Drug intelligence / Profile preview

JTC-801 free base

Development stage
Unknown
Lead developer
Japan Tobacco
Modality
Small Molecules
Administration
Oral
01

Overview

JTC-801 free base is a small molecule, orally active, selective antagonist of the nociceptin receptor (also known as opioid receptor-like1 or ORL1). It was developed as an analgesic agent and has been evaluated for its use in cancer treatment and pain management, including neuropathic, cancer-related, and postoperative pain. The compound blocks the nociceptin receptor with high affinity (Ki ~8.2 nM), thereby modulating pain signaling pathways distinct from classical opioid receptors. While it also weakly inhibits δ-, κ-, and μ-opioid receptors at higher concentrations, its primary mechanism is antagonism of the nociceptin receptor. Clinical development reached phase II trials but was discontinued[1][3][5][7].

Other names
N-(4-amino-2-methylquinolin-6-yl)-2-((4-ethylphenoxy)methyl)benzamide244218-93-7BXU45ZH6LIBXU-45ZH6LIBXU 45ZH6LI
02

Targets

NOP (Nociceptin/orphanin FQ peptide receptor)DOR (Opioid Receptor Delta 1)KOR (Kappa opioid receptor)MOR (Mu opioid receptor)

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