BioCentury
ARTICLE | Distillery Therapeutics

Neurology

July 10, 2018 9:39 PM UTC

Cell culture and mouse studies identified a TRPM8 antagonist that could help treat pain. Chemical synthesis of dibenzyl tryptamine analogs and HEK cell-based ion channel assays yielded a compound that inhibited TRPM8 with an IC50 value of 0.2 nM. In a mouse model of chemical-induced pain, the compound decreased cold hypersensitivity compared with vehicle. In a mouse model of chemotherapy-induced neuropathic pain, subcutaneous injection of the compound decreased cold allodynia compared with no treatment. Next steps could include testing the compound in additional models of pain.

Johnson & Johnson and Ice Therapeutics have Ice-3682, a small molecule TRPM8 antagonist in preclinical testing for interstitial cysitis, urinary tract disorders and overactive bladder (OAB)...