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Gefitinib + tamoxifen is a combination therapy that targets both the epidermal growth factor receptor (EGFR) and estrogen receptor (ER) pathways simultaneously. This combination approach aims to overcome resistance mechanisms in breast cancer treatment. Gefitinib inhibits EGFR tyrosine kinase activity, while tamoxifen acts as an estrogen receptor antagonist. The combination has been studied particularly for its potential in treating triple-negative breast cancer and hormone receptor-positive breast cancer that has developed resistance to single-agent therapy. Some research has explored hybrid ligands that connect tamoxifen or endoxifen with gefitinib via a covalent linkage, which may offer advantages of pharmacokinetic simplicity and fewer drug-drug interactions compared to administering the drugs separately.
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