Drug intelligence / Profile preview

erdafitinib + osimertinib

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

Overview

Erdafitinib + osimertinib is an investigational combination therapy consisting of two small molecule tyrosine kinase inhibitors. Erdafitinib is a pan-fibroblast growth factor receptor (FGFR) inhibitor, while osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. This combination has been studied as a strategy to overcome acquired resistance to EGFR-targeted therapies in non-small cell lung cancer (NSCLC), particularly in cases where FGFR1 amplification or other resistance mechanisms emerge after progression on osimertinib monotherapy. The rationale for combining these agents lies in targeting both the primary oncogenic driver (EGFR mutations) and bypass signaling pathways such as FGFR, which can mediate resistance to EGFR inhibition[1].

02

Targets

FGFR4 (Fibroblast growth factor receptor 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)FGFR3 (Fibroblast growth factor receptor 3)FGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)

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