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Crizotinib

Class
Targeted therapy
Subclass
Tyrosine kinase inhibitors
Generic name
Crizotinib
Brand names
Xalkori®
Common formulations
Capsule
Dosage and administration
Adults patients
Inflammatory myofibroblastic tumor in patients with ALK gene fusion, NPM-ALK fusion protein • Unresectable or recurrent or refractory
•
250 mg PO BID a duration until disease progression or unacceptable toxicity
Non-small cell lung cancer in patients with ALK gene fusion, NPM-ALK fusion protein, ROS1 gene fusion, ROS1 fusion protein • Metastatic
•
250 mg PO BID a duration until disease progression or unacceptable toxicity
Indications for use
Labeled indications
Adults
•
Treatment of inflammatory myofibroblastic tumor in patients with ALK gene fusion, NPM-ALK fusion protein (unresectable or recurrent or refractory)
•
Treatment of non-small cell lung cancer in patients with ALK gene fusion, NPM-ALK fusion protein, ROS1 gene fusion, ROS1 fusion protein (metastatic)
Safety risks
Boxed warnings
Gastrointestinal disorders
•
Use extreme caution with anaplastic large-cell lymphoma and with inflammatory myofibroblastic tumor.
Hematologic disorder
•
Use extreme caution with anaplastic large-cell lymphoma.
ILD
•
Use extreme caution with a history of pulmonary disease.
Contraindications
Who have congenital long QT syndrome
Warnings and precautions
Abnormal LFTs
•
Use caution with pre-existing hepatic disease.
Sudden vision loss
•
Use caution with pre-existing ocular disease.
Specific populations
Renal impairment
eGFR 30-50 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required. Monitor for hepatotoxicity.
eGFR 10-30 mL/min/1.73 m²
•
Use with caution. Start at dose of 250 mg once daily. Maximal dose of 200 mg BID. Titrate to response. Monitor for hepatotoxicity.
eGFR < 10 mL/min/1.73 m²
•
Use with caution. Start at dose of 250 mg once daily. Maximal dose of 200 mg BID. Titrate to response. Monitor for hepatotoxicity.
Renal replacement therapy
Continuous renal replacement
•
Reduce dose. Dose as in eGFR 10-30 mL/min/1.73 m². Start at a dose of 250 mg once daily. Maximal dose of 200 mg BID. Titrate to response. Monitor for hepatotoxicity.
Intermittent hemodialysis
•
Reduce dose. Dose as in eGFR < 10 mL/min/1.73 m². Start at a dose of 250 mg once daily. Maximal dose of 200 mg BID. Titrate to response. Monitor for hepatotoxicity.
Peritoneal dialysis
•
Reduce dose. Dose as in eGFR < 10 mL/min/1.73 m². Start at a dose of 250 mg once daily. Maximal dose of 200 mg BID. Titrate to response. Monitor for hepatotoxicity.
Hepatic impairment
Child-Pugh A (mild)
•
Use acceptable. No dose adjustment required. Monitor serum concentrations. Monitor serum aminotransferases. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=2a51b0de-47d6-455e-a94c-d2c737b04ff7.
Child-Pugh B (moderate)
•
Reduce dose by 80%. Start at dose of 200mg BID. Maximal dose of 400 mg per day. Do not exceed frequency of BID. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=2a51b0de-47d6-455e-a94c-d2c737b04ff7.
Child-Pugh C (severe)
•
Reduce dose by 50%. Start at dose of 250 mg once daily. Maximal dose of 250 mg per day. Do not exceed frequency of daily. Monitor serum aminotransferases. Monitor for toxicity. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=2a51b0de-47d6-455e-a94c-d2c737b04ff7#S12.3.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: D
•
Avoid use. Evidence of fetal harm in humans. This drug can harm a developing fetus.
•
Verify the pregnancy status of females of reproductive potential prior to initiating treatment.
•
Females of reproductive potential should use effective contraception during therapy and for at least 45 days after the last dose.
•
Because of the potential for genotoxicity, males with female partners of reproductive potential should use condoms during therapy and for at least 90 days after the last dose.
Breastfeeding
Little information available on breastfeeding safety.
•
Do not use during breastfeeding.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
Adverse reactions
Very common > 10%
•
↓ blood glucose, ↓ blood lymphocyte count, ↓ blood neutrophil count, ↓ platelet count, ↓ serum magnesium, ↓ serum sodium, dysgeusia, hypertension, hypoalbuminemia, ↑ blood glucose, ↑ liver enzymes, ↑ serum potassium, ↑ serum sodium, ↑ serum uric acid, peripheral neuropathy, abdominal pain, cough, diarrhea, fatigue, fever, itching, loss of appetite, musculoskeletal pain
Common 1-10%
•
Acute liver failure, anemia, bradycardia, ↓ serum calcium, ↓ serum phosphate, ↓ serum potassium, esophagitis, hypotension, interstitial lung disease, pulmonary embolism, ↑QTc interval, constipation, dizziness, dysphagia, dyspnea, headache, muscle cramps, nausea, syncope, visual disturbances, vomiting, weakness, weight gain, weight loss, stomatitis
Uncommon < 1%
•
Optic neuritis
Unknown frequency
•
Acute respiratory distress syndrome, diabetic ketoacidosis, laryngitis, maculopapular rash, nephrotoxicity, optic atrophy, peripheral edema, pharyngitis, arthralgia, back pain, blurred vision, diplopia, dysesthesia, hypoesthesia, myalgia, paresthesia, photophobia, photopsia, sinusitis
Interactions
Drug(s)
Check Interactions
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