This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Various

Coronary artery disease (CAD); Parkinson's disease (PD)

Myeloperoxidase (MPO)

In vitro and rat studies suggest a series of MPO inhibitors could help treat inflammation-associated diseases such as CAD and PD. SAR studies and in vitro testing of alkylindoles identified compounds that selectively inhibit MPO with low nanomolar IC50 values. In a low-density lipoprotein (LDL) oxidation assay, two of the compounds inhibited MPO-mediated LDL oxidation with low nanomolar IC50 values. Select compounds showed a good safety profile in normal rats. Next steps could include testing the compounds in animal models for CAD.
AZD3241, an MPO inhibitor from AstraZeneca plc, is in Phase II testing to treat PD.

SciBX 6(17); doi:10.1038/scibx.2013.420
Published online May 2, 2013

Patent and licensing status unavailable

Soubhye, J. et al. J. Med. Chem.; published online April 14, 2013;
doi:10.1021/jm4001538
Contact: Pierre G. Van Antwerpen, Free University of Brussels, Brussels, Belgium
e-mail:
pvantwer@ulb.ac.be