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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

  1. 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
  2. Drug-induced hepatotoxicity with fatal outcome has occurred with Xalkori (crizotinib) Pfizer Bulletin: Dec 29, 2013