BioCentury
ARTICLE | Distillery Therapeutics

Neurology

November 6, 2017 7:57 PM UTC

Mouse studies suggest endosome-targeting conjugates of CRLR and NK1R antagonists could help treat chronic pain. The conjugates were created by linking CRLR and NK1R antagonist tool compounds to the lipid cholestanol, which targets the conjugates to endosomes by binding an endosomal receptor. In three mouse models of chronic pain, intrathecal injection of the CRLR antagonist conjugate increased the duration of analgesia compared with unconjugated antagonist. In a mouse model of chemical-induced chronic pain, the combination of the NK1R and CRLR antagonist conjugates decreased mechanical pain compared with a combination of the unconjugated NK1R antagonists. Next steps could include a chronic pain trial of endosomal CRLR and NK1R inhibitors.

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