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BIEGi-1

Development stage: Preclinical
Modality: Small Molecules

Overview

BIEGi-1 is a binary epidermal growth factor receptor (EGFR) inhibitor small molecule that blocks EGFR's Rheb-GEF activity. It exhibits increased effectiveness in inhibiting this lysosomal, kinase-independent function of EGFR compared to the tyrosine kinase inhibitor afatinib. This unique mechanism suggests a distinct approach to targeting EGFR-driven tumor growth mechanisms, potentially relevant where canonical kinase inhibition is insufficient or resistance has developed.[1]

Targets

EGFR (Epidermal growth factor receptor)

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