Drug intelligence / Profile preview

gefitinib + nimotuzumab

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Gefitinib + nimotuzumab is a combination therapy consisting of two agents targeting the epidermal growth factor receptor (EGFR) pathway, used primarily in advanced or metastatic non-small cell lung cancer (NSCLC). Gefitinib is an oral small molecule tyrosine kinase inhibitor that selectively inhibits EGFR tyrosine kinase activity, thereby blocking downstream signaling involved in tumor cell proliferation and survival. Nimotuzumab is a humanized monoclonal antibody that binds to the extracellular domain of EGFR, preventing ligand binding and receptor activation. The rationale for combining these two drugs is to achieve dual inhibition of EGFR through different mechanisms—one at the intracellular kinase level (gefitinib) and one at the extracellular receptor level (nimotuzumab)—to potentially overcome resistance to single-agent EGFR inhibitors. Clinical studies have shown this combination has a manageable safety profile with common adverse events including rash and diarrhea; however, efficacy outcomes such as progression-free survival were not significantly superior compared to gefitinib alone[1][2][8].

02

Targets

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