Drug intelligence / Profile preview

SD-0006

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

SD‑0006 is an orally available small molecule diarylpyrazole that acts as a potent and selective ATP‑competitive inhibitor of p38α mitogen‑activated protein kinase (MAPK). It demonstrates high selectivity for p38α over other kinases (including modest selectivity over p38β and strong selectivity over p38γ/δ), binding at the ATP site with unique interactions outside the ATP pocket. In preclinical models and phase 1 clinical trials, SD‑0006 suppressed expression of multiple proinflammatory proteins such as TNFα and ameliorated disease severity in animal models of arthritis. The drug has shown efficacy in reducing inflammation by inhibiting the p38MAPK/HDAC4 pathway and promoting cell proliferation in nucleus pulposus cells. Developed primarily for inflammatory diseases such as arthritis, it was originated by Pfizer[2][3][5][8].

Other names
2-{4-[5-(4-chlorophenyl)-4-pyrimidin-4-yl-1H-pyrazol-3-yl]piperidin-1-yl}-2-oxoethanol5-p-chlorophenyl-3-[N-(2-hydroxyacetyl)piperidin-4-yl]-4-pyrimidin-4-yl-1H-pyrazole
02

Targets

MAPK14 (p38 mitogen-activated protein kinase alpha)

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