Medical College of Wisconsin
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Tyrosine kinase inhibitors for EGFR- and ALK-mutated non-small cell lung cancer ADMET & DMPK ADMET & DMPK 4(3)(2016) 186-211




Discovery of the epidermal growth receptor (EGFR) activating mutations and anaplastic lymphoma kinase (ALK) rearrangements has expanded the therapeutic landscape in non-small cell lung cancer (NSCLC). Survival outcomes for patients with these mutations have improved dramatically with EGFR and ALK tyrosine kinase inhibitors (TKIs). Multiple generations of EGFR and ALK TKIs have been rapidly developed, and patients and clinicians now have several options for first- and second-line treatments. While these small molecule TKIs have some similarities in therapeutic and pharmacologic profiles, the differences can be clinically substantial, allowing tailored treatment for each unique patient. This review details the clinical efficacy, pharmacology, safety profiles, CNS penetration, and mechanisms of resistance of the four EGFR TKIs and three ALK TKIs that are currently approved by the United States Food and Drug Administration (US FDA).

Author List

Jonathan R. Thompson, Smitha P. Menon, Grace K. Dy


Jonathan R. Thompson MD Assistant Professor in the Medicine department at Medical College of Wisconsin

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