Chemical: Drug
crizotinib
PharmGKB contains no prescribing info for this . Contact us to report known genotype-based dosing guidelines, or if you are interested in developing guidelines.
Annotated Labels
- Annotation of FDA Label for crizotinib and ALK,ROS1
- Annotation of EMA Label for crizotinib and ALK
- Annotation of PMDA Label for crizotinib and ALK
- Annotation of HCSC Label for crizotinib and ALK
1. Annotation of FDA Label for crizotinib and ALK,ROS1
Summary
The FDA-approved drug label for crizotinib (XALKORI) states that it is indicated for treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are ALK-positive as detected by an FDA-approved test, and for patients with metastatic NSCLC whose tumors are ROS1-positive.
There's more of this label. Read more.
2. Annotation of EMA Label for crizotinib and ALK
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.
3. Annotation of PMDA Label for crizotinib and ALK
Summary
Crizotinib is indicated for the treatment of patients with non-small cell lung cancer. The PMDA package insert for crizotinib states positive confirmation of the ALK fusion gene is necessary prior to treatment.
There's more of this label. Read more.
4. Annotation of HCSC Label for crizotinib and ALK
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.
The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.
The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.
Links in the "Gene" column lead to PharmGKB Gene Pages.
List of all variant annotations for crizotinib
| Gene ? |
Variant?
(147) |
Alternate Names ? | Chemicals ? |
Alleles
?
(+ chr strand) |
Function ? |
Amino Acid?
Translation |
|
|---|---|---|---|---|---|---|---|
VA
|
ABCB1 | *2 (PMID: 11503014) | N/A | N/A | N/A |
Overview
- crizotinib
- Xalkori
PharmGKB Accession Id
PA165946122
Type(s):
Drug
Metabolite(s):
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) and ROS1-positive NSCLC.
Source: PharmGKB [Article:27328934] [Article:23386065]
Other Vocabularies
- ATC: Protein kinase inhibitors (L01XE)
- UMLS: crizotinib (C2974289)
- RxNorm: crizotinib (1148495)
- NDFRT: CRIZOTINIB (N0000183253)
Information pulled from DrugBank has not been reviewed by PharmGKB.
Chemical Properties
Canonical SMILES
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 ?
| Evidence | Gene |
|---|---|
| ABCB1 | |
| ALK | |
| CYP1A2 | |
| CYP2B6 | |
| CYP2C19 | |
| CYP2C8 | |
| CYP2C9 | |
| CYP2D6 | |
| CYP3A | |
| CYP3A4 | |
| CYP3A5 | |
|
|
MET |
| ROS1 | |
| SLCO1B1 | |
| SLCO1B3 |
Drug Targets
| Gene | Description |
|---|---|
| ALK | [PMID: 26654422] (source: PharmGKB ) |
| ROS1 | [PMID: 27328934] (source: PharmGKB ) |
Curated Information ?
| Evidence | Disease |
|---|---|
|
|
Bradycardia |
|
|
Carcinoma, Non-Small-Cell Lung |
|
|
Nausea |
|
|
Vision Disorders |
