Drug intelligence / Profile preview

afatinib + cetuximab

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

Overview

Afatinib + cetuximab is a combination therapy for the treatment of advanced non-small cell lung cancer (NSCLC) with activating mutations in the epidermal growth factor receptor (EGFR) gene, particularly after progression on first-generation EGFR tyrosine kinase inhibitors (TKIs). Afatinib is an irreversible ErbB family blocker that inhibits signaling from EGFR, HER2, and HER4. Cetuximab is a monoclonal antibody that binds to the extracellular domain of EGFR, blocking ligand binding and receptor activation. The combination has shown preclinical and clinical activity in overcoming resistance to first- or third-generation TKIs, especially in cases with T790M or L718Q mutations[1][2][5]. However, when used as front-line therapy for treatment-naïve patients with EGFR-mutant NSCLC, the combination did not improve progression-free survival compared to afatinib alone and was associated with increased toxicity[4][7].

Brand names
Gilotrif + ErbituxGiotrif + Erbitux
Other names
afatinib and cetuximabafatinib plus cetuximab
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR (Epidermal growth factor receptor)

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