Drug intelligence / Profile preview

RO-4987655

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

Overview

RO-4987655 is an orally active and highly selective small molecule inhibitor of mitogen‑activated protein kinase kinase 1 (MAP2K1 or MEK1), a key enzyme in the MAPK/ERK signaling pathway. By binding to and inhibiting MEK1/MEK2 with high potency (IC50 of 5.2 nM), it disrupts downstream cell signaling involved in cell proliferation and survival. This mechanism confers potential antineoplastic activity against tumors with constitutive activation of the RAS/RAF/MEK/ERK pathway. Developed as a novel cancer chemotherapeutic agent, RO‑4987655 has been investigated primarily for solid tumors and other neoplasms[1][4][6][7].

Other names
3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-5-[(3-oxo-1,2-oxazinan-2-yl)methyl]benzamide
02

Targets

MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)

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