erlotinib + gefitinib

Erlotinib + gefitinib is a combination of two small molecule tyrosine kinase inhibitors that target the epidermal growth factor receptor (EGFR) tyrosine kinase domain. Both drugs inhibit EGFR by binding to its ATP-binding site, thereby blocking downstream signaling pathways involved in cell proliferation and survival. These agents are primarily used as targeted therapies for non-small cell lung cancer (NSCLC) with activating EGFR mutations. While both drugs have similar mechanisms of action and efficacy profiles when used individually, there is no established clinical use or approval for their combined administration as a single regimen; they are typically studied or prescribed separately[1][4][5]. Each drug has been developed and marketed independently—erlotinib by Genentech/Roche and Astellas Pharma under the brand name Tarceva, and gefitinib by AstraZeneca under the brand name Iressa[2][7]. The combination would theoretically provide dual inhibition of EGFR but is not standard practice due to overlapping mechanisms and toxicity profiles.

Brand names

IressaTarceva

Other names

gefitinib and erlotinibEGFR-TKI combination (gefitinib + erlotinib)