Drug intelligence / Profile preview

GDC-0879

Development stage
Preclinical
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GDC-0879 is a **potent, selective, and orally bioavailable small molecule inhibitor of B-Raf kinase**, primarily targeting the Raf/MEK/ERK signaling pathway, which is implicated in various cancers including those harboring the BRAFV600E mutation. It demonstrates high selectivity and potency against mutant B-Raf, showing significant inhibition of ERK phosphorylation and tumor progression in preclinical models. GDC-0879 has also been shown to bind C-Raf and A-Raf, with minimal activity against other kinases. Beyond oncology, it has demonstrated the ability to promote podocyte survival by paradoxically activating the MAPK pathway, suggesting potential utility in kidney disease research. The drug was developed for research purposes and has not advanced to clinical approval[1][3][4][5].

Other names
2-[4-[(1E)-1-hydroxyimino-2,3-dihydroinden-5-yl]-3-pyridin-4-ylpyrazol-1-yl]ethanolCAS 905281-76-7CAS905281-76-7CAS-905281-76-7
02

Targets

ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)CSNK1D (Casein kinase I delta)BRAF V600ERAF1 (c-Raf-1 (Y340D/Y341D))

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