Drug intelligence / Profile preview

binimetinib + lifirafenib

Development stage
Unknown
Lead developer
BeiGene
Modality
Small Molecules
Administration
Oral
01

Overview

binimetinib + lifirafenib is a **combination of two investigational small molecule kinase inhibitors** used in clinical trials for advanced solid tumors, especially cancers with MAPK pathway activation, such as BRAF or RAS-mutant malignancies. **Binimetinib** is a reversible inhibitor of MEK1/2, blocking part of the MAPK pathway downstream of RAS and BRAF. **Lifirafenib** (also known by code names BGB-283 and BPI-283) is a pan-RAF inhibitor, targeting mutant BRAF, wild-type BRAF, and CRAF, and also inhibiting EGFR family kinases. The combination is intended to suppress cell proliferation and tumor growth by dual inhibition of RAF and MEK kinases, overcoming resistance seen with single-agent BRAF or MEK inhibitors. The drugs have primarily been investigated as oral therapies in Phase 1 and Phase 2 clinical trials for solid tumors, including advanced melanoma, non-small cell lung cancer, and colorectal cancer with MAPK pathway alterations.

02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)BRAF (B-Raf proto-oncogene, serine/threonine kinase)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)RAF1 (c-Raf-1 (Y340D/Y341D))MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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