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gefitinib + osimertinib

Development stage: Unknown
Lead developer: Dana-Farber Cancer Institute
Modality: Small Molecules
Administration: Oral

Overview

A combination of two EGFR tyrosine kinase inhibitors (TKIs) used to treat EGFR-mutant non-small cell lung cancer (NSCLC). Gefitinib is a first-generation EGFR TKI while osimertinib is a third-generation EGFR TKI that specifically targets the T790M resistance mutation. This combination is designed as a preemptive strategy to delay or prevent the emergence of resistance mechanisms, particularly in cases where T790M and C797S mutations occur in trans. The combination has shown promising response rates in clinical trials with manageable toxicity profiles.

Targets

EGFR (Epidermal growth factor receptor)

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