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Buparlisib + gefitinib is an investigational combination therapy consisting of two small molecule inhibitors used in oncology research. Buparlisib (BKM120) is an oral pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor that targets the PI3K/AKT/mTOR signaling pathway, which is frequently activated in various cancers. Gefitinib (ZD1839), marketed as Iressa, is a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved for the treatment of non-small cell lung cancer (NSCLC) with specific EGFR mutations. The rationale for combining these agents stems from preclinical and early clinical evidence suggesting that dual inhibition of EGFR and PI3K pathways may overcome resistance mechanisms to single-agent therapies and enhance anti-tumor activity in patients with advanced solid tumors such as NSCLC. Clinical studies have observed mild anti-tumor activity with this combination; however, further investigation into efficacy and safety profiles continues[1][3].
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