Crizotinib | Xalkori

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side effects
tests to perform
Dosing Guidelines
additional resources

Timeline of Crizotinib side effects:

A timeline infographic illustrating various side effects of crizotinib and their onset and incidence rates, including nausea and vomiting, bradycardia, constipation, peripheral neuropathy, vision disorders, diarrhea, and hepatotoxicity.

Other Crizotinib side effects:

A medical infographic showing the incidence rates of various side effects of crizotinib including: edema, fatigue, pneumonia/ILD, neutropenia & leukopenia, and cardiac events with respective symbols and percentages.

Tests to perform before starting treatment:

Vial of blood and magnifying glass examining it.
    • Serum levels of calcium, potassium, and magnesium.

    • Creatinine levels.

    • ALT, AST, and bilirubin (liver function test).

    • Complete blood test with differential wbc count.

Digital illustration of a human eye with a green iris, black pupil, surrounded by pink eyelid and eye skin.
  • Record vision status.

    Vision disorder are common when taking crizotinib. Discuss possible symptoms with patients: most commonly visual impairment, photopsia, blurred vision, and vitreous floaters.

Blood pressure cuff used to measure blood pressure.
    • ECG: check for bradycardia and QTc prolongation.

    • Take baseline heart rate and blood pressure.

A health monitoring timeline chart showing blood test and checkup schedule over 8 weeks, divided into two months, with progressive testing and monitoring instructions.

Tests to perform during treatment:

General dose guidelines:

illustration of a medication bottle labeled 250 mg, to be taken twice a day.
  • Recommended starting dose: 250mg 2x/ day

    Can be taken with or without food (avoid grapefruit products- CYP3A inhibitor, and St. John’s wort- CYP3A inducer).

    Medication should be taken at the same time each day.

    Tablets should be swallowed whole, do not use if compromised (broken, cracked, etc.).

A medication bottle with a label indicating 200mg dosage taken twice a day. An arrow labeled '1st reduction' points downward from the bottle.
  • First reduction: 200mg 2x/day

    Confirm condition does not fall under specific dose reductions.

A medicine bottle labeled 250mg taken once daily, with a pink arrow indicating a second reduction dose, showing a decreased dosage.
  • Second reduction: 250mg 1x/day

    Confirm condition does not fall under specific dose reductions.

A red circle with a diagonal line through it, indicating a prohibition or 'no' symbol.
  • Discontinue if patient cannot tolerate 250mg 1x/day.

Specific dose guidelines:

Red blood drop icon on white background.
  • Grade 3: withhold until recovered to grade 2 then resume same dose.

    Grade 4: withhold until recovered to grade 2 then resume lower dose.

Illustration of a human liver in brown color on a white background.
  • Non-hematologic toxicity:

    • Grade 3 or 4 ALT/AST elevation with less than grade 1 total bilirubin: withhold until recovery then resume at lower dose.

    • Grade 2/3/4 ALT/AST elevation with grade 2/3/4 total bilirubin: permanently discontinue.

    Hepatic impairment”

    • Moderate impairment: 200mg 2x/day.

    • Severe impairment: 250mg 1x/ day.

Illustration of two kidneys with their connecting ureters.
  • Severe not requiring peritoneal dialysis or hemodialysis: 250mg 1x/ day.

Pink heart with an electrocardiogram line running through it.
  • Grade 2 or 3: withhold until recovery and investigate concomitant medication.

    Grade 4: permanently discontinue if no concomitant medication is found.

A minimalist digital illustration of a human eye with a green iris surrounded by pink skin.
  • Discontinue during evaluation of severe vision loss.

Illustration of an electrocardiogram (ECG) waveform with a blue highlighted area behind it indicating the QT interval.
  • Grade 3: withhold until recovery then resume lower dose.

    Grade 4: permanently discontinue.

Crizotinib Monograph

Additional resources:

Crizotinib significantly prolongs progression-free survival compared to chemotherapy

Crizotinib was the first ALKi developed and was established as a superior treatment to standard first-line chemotherapy in delaying disease progression.

First-Line Crizotinib versus Chemotherapy in ALK-Positive Lung Cancer

CNS activity with crizotinib

CNS penetration and intracranial efficacy are more limited than later-generation ALK inhibitors.

Alectinib versus Crizotinib in Untreated ALK-Positive Non–Small-Cell Lung Cancer
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