Drug intelligence / Profile preview

adezmapimod

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

Adezmapimod is a small molecule, first-generation inhibitor of the p38 mitogen-activated protein kinase (MAPK) signaling pathway, with high selectivity for the alpha (MAPK14) and beta (MAPK11) isoforms. It functions as an ATP-competitive inhibitor, preventing the phosphorylation of downstream substrates and thereby suppressing the production of pro-inflammatory cytokines, including tumor necrosis factor-alpha (TNF-α) and interleukin-2 (IL-2). While adezmapimod has been extensively utilized as a research tool to investigate cellular processes such as inflammation, apoptosis, and autophagy, and has shown activity in preclinical models of triple-negative breast cancer (TNBC), it has not been developed for clinical use in humans. The compound is often identified in literature by the code names SB203580 or RWJ-67657.

Brand names
Seroguard
Other names
4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)imidazole
02

Targets

MAPK14 (p38 mitogen-activated protein kinase alpha)

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