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exarafenib + STX-241
- Development stage
- Unknown
- Lead developer
- Pierre Fabre
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
exarafenib + STX-241 (identified in some pipeline documents as IRL-345 + STX-347 due to optical character recognition errors) is an investigational combination targeted therapy being developed by Pierre Fabre Médicament for the treatment of solid tumors. Exarafenib (NFX-179) is a potent, selective, and orally bioavailable Type II pan-RAF inhibitor that targets ARAF, BRAF, and CRAF kinases, effectively suppressing the MAPK/ERK signaling pathway. STX-241 is a highly selective, CNS-penetrant, small molecule inhibitor of the Epidermal Growth Factor Receptor (EGFR), specifically designed to target the L858R mutation. The combination aims to provide a dual blockade of the EGFR and RAF/MEK/ERK pathways to achieve synergistic anti-tumor activity and overcome resistance mechanisms in cancers such as non-small cell lung cancer (NSCLC). The regimen is currently in Phase 1 clinical development.
- Other names
- exarafenib and STX-241 combination
02
Targets
ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)RAF1 (c-Raf-1 (Y340D/Y341D))BRAF (B-Raf proto-oncogene, serine/threonine kinase)
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