Ceritinib

Information about Ceritinib

Ceritinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NSCLC). 

Liver safety of Ceritinib

Ceritinib is associated with a moderate rate of serum aminotransferase elevations during therapy and rare instances of clinically apparent acute liver injury. 

Mechanism of action of Ceritinib

Ceritinib (se ri' ti nib) is a small molecule tyrosine kinase receptor inhibitor with potent activity against anaplastic lymphoma kinase (ALK) that is rearranged and mutated in selected cancers including approximately 5% of non-small cell lung cancer (NSCLC).  The mutated, rearranged ALK promotes unregulated cell growth and proliferation and is overexpressed in some cancer cells.  Ceritinib has been found to inhibit mutated ALK in cell culture and in several clinical trials was found to induce objective responses in a proportion of patients with advanced ALK-positive NSCLC. 

FDA approval information for Ceritinib

Ceritinib received accelerated approval for use crizotinib-refractory, ALK-positive NSCLC in the United States in 2014.  Ceritinib is available in capsules of 150 mg under the brand name Zykadia. 

Dosage and administration for Ceritinib

The recommended initial dose is 750 mg (5 capsules) once daily, continued until progressive disease or intolerable toxicity occurs. 

Side effects of Ceritinib

Side effects are common and include diarrhea, nausea and vomiting, abdominal pain, fatigue, anorexia and constipation.  Uncommon, but potentially severe side effects include severe diarrhea leading to dehydration and renal failure, interstitial lung disease, prolongation of the QTc interval, bradycardia, hyperglycemia, and embryo-fetal toxicity.

 

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