Drug intelligence / Profile preview

erlotinib + cetuximab

Development stage
Phase 2
Lead developer
Genentech
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Erlotinib + cetuximab is a combination therapy targeting the epidermal growth factor receptor (EGFR) pathway in cancer. Erlotinib is a small molecule tyrosine kinase inhibitor that blocks EGFR signaling, thereby inhibiting cancer cell proliferation and survival. Cetuximab is a monoclonal antibody that binds to the extracellular domain of EGFR, preventing ligand binding and receptor activation. The rationale for combining these agents is to achieve dual inhibition of EGFR through different mechanisms—one intracellular (erlotinib) and one extracellular (cetuximab)—which may overcome resistance seen with single-agent therapy. This combination has been studied primarily in non-small cell lung cancer (NSCLC), head and neck squamous cell carcinoma (HNSCC), and other advanced solid tumors, particularly in patients who have progressed on prior therapies or have TKI-resistant mutations[1][2][4][5].

Other names
erlotinib hydrochloride
02

Targets

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