Drug intelligence / Profile preview

lifirafenib

Development stage
Phase 1
Lead developer
BeiGene
Modality
Small Molecules
Administration
Oral
01

Overview

Lifirafenib is an investigational, orally available small molecule inhibitor targeting both monomeric and dimeric forms of RAF kinases (including BRAF, ARAF, and CRAF) as well as the epidermal growth factor receptor (EGFR). It is designed to inhibit key components of the MAPK signaling pathway implicated in tumorigenesis. Lifirafenib has demonstrated antitumor activity in preclinical models and clinical studies involving patients with solid tumors harboring mutations in BRAF (including V600E and non-V600E), KRAS, or NRAS. The drug also exhibits inhibitory activity against other kinases such as DDR1/2, EPHA3, FLT3, VEGFR2, ABL1, RET, EPHGA7/B2, MNK2, ZAK and PDGF receptors. Lifirafenib is being developed primarily for advanced or refractory solid tumors with MAPK pathway aberrations. It has been studied both as monotherapy and in combination with MEK inhibitors such as mirdametinib[2][3][4][5][6][7]. Developers: BeiGene

Other names
lifirafenibBeigene-283Beigene283Beigene 283
02

Targets

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

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