Chemical: Drug
crizotinib

PharmGKB contains no dosing guidelines for this . To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.


Annotated Labels

  1. FDA Label for crizotinib and ALK
  2. EMA Label for crizotinib and ALK
  3. PMDA Label for crizotinib and ALK
  4. HCSC Label for crizotinib and ALK

last updated 10/25/2013

1. FDA Label for crizotinib and ALK

Genetic testing required

Summary

The drug label for crizotinib (XALKORI) states that detection of ALK-positive non-small cell lung cancer (NSCLC) using an FDA-approved test is necessary for selection of patients for treatment with the drug, as it is only indicated for use in these patients.

There's more of this label. Read more.


last updated 10/25/2013

2. EMA Label for crizotinib and ALK

Genetic testing required

Summary

The EMA European Public Assessment Report (EPAR) requires testing of ALK prior to treatment with crizotinib, indicated for patients with ALK-positive advanced non-small cell lung cancer.

There's more of this label. Read more.


last updated 01/26/2015

3. PMDA Label for crizotinib and ALK

Genetic testing required

Summary

The PMDA package insert for crizotinib states that it is indicated for individuals with anaplastic lymphoma kinase (ALK)-positive non-small-cell lung cancer (NSCLC).

There's more of this label. Read more.


last updated 06/08/2015

4. HCSC Label for crizotinib and ALK

Genetic testing required

Summary

The product monograph for crizotinib (XALKORI) states that it is indicated for patients with anaplastic lymphoma kinase (ALK)-positive locally advanced or metastatic non-small cell lung cancer.

There's more of this label. Read more.


PharmGKB contains no Clinical Variants that meet the highest level of criteria.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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Overview

Generic Names
  • crizotinib
Trade Names
  • Xalkori
Brand Mixture Names

PharmGKB Accession Id

PA165946122

Type(s):

Drug

Description

Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON).

Source: PharmGKB

Indication

Crizotinib is indicated for the treatment of ALK-positive Non-Small-Cell Lung Carcinoma (NSCLC).

Source: PharmGKB

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Chemical Properties

Chemical Formula

C21H22Cl2FN5O

Source: PubChem Compound

Canonical SMILES

C[C@H](C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N

Source: PubChem Compound

Average Molecular Weight

450.336683

Source: PubChem Compound

Monoisotopic Molecular Weight

449.118544

Source: PubChem Compound

IUPAC Names

  • 3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ALK [PMID: 26654422] (source: PharmGKB)
No related drugs are available.

Curated Information ?

Publications related to crizotinib: 12

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenomics in the treatment of lung cancer: an update. Pharmacogenomics. 2015. Morales-Espinosa Daniela, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Novel targeted therapies for resistant ALK-rearranged non-small-cell lung cancer: ceritinib and beyond. OncoTargets and therapy. 2015. Kanaan Zeyad, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
EMA Initiatives and Perspectives on Pharmacogenomics. British journal of clinical pharmacology. 2014. Ehmann Falk, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Clinical Implementation of Germline Cancer Pharmacogenetic Variants during the Next-Generation Sequencing Era. Clinical pharmacology and therapeutics. 2013. Gillis Nancy K, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Challenges in pharmacogenetics. European journal of clinical pharmacology. 2013. Cascorbi Ingolf, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics and pharmacogenomics: a bridge to individualized cancer therapy. Pharmacogenomics. 2013. Weng Liming, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics and pharmacogenomics: role of mutational analysis in anti-cancer targeted therapy. The pharmacogenomics journal. 2012. Savonarola A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ROS1 as a 'druggable' receptor tyrosine kinase: lessons learned from inhibiting the ALK pathway. Expert review of anticancer therapy. 2012. Ou Sai-Hong Ignatius, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2012. Doebele Robert C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen. Chemical biology & drug design. 2011. Zhang Sen, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
ALK mutations conferring differential resistance to structurally diverse ALK inhibitors. Clinical cancer research : an official journal of the American Association for Cancer Research. 2011. Heuckmann Johannes M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Crizotinib: a novel and first-in-class multitargeted tyrosine kinase inhibitor for the treatment of anaplastic lymphoma kinase rearranged non-small cell lung cancer and beyond. Drug design, development and therapy. 2011. Ou Sai-Hong Ignatius. PubMed

LinkOuts

PubChem Compound:
11626560

Clinical Trials

These are trials that mention crizotinib and are related to either pharmacogenetics or pharmacogenomics.

No trials loaded.

NURSA Datasets

provided by nursa.org

No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.