Crizotinib

XALKORI

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Pronunciation: kriz-OE-ti-nib (zal-KOR-ee)

Crizotinib ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Crizotinib ballicule

Crizotinib XALKORI mascot mnemonic cartoon — Visual mnemonic: Crizotinib mascot
**“Al Gore, Crispy tiny nibbler”**

What it isALK and ROS1 tyrosine kinase inhibitor; ALK- or ROS1-positive lung cancer.

Why this oneIt was the first ALK inhibitor and remains an option in ROS1 disease.

What limits itPoor CNS penetration, so brain relapse is common and later agents replaced it. Visual disturbance, edema and hepatotoxicity.

Crizotinib molecular structure (skeletal formula) — Molecular structure: Crizotinib

Crizotinib prescription history

Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Crizotinib enters in 2011 (estimated).

FDA-approved for

ALK- or ROS1-positive non-small cell lung cancer (2011)

Principal riskPoor CNS penetration, so brain relapse is common

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades2 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
ALK- or ROS1-positive metastatic NSCLC	Adults	250 mg BID	250 mg BID	250 mg BID
Relapsed/refractory systemic ALK-positive ALCL	Peds ≥1 yr & young adults	280 mg/m2 BID via BSA table (capsules or pellets): 0.38–0.46 m2 120 mg; 0.47–0.51 140 mg; 0.52–0.61 150 mg; 0.62–0.80 200 mg; 0.81–0.97 250 mg; 0.98–1.16 300 mg; 1.17–1.33 350 mg; 1.34–1.51 400 mg; 1.52–1.69 450 mg; ≥1.7 m2 500 mg — all BID (Table 2)	Same BSA-band dose until progression or unacceptable toxicity; reductions per Table 5	500 mg BID (BSA ≥1.7 m2)
Unresectable/recurrent/refractory ALK-positive IMT	Adults	250 mg BID	250 mg BID	250 mg BID
Unresectable/recurrent/refractory ALK-positive IMT	Peds ≥1 yr	280 mg/m2 BID via BSA table (capsules or pellets): 0.38–0.46 m2 120 mg; 0.47–0.51 140 mg; 0.52–0.61 150 mg; 0.62–0.80 200 mg; 0.81–0.97 250 mg; 0.98–1.16 300 mg; 1.17–1.33 350 mg; 1.34–1.51 400 mg; 1.52–1.69 450 mg; ≥1.7 m2 500 mg — all BID (Table 3)	Same BSA-band dose until progression or unacceptable toxicity; reductions per Table 5	500 mg BID (BSA ≥1.7 m2)

Renal Severe renal impairment: reduce dose (see label section 2.8)

Hepatic Moderate or severe hepatic impairment: reduce dose (see label section 2.7)

Instructions

Select patients by ALK or ROS1 positivity in tumor specimens
Monitor LFTs every 2 weeks for first 2 months then monthly; monitor CBC weekly for first month then monthly
Obtain baseline and follow-up ophthalmologic/retinal exams in pediatric ALCL/IMT within 1 month then every 3 months

Available strengths

cap 20, 50, 150, 200, 250 mg

Cautions

Hepatotoxicity, including fatal — monitor with periodic liver testing
Interstitial lung disease/pneumonitis — permanently discontinue
QT interval prolongation — monitor ECG and electrolytes
Bradycardia — monitor heart rate and blood pressure
Severe visual loss — discontinue if it occurs
GI toxicity (nausea, vomiting, diarrhea, stomatitis) in pediatric/young adult ALCL and pediatric IMT
Embryo-fetal toxicity

Adverse reactions

Vision disorders
Nausea, diarrhea, vomiting, constipation
Edema
Elevated transaminases
Fatigue, decreased appetite, dizziness, neuropathy
(ALCL) neutropenia, lymphopenia, thrombocytopenia

Pregnancy Can cause fetal harm; embryotoxicity/fetotoxicity in animals; advise effective contraception

Lactation No data; advise not to breastfeed during treatment and for 45 days after last dose

Cost

Crizotinib (XALKORI)

Strength		#/mo	CostPlus
20 mg	cap	60 BID	not offered
50 mg	cap	60 BID	not offered
150 mg	cap	60 BID	not offered
200 mg	cap	60 BID	not offered
250 mg	cap	60 BID	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Crizotinib is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2029 est.

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