This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Inflammation

Inflammatory disease

p38 mitogen-activated protein kinase (p38 MAPK; MAPK14); tumor necrosis factor-a (TNF-a)

In vitro studies identified dibenzoxepinone-based p38 MAPK inhibitors that could help treat inflammatory diseases. In an in vitro assay, the most potent member of a compound series inhibited p38 MAPK with an IC50 of 1.6 nM. In human whole blood, the same compound inhibited TNF-a release with an IC50 of 125 nM. Next steps could include evaluating the lead inhibitor in animal models of inflammatory disease.
At least four companies have p38 MAPK inhibitors in Phase II testing or earlier to treat various autoimmune or inflammatory diseases.

SciBX 6(45); doi:10.1038/scibx.2013.1296
Published online Nov. 21, 2013

Patent and licensing status unavailable

Baur, B. et al. J. Med. Chem.; published online Oct. 17, 2013;
doi:10.1021/jm401276h
Contact: Stefan A. Laufer, Eberhard Karls University of Tuebingen, Tuebingen, Germany
e-mail:
stefan.laufer@uni-tuebingen.de