Crizotinib

What is Crizotinib?

• Crizotinib (Xalkori) is a kinase inhibitor used to treat Anaplastic large cell lymphoma, Non-small cell lung cancer that is ALK positive or ROS1 positive and has metastasized (spread to other parts of the body).

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Crizotinib structure

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Crizotinib-Structural Formula V1

What are the uses of this medicine?

Crizotinib (Xalkori) to treat:

• Anaplastic large cell lymphoma that is ALK positive and systemic. It is used in children aged 1 year and older and young adults with relapsed or refractory disease.
• Non-small cell lung cancer that is ALK positive or ROS1 positive and has metastasized (spread to other parts of the body).

How does this medicine work?

• Crizotinib (kriz oh’ ti nib) is an orally available, small molecule inhibitor of the tyrosine kinase receptor of mutated anaplastic lymphoma kinase (ALK), which is the result of a chromosomal translocation found in about 5% of lung cancers.
• Patients with non-small cell lung cancer with the ALK mutation often respond to crizotinib therapy with shrinkage of the tumor and apparent improvement in survival.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

• Concomitant use of crizotinib with strong CYP3A inhibitors increases crizotinib plasma concentrations, which may increase the risk of adverse reactions of Xalkori. Avoid concomitant use of strong CYP3A inhibitors.
• Concomitant use of crizotinib with strong CYP3A inducers decreases crizotinib plasma concentrations, which may decrease the efficacy of Xalkori. Avoid concomitant use of strong CYP3A inducers.
• Avoid concomitant use of Xalkori with CYP3A substrates where minimal concentration changes may lead to serious adverse reactions.
• Xalkori can prolong the QT/QTc interval. Avoid concomitant use of Xalkori with drugs that prolong the QT interval.
• Concomitant use of Xalkori with drugs that cause bradycardia (e.g., beta-blockers, non-dihydropyridine calcium channel blockers, clonidine, and digoxin).

Is this medicine FDA approved?

• On August 24, 2011, the U.S. Food and Drug Administration approved crizotinib to treat certain late-stage (locally advanced or metastatic) non-small cell lung cancers that express the abnormal anaplastic lymphoma kinase (ALK) gene. Approval required a companion molecular test for the EML4-ALK fusion.
• In March 2016, the U.S. Food and Drug Administration approved crizotinib in ROS1-positive non-small cell lung cancer.

How should this medicine be used?

• Select patients for the treatment of metastatic NSCLC with Xalkori based on the presence of ALK or ROS1 positivity in tumor specimens.

Recommended dosage:

• Recommended Dosage for ALK- or ROS1-Positive Metastatic Non-Small Cell Lung Cancer:
• The recommended dosage is 250 mg orally twice daily.

Recommended Dosage for Relapsed or Refractory, Systemic ALK-Positive Anaplastic Large Cell Lymphoma:

• The recommended dosage of Xalkori for patients with ALCL is 280 mg/m2 orally twice daily until disease progression or unacceptable toxicity.

• Antiemetics are recommended prior to and during treatment with Xalkori to prevent nausea and vomiting.
• Consider intravenous or oral hydration for patients at risk of dehydration, and replace electrolytes as clinically indicated

Administration:

• Xalkori should be taken exactly as prescribed by your healthcare provider.
• Xalkori capsules should be swallowed whole.
• Xalkori may be taken with or without food.
• Your healthcare provider may change your dose, temporarily stop, or permanently stop treatment with Xalkori if you have certain side effects. Do not change the dose or stop treatment with Xalkori unless your healthcare provider tells you to.
• If a dose of Xalkori 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 Xalkori, do not take an extra dose. The next dose should be taken at the regular time.
• Xalkori should be given to children under adult supervision.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Capsules: 250 mg, 200 mg.

This medicine is available in fallowing brand namesː

• Xalkori

What side effects can this medication cause?

The most common side effects of this medicine include: The most common side effects of Xalkori in people with NSCLC include:

• vision problems
• nausea, diarrhea, or vomiting
• swelling of your hands, feet, face, and eyes
• constipation
• increased liver function blood tests
• tiredness
• decreased appetite
• upper respiratory infection
• dizziness
• feeling of numbness or tingling in your arms or legs

The most common side effects of Xalkori in people with ALCL include:

• diarrhea, vomiting, or nausea
• vision problems
• headache
• muscle and joint pain
• mouth sores
• tiredness
• decreased appetite
• fever
• stomach-area (abdominal) pain
• cough
• itchy skin
• low blood counts
• abnormal liver tests
• low levels of electrolytes
• abnormal kidney tests
• low and high blood sugar levels

• Xalkori may cause fertility problems in females and males, which may affect the ability to have children.

Xalkori may cause serious side effects, including:

• Liver problems
• pneumonitis
• Heart problems
• Severe vision problems
• Severe stomach, intestine, and mouth (gastrointestinal) problems in people with ALCL

What special precautions should I follow?

• Fatal hepatotoxicity has occurred. Monitor with periodic liver testing. Temporarily suspend, dose reduce, or permanently discontinue Xalkori.
• Severe, life-threatening, or fatal interstitial lung disease (ILD)/pneumonitis can occur in patients treated with Xalkori. Permanently discontinue in patients with ILD/pneumonitis.
• QTc prolongation can occur in patients treated with Xalkori. Monitor electrocardiograms and electrolytes in patients who have a history of or predisposition for QTc prolongation, or who are taking medications that prolong QT. Temporarily suspend, dose reduce, or permanently discontinue Xalkori.
• Symptomatic bradycardia can occur in patients receiving Xalkori. Monitor heart rate and blood pressure regularly. Temporarily suspend, dose reduce, or permanently discontinue Xalkori.
• Xalkori can cause visual changes including severe visual loss. Discontinue Xalkori in patients with severe visual loss. Monitor and evaluate for ocular toxicity throughout treatment.
• Xalkori can cause severe nausea, vomiting, diarrhea, and stomatitis. Provide standard antiemetic and antidiarrheal agents. Temporarily suspend, dose reduce, or permanently discontinue Xalkori.
• Xalkori Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and use of effective contraception.

What to do in case of emergency/overdose?

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on findings from animal studies and its mechanism of action, Xalkori can cause fetal harm when administered to a pregnant woman.
• There are no available data on the use of Xalkori during pregnancy.

Can this medicine be used in children?

• The safety and effectiveness of Xalkori have been established in pediatric patients 12 months of age and older with relapsed or refractory, systemic ALK-positive ALCL.
• The safety and effectiveness have not been established in pediatric patients younger than 12 months of age with ALCL or in any pediatric patients with NSCLC.

What are the active and inactive ingredients in this medicine?

• Active ingredient: crizotinib
• Inactive ingredients: colloidal silicon dioxide, microcrystalline cellulose, anhydrous dibasic calcium phosphate, sodium starch glycolate, and magnesium stearate.
• Pink opaque capsule shell contains: gelatin, titanium dioxide, and red iron oxide.
• White opaque capsule shell contains: gelatin and titanium dioxide.
• Printing ink contains: shellac, propylene glycol, strong ammonia solution, potassium hydroxide, and black iron oxide.

Who manufactures and distributes this medicine?

• Packager: Pfizer Laboratories Div Pfizer Inc

What should I know about storage and disposal of this medication?

• Store Xalkori at room temperature between 68°F to 77°F (20°C to 25°C).

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• Dailymed label info on Crizotinib
• FDA Crizotinib

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