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p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3. It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.1 VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.

Inn NameNeflamapimod
Usan NameNeflamapimod
Lab CodesVX-745, VRT-031745, VD-31745
Chemical Name5-(2,6-dichlorophenyl)-2-[(2,4-difluorophenyl)sulfanyl]-6H-pyrimido[1,6-b]pyridazin-6-one
Chemical StructureNeflamapimod.png
Molecular FormulaC19H9Cl2F2N3OS
Cas Registry Number209410-46-8
New Molecular EntityYes
OriginatorVertex Pharmaceuticals
DeveloperEIP Pharma
Mechanism Of ActionP38 mitogen-activated protein kinase inhibitor
Who Atc CodesM01 (Antiinflammatory and Antirheumatic Products)
N06D-X (Other anti-dementia drugs)
N07X (Other Nervous System Drugs)
Ephmra CodesM1 (Anti-Inflammatory and Anti-Rheumatic Products)
N7D9 (All other anti-Alzheimer products)
N7X (All other CNS drugs)
IndicationAlzheimer's Disease

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