Crizotinib (Xalkori)

General information

Class/mechanism: Tyrosine kinase inhibitor; inhibits anaplastic lymphoma kinase (ALK), c-MET and subsequent expression of Hepatocyte Growth Factor Receptor (HGFR), and Recepteur d’Origine Nantais (RON). Inhibits activity of fusion proteins involving ALK, such as EML4-ALK and NPM-ALK.^[1]^[2]
Route: PO
Extravasation: n/a

For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.^[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Anaplastic large cell lymphoma, pediatric

2021-01-14: Approved for 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. (New disease entity; based on COG ADVL0912)

Inflammatory myofibroblastic tumor

2022-07-14: Approved for adult and pediatric patients 1 year of age and older with unresectable, recurrent, or refractory inflammatory anaplastic lymphoma kinase (ALK)-positive myofibroblastic tumors (IMT). (New disease entity; based on COG ADVL0912 & PROFILE 1013)

Non-small cell lung cancer

2011-08-26: Initial accelerated approval for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic lymphoma kinase (ALK)-positive. (Based on PROFILE 1001 ALK)
- 2013-11-20: Converted to full approval for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive. (Indication removed from locally advanced setting; based on PROFILE 1005, PROFILE 1007, PROFILE 1014)
2016-03-11: Approved for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are ROS1-positive. (New mutation-specific indication; based on PROFILE 1001 ROS1)

History of changes in EMA indication

2012-10-23: Initial marketing authorization as Xalkori.

History of changes in Health Canada indication

2012-04-25: Initial notice of compliance with conditions as monotherapy for use in patients with ALK-positive advanced (not amenable to curative therapy) or metastatic non-small cell lung cancer (NSCLC).
- 2015-11-18: Conditions were met
2017-08-28: New indication for patients with ROS-1 positive advanced non-small cell lung cancer (NSCLC).

History of changes in PMDA indication

2012-03-30: Initial approval for the treatment of unresectable advanced/relapsed ALK fusion gene-positive non-small cell lung cancer.
2017-05-18: New additional indication for the treatment of unresectable advanced/relapsed ROS1 fusion gene-positive non-small cell lung cancer.

Also known as

Code names: PF-02341066
Brand name: Crizalk, Crizocap, Crizonix, Xalkori

References

[insert-1] 1.0 ^1.1 ^1.2 Crizotinib (Xalkori) package insert

[2] Crizotinib (Xalkori) package insert (locally hosted backup)

[3] Crizotinib (Xalkori) patient drug information (Chemocare)

[4] Crizotinib (Xalkori) patient drug information (UpToDate)

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