Drug intelligence / Profile preview

BMS-908662 + cetuximab

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral (BMS-908662), Intravenous (cetuximab)
01

Overview

BMS-908662 + cetuximab is an experimental combination therapy that pairs BMS-908662, an orally active small molecule pan-RAF kinase inhibitor, with cetuximab, a monoclonal antibody targeting epidermal growth factor receptor (EGFR). BMS-908662 inhibits RAF kinases (including BRAF and CRAF), interfering with the RAF/MEK/ERK signaling pathway, which is often dysregulated in cancer through BRAF or KRAS mutations[3][5][7][8][9]. Cetuximab binds to EGFR, blocking downstream signaling involved in cell proliferation and survival. The combination is under investigation as an antineoplastic therapy, notably in colorectal cancer, with the rationale that simultaneous inhibition of EGFR and RAF/MEK/ERK pathways could overcome resistance to single-agent therapies and enhance antitumor activity[1]. Both drugs have well-characterized mechanisms: BMS-908662 disrupts RAF-dependent signaling, while cetuximab prevents EGFR activation.

Other names
XL281 + cetuximab
02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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