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crizotinib (Xalkori)
Indications:
- non small cell lung carcinoma with mutations in the anaplastic lymphoma kinase (ALK) protein; not recommended (NICE)
Dosage:
- 250 mg PO BID for 25 weeks or more
Adverse effects:
- nausea (55%) & vomiting (39%) most common
- hepatotoxicity (< 1%), may be fatal [2]
Mechanism of action:
- selective, ATP-competitive, small molecule, orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK) & MET/HGF receptor tyrosine kinases [1]
Related
ceritinib; pelitinib (Zykadia)
General
small inhibitory antineoplastic agent (ib drug)
References
- Bang Y et al,
Clinical activity of the oral ALK inhibitor PF-02341066 in
ALK-positive patients with non-small cell lung cancer (NSCLC).
J Clin Oncol 28:18s, 2010 (suppl; abstr 3)
http://abstract.asco.org/AbstView_74_50854.html
- Drug-induced hepatotoxicity with fatal outcome has occurred
with Xalkori (crizotinib)
Pfizer Bulletin: Dec 29, 2013