental consumption.

How Long Does Xalkori Take to Work?

Your oncologist may wait a few months after starting Xalkori to do imaging studies, which will help determine how well the cancer is responding to the treatment.

What Are the Side Effects of Xalkori?

This is not a complete list of side effects, and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your healthcare provider or a pharmacist. You may report side effects to the Food and Drug Administration (FDA) at www.fda.gov/medwatch or 800-FDA-1088.

Common Side Effects 

Side effects of Xalkori may be slightly different when taken for lung cancer versus being taken for lymphoma. The most common side effects, when taken for NSCLC, include:

  • Gastrointestinal (GI) upset, including nausea, vomiting, or diarrhea
  • Vision changes
  • Swelling to the face, hands, or feet (peripheral edema)
  • Constipation
  • Changes in liver tests
  • Feeling tired
  • Numbness/tingling to the arms or legs
  • Decreased appetite
  • Dizziness
  • Upper respiratory infection

The most common side effects of Xalkori when it’s taken for lymphoma include the list above but also:

  • Itching skin
  • Headache
  • Fever 
  • Mouth sores
  • Abdominal pain
  • Cough
  • Low blood counts
  • Abdominal pain
  • Abnormal kidney tests
  • Changes in blood sugar levels
  • Muscle or joint pain

If you have nausea when taking crizotinib, taking your dose with food may be helpful. Crizotinib-related diarrhea can be managed with standard measures, such as antidiarrheal medications, dietary changes, and hydration. Your healthcare team can provide more guidance on strategies for managing these side effects.

Although GI effects with crizotinib are common, they tend to improve over time.

Severe Side Effects

Call your healthcare provider immediately if you have serious side effects. Dial 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

  • Decreased white blood cells, platelets, and hemoglobin
  • Pneumonitis (inflammation of the lungs), which can cause shortness of breath, cough, and wheezing
  • Vision disorders, including blurred vision and vision impairment
  • Bradycardia (low heart rate), which can cause chest pain, shortness of breath, easy fatigue, lightheadedness, or dizziness, and shortness of breath


Long-Term Side Effects 

Xalkori has the potential to cause infertility in both men and women. Talk to your healthcare provider if this is a concern for you.

Report Side Effects

Xalkori may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (800-332-1088).

Dosage: How Much Xalkori Should I Take?

Drug Content Provided and Reviewed by IBM Micromedex®

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (capsules):
    • For non-small cell lung cancer:
      • Adults—250 milligrams (mg) 2 times a day. Your doctor may adjust your dose as needed and tolerated.
      • Children—Use and dose must be determined by your doctor.
    • For systemic anaplastic large cell lymphoma:
      • Adults and children 1 year of age and older—Dose is based on body surface area (BSA) and must be determined by your doctor. The dose is usually 280 milligrams per square meter (mg/m[2]) of BSA, taken 2 times a day. Your doctor may adjust your dose as needed and tolerated.
        • BSA 1.70 meter squared (m2) or more—500 mg 2 times a day.
        • BSA 1.52 to 1.69 m2—450 mg 2 times a day.
        • BSA 1.17 to 1.51 m2—400 mg 2 times a day.
        • BSA 0.81 to 1.16 m2—250 mg 2 times a day.
        • BSA 0.60 to 0.80 m2—200 mg 2 times a day.
      • Children younger than 1 year of age—Use and dose must be determined by your doctor.
    • For inflammatory myofibroblastic tumor:
      • Adults—250 milligrams (mg) 2 times a day. Your doctor may adjust your dose as needed and tolerated.
      • Children 1 year of age and older—Dose is based on body surface area (BSA) and must be determined by your doctor. The dose is usually 280 milligrams per square meter (mg/m[2]) of BSA, taken 2 times a day. Your doctor may adjust your dose as needed and tolerated.
        • BSA 1.70 meter squared (m2) or more—500 mg 2 times a day.
        • BSA 1.52 to 1.69 m2—450 mg 2 times a day.
        • BSA 1.17 to 1.51 m2—400 mg 2 times a day.
        • BSA 0.81 to 1.16 m2—250 mg 2 times a day.
        • BSA 0.60 to 0.80 m2—200 mg 2 times a day.
      • Children younger than 1 year of age—Use and dose must be determined by your doctor.

Modifications 

You may need a dose adjustment if you experience severe side effects or have abnormal blood test results. Typically, your healthcare provider will hold your treatment with Xalkori until any side effects improve before resuming it at a lower dose.

Routine bloodwork monitoring, including tests to evaluate complete blood count (CBC), kidney function, and liver function, is recommended throughout therapy.

If there is any pre-existing liver or kidney dysfunction, your healthcare provider may start you at a lower dose of Xalkori. 

Missed Dose 

If you miss a dose, take it as soon as you remember unless it's within six hours of the next dose. In that case, skip the missed dose and resume your regular dosing schedule. Never double up the medication to make up for a missed dose.

Overdose: What Happens If I Take Too Much Xalkori?

Notify your healthcare team immediately if you take more Xalkori than prescribed. Depending on how much was taken, they may want to keep an eye on things such as lab tests and heart rhythm to ensure everything is OK.

What Happens If I Overdose on Xalkori?

If you think you or someone else may have overdosed on Xalkori, call a healthcare provider or the Poison Control Center (800-222-1222).

If someone collapses or isn't breathing after taking Xalkori, call 911 immediately.

Precautions

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It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. It may also cause birth defects if the father is using it when his sexual partner becomes pregnant. If you are a woman who can get pregnant, your doctor may do tests to make sure you are not pregnant before starting treatment. Female patients should use effective birth control during treatment with this medicine and for at least 45 days after the last dose. Male patients who have female partners should use effective birth control during treatment with this medicine and for at least 90 days after the last dose. If you think you have become pregnant while using this medicine, tell your doctor right away.

This medicine may cause swelling of the lungs (pneumonitis), which can be life-threatening and requires immediate medical attention. Check with your doctor right away if you have a cough with or without mucous, trouble breathing, or a fever.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, unusual tiredness or weakness, or yellow eyes or skin. These could be symptoms of a serious liver problem.

Contact your doctor right away if you have any changes to your heart rhythm. You might feel dizzy or faint, or you might have a slow, fast, pounding, or uneven heartbeat. Make sure your doctor knows if you or anyone in your family has ever had a heart rhythm problem including QT prolongation.

This medicine may cause serious stomach or bowel problems. Check with your doctor right away if you have black, tarry stools, colicky or burning stomach pain, constipation, diarrhea, loss of appetite, nausea, pain in the back of throat or chest when swallowing, or vomiting blood or material that looks like coffee grounds.

Cancer medicines can cause constipation, diarrhea, nausea, or vomiting in most people, sometimes even after receiving medicines to prevent it. Ask your doctor or nurse about other ways to control these side effects.

This medicine may cause dizziness, tiredness, blurred vision, or other vision problems (eg, flashes of lights, floaters, sensitivity of the eyes to light). If any of these occur, do not drive or do anything else that could be dangerous until you know how this medicine affects you. Check with your doctor if visual changes occur. Your doctor may want your eyes be checked by an ophthalmologist (eye doctor).

This medicine may cause an increased sensitivity of the skin to sunlight (photosensitivity). Check with your doctor right away if you have itching, redness or other discoloration of the skin, severe sunburn, or skin rash. Use sunscreen or sunblock lotions with a sun protection factor (SPF) on a regular basis when you are outdoors. Wear protective clothing and hats and avoid sunlamps and tanning beds.

Talk with your doctor before using this medicine if you plan to have children. Some men and women who use this medicine have become infertile (unable to have children).

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (eg, St. John's wort) or vitamin supplements.

What Are Reasons I Shouldn't Take Xalkori?

Do not take Xalkori if you are allergic to it or its ingredients. You should not take Xalkori during pregnancy or if you are breastfeeding.

What Other Medications Interact With Xalkori?

Other medications and substances can interact with Xalkori. Before starting treatment, talk with your healthcare provider about any other medicines you take or plan to take, including over-the-counter (OTC) products, prescription drugs, vitamins, herbs, or plant-based medicines.

Some of the medications that should be avoided when taking Xalkori due to potential interactions include:

Other interactions may occur. Talk with your pharmacist or healthcare provider for more detailed information about medication interactions with Xalkori.

What Medications Are Similar?

Other targeted medications that treat ALK+ metastatic lung cancer are available. These medications include:

  • Zykadia (ceritinib)
  • Alecensa (alectinib)
  • Alunbrig (brigatinib)
  • Lobrena (lorlatinib)

These medications should not be taken along with Xalkori.

Frequently Asked Questions

  • What is Xalkori used for?

    Xalkori treats non-small cell lung cancer that has spread to other areas of the body and has an ALK or ROS-1 mutation. It is also used to treat anaplastic large cell lymphoma that has an ALK mutation and has come back after chemotherapy.

  • How does Xalkori work?

    Xalkori works by blocking ALK and ROS-1 receptors, which slows the growth of cancer cells.

  • What are the side effects of Xalkori?

    Common side effects associated with taking Xalkori include gastrointestinal problems (e.g., nausea, vomiting, diarrhea), changes in liver and kidney function test results, headache, abdominal pain, and decreased appetite.

  • How to stop taking Xalkori?

    Do not stop taking Xalkori unless instructed to do so by your healthcare provider.

How Can I Stay Healthy While Taking Xalkori?

Xalkori can be an important medication to help treat your cancer. It's essential to take Xalkori as prescribed. If you experience any side effects, notify your healthcare provider to discuss how to treat them. Don't be afraid to report side effects out of fear your medication may be discontinued, especially if it is helping to treat your cancer. Sometimes a dose reduction is needed to manage side effects while you continue treatment.

Medical Disclaimer

5 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. U.S. Food and Drug Administration. Xalkori label.

  2. Sahu A, Prabhash K, Noronha V, et al. Crizotinib: a comprehensive review. South Asian J Cancer. 2013;2(2):91-7. doi:10.4103/2278-330X.110506

  3. Rothenstein JM, Letarte N. Managing treatment-related adverse events associated with Alk inhibitors. Curr Oncol. 2014 ;21(1):19-26. doi:10.3747/co.21.1740

  4. Prescribers' Digital Reference. Crizotinib - drug summary.

  5. American Cancer Society. Targeted drug therapy for non-small cell lung cancer.

By Julie Scott, MSN, ANP-BC, AOCNP
Julie is an Adult Nurse Practitioner with oncology certification and a healthcare freelance writer with an interest in educating patients and the healthcare community.