pharmacopeia
GET
/api/v1/drug/crizotinib

Mechanism of action

Sourced from openFDA

Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins.

Cytochrome P450 2B6Cytochrome P450 3AOrganic Cation Transporter 1Organic Cation Transporter 2P-GlycoproteinReceptor Tyrosine Kinase

Indications

Sourced from openFDA
  • XALKORI is a kinase inhibitor indicated for the treatment of • adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK) or ROS1-positive as detected by an FDA-approved test. ( 1.1 , 2.1 ) • pediatric patients 1 year of age and older and young adults with relapsed or refractory, systemic anaplastic large cell lymphoma (ALCL) that is ALK-positive.ICD-10: C34.90, C85.90

Contraindications

Sourced from openFDA
  • None. None.contraindicated

Dosage & administration

Sourced from openFDA

• Metastatic NSCLC: The recommended dosage is 250 mg orally twice daily. ( 2.3 ) • Systemic ALCL: The recommended dosage is 280 mg/m 2 orally twice daily based on body surface area. ( 2.3 ) • Unresectable IMT: o Adult: The recommended dosage is 250 mg orally twice daily. ( 2.3 ) o Pediatric: The recommended dosage is 280 mg/m 2 orally twice daily based on body surface area. ( 2.3 ) • See full prescribing information for dosage adjustments by indication for patients with moderate or severe hepatic impairment or severe renal impairment. ( 2.7 , 2.8 ) 2.1 Patient Selection Select patients for the treatment of metastatic NSCLC with XALKORI based on the presence of ALK or ROS1 positivity in tumor specimens [see Clinical Studies (14.1 , 14.2 , 14.3) ] . Information on FDA-approved tests for the detection of ALK and ROS1 rearrangements in NSCLC is available at http://www.fda.gov/companiondiagnostics . 2.2 Recommended Testing During Treatment with XALKORI • Monitor liver function tests, including alanine aminotransferase (ALT), aspartate aminotransferase (AST), and total bilirubin, every 2 weeks during the first 2 months of treatment, then once a month, and as clinically indicated, with more frequent repeat testing for increased liver transaminases, alkaline phosphatase, or total bilirubin in patients who develop increased transaminases [see Warnings and Precautions (5.1) ] .

Warnings & precautions

Sourced from openFDA

• Hepatotoxicity: Fatal hepatotoxicity has occurred. Monitor with periodic liver testing. Temporarily suspend, dose reduce, or permanently discontinue XALKORI. ( 2.2 , 2.6 , 5.1 ) • Interstitial Lung Disease (ILD)/Pneumonitis: Permanently discontinue in patients with ILD/pneumonitis. ( 2.6 , 5.2 ) • QT Interval Prolongation: 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. ( 2.6 , 5.3 ) • Bradycardia: XALKORI can cause bradycardia. Monitor heart rate and blood pressure regularly. Temporarily suspend, dose reduce, or permanently discontinue XALKORI. ( 2.6 , 5.4 ) • Severe Visual Loss: XALKORI can cause visual changes including severe visual loss. Monitor and evaluate for ocular toxicity throughout treatment. Discontinue XALKORI in patients with severe visual loss. ( 2.2 , 2.6 , 5.5 ) • Gastrointestinal Toxicity in Pediatric and Young Adult Patients with ALCL or Pediatric Patients with IMT: XALKORI can cause severe nausea, vomiting, diarrhea, and stomatitis. Provide standard antiemetic and antidiarrheal agents. Temporarily suspend, dose reduce, or permanently discontinue XALKORI. ( 2.6 , 5.6 ) • Embryo-Fetal Toxicity: Can cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and use of effective contraception.

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: • Hepatotoxicity [see Warnings and Precautions (5.1) ] • Interstitial Lung Disease/Pneumonitis [see Warnings and Precautions (5.2) ] • QT Interval Prolongation [see Warnings and Precautions (5.3) ] • Bradycardia [see Warnings and Precautions (5.4) ] • Severe Visual Loss [see Warnings and Precautions (5.5) ] • Gastrointestinal Toxicity in Pediatric and Young Adult Patients with ALCL or Pediatric Patients with IMT [see Warnings and Precautions (5.6) ] The most common adverse reactions (≥25%) in adult patients with NSCLC are vision disorders, nausea, diarrhea, vomiting, edema, constipation, elevated transaminases, fatigue, decreased appetite, upper respiratory infection, dizziness, and neuropathy. ( 6.1 ) The most common adverse reactions (≥35%) in patients with ALCL are diarrhea, vomiting, nausea, vision disorder, headache, musculoskeletal pain, stomatitis, fatigue, decreased appetite, pyrexia, abdominal pain, cough, and pruritus. Grade 3–4 laboratory abnormalities (≥15%) are neutropenia, lymphopenia, and thrombocytopenia. ( 6.1 ) The most common adverse reactions (≥35%) in adult patients with IMT are vision disorders, nausea, and edema. ( 6.1 ) The most common adverse reactions (≥35%) in pediatric patients with IMT are vomiting, nausea, diarrhea, abdominal pain, rash, vision disorder, upper respiratory tract infection, cough, pyrexia, musculoskeletal pain, fatigue, edema, constipation, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc.

Use in specific populations

Sourced from openFDA

Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action, XALKORI can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology (12.1) ] . There are no available data on the use of XALKORI in pregnant women. In animal reproduction studies, oral administration of crizotinib to pregnant rats during organogenesis at exposures similar to those expected with the maximum recommended human dose resulted in embryotoxicity and fetotoxicity (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data Crizotinib was administered to pregnant rats and rabbits during organogenesis to study the effects on embryo-fetal development. Postimplantation loss was increased at doses ≥50 mg/kg/day (approximately 0.6 times the recommended human dose based on AUC) in rats.

Pharmacokinetics

Sourced from openFDA
Metabolism
Following XALKORI 250 mg capsules twice daily, steady-state was reached within 15 days with a median accumulation ratio of 4.8. Steady-state minimum concentration (C min.ss ) and AUC increased in a greater than dose-proportional manner over the dose range of 200 mg to 300 mg twice daily (0.8 to 1.2 times the approved recommended dosage).

Approval history

Sourced from openFDA
  • Aug 26, 2011NDANDA202570Pf Prism Cv
  • Sep 7, 2023NDANDA217581Pf Prism Cv

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
12,556 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death2,29718%
  2. 2Disease Progression1,2159.7%
  3. 3Nausea1,1148.9%
  4. 4Neoplasm Progression1,1128.9%
  5. 5Diarrhoea8436.7%
  6. 6Vomiting7906.3%
  7. 7Fatigue5534.4%
  8. 8Off Label Use4693.7%
  9. 9Oedema Peripheral4433.5%
  10. 10Constipation4393.5%
  11. 11Dyspnoea4283.4%
  12. 12Lung Neoplasm Malignant4183.3%
  13. 13Visual Impairment4043.2%
  14. 14Decreased Appetite3783.0%
  15. 15Asthenia3392.7%

Literature

View JSON

Recent PubMed references pinned to Crizotinib as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

View JSON

The 10 most recently updated of 171 ClinicalTrials.gov registrations naming Crizotinib as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Crizotinib work?
Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d'Origine Nantais (RON). Translocations can affect the ALK gene resulting in the expression of oncogenic fusion proteins.
What is Crizotinib used for?
According to FDA labeling, Crizotinib carries indications including: XALKORI is a kinase inhibitor indicated for the treatment of • adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK) or ROS1-positive as detected by an FDA-approved test. ( 1.1 , 2.1 ) • pediatric patients 1 year of age and older and young adults with relapsed or refractory, systemic anaplastic large cell lymphoma (ALCL) that is ALK-positive.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Crizotinib?
Crizotinib is classified as Anaplastic lymphoma kinase (ALK) inhibitors, Kinase Inhibitor, Cytochrome P450 2B6 Inhibitors, Cytochrome P450 3A Inhibitors, Organic Cation Transporter 1 Inhibitors, Organic Cation Transporter 2 Inhibitors, P-Glycoprotein Inhibitors, Receptor Tyrosine Kinase Inhibitors, Cellular Proliferation Alteration.
What are the brand names for Crizotinib?
Crizotinib is marketed under brand names including Xalkori.
What are the contraindications for Crizotinib?
Crizotinib labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.
Note. Data for crizotinib is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients