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RO5212054

Development stage: Phase 1
Lead developer: Roche
Modality: Small Molecules
Administration: Oral

Overview

RO5212054 is an orally available small-molecule inhibitor that selectively targets the mutant Serine/threonine-protein kinase BRAF (BRAF) V600E kinase, a key component of the MAPK/ERK signaling pathway implicated in various cancers. By inhibiting this mutated form of BRAF, RO5212054 disrupts downstream signaling involved in cell proliferation and survival, offering potential antineoplastic (anti-cancer) activity. The drug was developed by Roche and has been primarily investigated for use in patients with advanced solid tumors harboring BRAF V600 mutations. Clinical studies have focused on its safety, tolerability, and pharmacokinetics in this patient population[1][2][5][8].

Other names: RO5212054RO-5212054RO 5212054PLX3603PLX-3603PLX 3603RG7256RG-7256RG 7256

Targets

BRAF V600E

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