Drug intelligence / Profile preview

erlotinib + gefitinib + osimertinib

Development stage
Preclinical
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination of three epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): erlotinib, gefitinib, and osimertinib. All three are small molecule inhibitors targeting the EGFR pathway, which is frequently mutated in non-small cell lung cancer (NSCLC). Erlotinib and gefitinib are first-generation reversible EGFR TKIs, while osimertinib is a third-generation irreversible inhibitor that also targets the T790M resistance mutation. The rationale for combining these agents is to preemptively suppress or delay the emergence of resistance mutations by simultaneously inhibiting multiple forms of mutant EGFR. This approach has been proposed as a strategy to extend progression-free survival in patients with EGFR-mutant NSCLC compared to monotherapy with any single agent[1][3][5]. However, this specific triple combination has not been widely studied in clinical trials; most published data focus on dual combinations or sequential use.

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)

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