Crizotinib

Information about Crizotinib

Crizotinib is a selective tyrosine kinase receptor inhibitor used in the therapy of selected cases of advanced non-small cell lung cancer. 

Liver safety of Crizotinib

Crizotinib is associated with transient elevations in serum aminotransferase levels during treatment and rare instances of clinically apparent acute liver injury that can be severe and even fatal. 

Mechanism of action of Crizotinib

Crizotinib (kriz oh’ ti nib) is an orally available, small molecule inhibitor of the tyrosine kinase receptor of mutated anaplastic lymphoma kinase (ALK), which is the result of a chromosomal translocation found in about 5% of lung cancers.  Patients with non-small cell lung cancer with the ALK mutation often respond to crizotinib therapy with shrinkage of the tumor and apparent improvement in survival. 

FDA approval information for Crizotinib

Crizotinib received accelerated approval for use in the United States in 2011 for the treatment of advanced non-small cell lung cancer with the ALK translocation (a test for this genetic rearrangement was also approved). 

Dosage and administration for Crizotinib

Crizotinib is available in capsules of 200 and 250 mg under the brand name Xalkori.  The recommended dose is 250 mg by mouth twice daily, with dose modification based upon tolerance. 

Side effects of Crizotinib

Side effects are common and include diarrhea, nausea, vomiting, anorexia, fatigue, constipation, visual disturbances and edema.  Uncommon, but potentially serious side effects include interstitial lung disease, QTc interval prolongation and bradycardia. 

 

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