Drug intelligence / Profile preview

afatinib + erlotinib + gefitinib

Development stage
Unknown
Lead developer
Boehringer Ingelheim
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a combination of three small molecule tyrosine kinase inhibitors (TKIs): afatinib, erlotinib, and gefitinib. Each drug targets the epidermal growth factor receptor (EGFR) tyrosine kinase domain, inhibiting its activity and 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. Afatinib is a second-generation irreversible EGFR TKI that also inhibits other members of the ErbB family, while erlotinib and gefitinib are first-generation reversible EGFR TKIs[5][6][9]. All three drugs have demonstrated efficacy in prolonging progression-free survival in patients with advanced NSCLC harboring EGFR mutations[1][2][5]. However, each has a distinct safety profile; afatinib tends to be associated with higher rates of certain adverse events such as diarrhea and skin toxicities compared to erlotinib or gefitinib[1][6].

02

Targets

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

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