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Crizotinib

Pronunciation: kriz-oh-tee-nib
Generic name: crizotinib
Brand name: Xalkori
Dosage form: oral capsule, oral pellets
Drug class: Multikinase inhibitors

Medically reviewed by Carmen Pope, BPharm. Last updated on Jan 22, 2024.

What is crizotinib?

Crizotinib (Xalkori) is an oral kinase inhibitor that may be used to treat:

Crizotinib works by blocking the effects of receptor tyrosine kinases (RTKs), such as ALK, hepatocyte growth factor receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d’Origine Nantais (RON). RTKs are essential components of signaling pathways that mediate cell-to-cell communication. Defects in RTKs can result in increased cell proliferation and survival in tumors expressing these proteins. Laboratory research has shown crizotinib-induced cell death and tumor regression in ALCL-derived cell lines that contained nucleophosmin-ALK or c-Met.

Crizotinib was FDA-approved on August 26, 2011. When it was approved, it was the first therapy to be approved for patients with ROS1-positive NSCLC.

Warnings

Crizotinib can cause serious heart, lung, or liver problems. Call your doctor at once if you have: fast or pounding heartbeats, sudden dizziness, shortness of breath, tiredness, itching, upper stomach pain, dark urine, clay-colored stools, or jaundice (yellowing of the skin or eyes).

Visual changes including severe visual loss have been reported with crizotinib. Your healthcare provider will monitor you for any vision changes; tell them right away if you experience any vision loss.

Crizotinib can cause severe nausea, vomiting, diarrhea, and mouth ulcers, especially in children or young adults. Your healthcare provider will monitor children for this, prescribe standard antidiarrheal or antiemetics, and review treatment if necessary.

Can harm an unborn baby. Do not take crizotinib if you are pregnant. Use effective birth control while you are using this medicine and for at least 3 months after your treatment ends, whether you are a man or a woman.

It is not known if Crizotinib is safe and effective in older adults with ALCL or children younger than 1 year of age with ALCL or IMT.

Before taking

Before taking crizotinib, tell your healthcare provider about all of your medical conditions, including if you:

This medicine may affect fertility (ability to have children) in both men and women. However, it is important to use birth control to prevent pregnancy because crizotinib can harm an unborn baby.

Pregnancy

Crizotinib can harm an unborn baby or cause birth defects if the mother or the father is using this medicine. You may need to have a negative pregnancy test before starting this treatment. If you are a woman, do not use crizotinib if you are pregnant. Use effective birth control to prevent pregnancy while you are using this medicine and for at least 45 days after your last dose. Tell your healthcare provider right away if you inadvertently become pregnant or think you might be pregnant during treatment.

Males who have female partners who can become pregnant should use condoms during treatment with crizotinib and for 90 days after the last dose.

Tell your doctor right away if a pregnancy occurs while either the mother or the father is using crizotinib.

Breastfeeding

It is not known if crizotinib passes into your breast milk. Do not breastfeed during treatment and for 45 days after the last dose. Talk to your healthcare provider about the best way to feed your baby during this time.

How should I take crizotinib?

Take crizotinib exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose.

Crizotinib is usually taken twice per day, with or without food. Crizotinib comes in capsules and oral pellets.

Your healthcare provider will check your blood cell counts weekly during the first month of treatment with crizotinib and then at least monthly during treatment.

What happens if I miss a dose?

If a dose of crizotinib is missed, it should be taken as soon as you remember. If it is close to the time of the next dose (within 6 hours), the missed dose should be skipped, and the next dose should be taken at the regular time.

If you vomit after taking a dose of crizotinib, do not take an extra dose. The next dose should be taken at the regular time.

Dosing information

The usual dosages are as follows. Your healthcare provider may adjust the dose based on your response or individual factors. Take the dose that they have prescribed.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if your next dose is due in less than 6 hours. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What to avoid

Grapefruit may interact with crizotinib and lead to unwanted side effects. Avoid the use of grapefruit products.

This medicine may cause blurred vision and may impair your reactions. Avoid driving or hazardous activity until you know how this medicine will affect you.

Crizotinib can pass into body fluids (urine, feces, vomit). Caregivers should wear rubber gloves while cleaning up a patient's body fluids, handling contaminated trash or laundry, or changing diapers. Wash hands before and after removing gloves. Wash soiled clothing and linens separately from other laundry.

Avoid spending prolonged time in sunlight. Crizotinib can make your skin sensitive to the sun (photosensitivity), and you may burn more easily. You should use sunscreen and wear protective clothing that covers your skin to help protect against sunburn if you have to be in the sunlight during treatment with crizotinib.

What are the side effects of crizotinib?

Get emergency medical help if you have signs of an allergic reaction to crizotinib: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Crizotinib may cause serious side effects, including:

Your healthcare provider may refer you to an eye specialist before starting crizotinib and within 1 month of starting it to check for vision problems. You should have an eye examination every 3 months during treatment and more often if there are any new vision problems.

Crizotinib may cause severe diarrhea, nausea, vomiting, or mouth sores. Tell your healthcare provider right away if problems with swallowing, vomiting, or diarrhea develop during treatment.

Call your doctor at once if you have:

Common crizotinib side effects may include:

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

What other drugs will affect crizotinib?

Sometimes it is not safe to use certain medications at the same time. Some drugs can affect your blood levels of other drugs you take, which may increase side effects or make the medications less effective. Medications that may interact with crizotinib include:

Crizotinib can cause serious heart problems. Your risk may be higher if you also use certain other medicines for infections, asthma, heart problems, high blood pressure, depression, mental illness, cancer, malaria, or HIV.

Not all possible interactions are listed here. Tell your doctor about all your current medicines and any medicine you start or stop using.

Storage

Store at room temperature 20° to 25°C (68° to 77°F); excursions permitted between 15° to 30°C (59° to 86°F).

Ingredients

Capsules

Active: crizotinib 200mg, 250mg

Inactive ingredients: colloidal silicon dioxide, microcrystalline cellulose, anhydrous dibasic calcium phosphate, sodium starch glycolate, magnesium stearate, and hard gelatin capsule shells.

Pink opaque capsule shell contains gelatin, titanium dioxide, and red iron oxide.

The white opaque capsule shell contains gelatin and titanium dioxide.

The printing ink contains shellac, propylene glycol, strong ammonia solution, potassium hydroxide, and black iron oxide.

Oral Pellets

Active: crizotinib 20mg, 50mg, 150mg

Inactive: The uncoated pellets contain poloxamer and stearyl alcohol. The film-coating contains hypromellose, glyceryl monostearate, medium-chain triglycerides, polyethylene glycol/macrogol, sucrose, and talc.

Manufacturer

Crizotinib is distributed under the brand name Xalkori by Pfizer Labs, Division of Pfizer Inc, NY, NY 10017.

Popular FAQ

We can estimate from graphs plotting progression-free survival that Xalkori starts to work within approximately 2 months, but most trials report on how long Xalkori keeps a person’s cancer from getting worse, not how quickly it works. This is called progression-free survival. Continue reading

Xalkori is pronounced “zal-KOR-ee”. Xalkori is the brand name product for crizotinib (pronounced “kriz OH ti nib”), the generic name of the drug. Continue reading

Xalkori treats three types of cancers with genetic mutations: non-small cell lung cancer (NSCLC), anaplastic large cell lymphoma (ALCL), a type of blood cancer, and (ALK)-positive inflammatory myofibroblastic tumors (IMT). Continue reading

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.