This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Neurology

Pain

m-Opioid receptor (OPRM1; MOR); metabotropic glutamate receptor subtype 5 (mGluR5; GRM5)

A mouse study suggests bivalent ligands with OPRM1 agonist and mGluR5 antagonist activity could help treat chronic inflammatory pain. In lipopolysaccharide (LPS)-pretreated mice, intrathecal administration of bivalent inhibitors yielded a more potent anti-nociceptive response in tail flick assays than administration of monovalent inhibitors without inducing acute tolerance. Next steps include generation of bivalent ligands for other heteromeric receptors.
At least six companies have mGluR5 antagonists in Phase III or earlier development for neurology indications.

SciBX 6(29); doi:10.1038/scibx.2013.765
Published online Aug. 1, 2013

Series of bivalent ligands patented; licensing status unavailable

Akgün, E. et al. Proc. Natl. Acad. Sci. USA; published online June 24, 2013;
doi:10.1073/pnas.1305461110
Contact: Philip S. Portoghese, University of Minnesota, Minneapolis, Minn.
e-mail:
porto001@maroon.tc.umn.edu