BioCentury
ARTICLE | Distillery Therapeutics

Neurology

February 11, 2019 9:17 PM UTC

In vitro and rat studies identified a benzimidazole-based PTGER4 antagonist that could help treat pain. High throughput screening of Bayer AG's compound library, in vitro enzymatic activity assays and optimization of hits yielded a benzimidazolecarboxylic acid-based compound (BAY 1316957) that antagonized PTGER4 with an IC50 of 15.3 nM. In a rat model of prostaglandin E2 (PGE2)-induced pain, the compound decreased mechanical allodynia compared with vehicle. Next steps by Bayer could include testing BAY 1316957 in other mouse models of pain.

AskAt Inc. has the PTGER4 antagonist ARY-007 in Phase II testing for pain and Phase I testing for allergy. AskAt and Arrys Therapeutics Inc. have the compound in preclinical testing for cancer...