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Cancer and Metastasis Reviews · 2025 · Vol. 44 · Issue 4 · Springer
Gefitinib is a first-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) used in the treatment of non-small cell lung cancer (NSCLC). It is metabolized extensively in the liver by enzymes encoded by CYP3A4 , CYP2D6, and CYP3A5 and is the substrate of membrane transporters including ABCB1 and ABCG2 . Evidence shows that single-nucleotide polymorphisms (SNPs) in these metabolizing and transporting...