Drug intelligence / Profile preview

AMTB

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

AMTB is a potent and selective small molecule antagonist of the Transient Receptor Potential Melastatin 8 (TRPM8) ion channel. TRPM8 is a non-selective cation channel primarily known for its role as a cold and menthol sensor, but it is also implicated in various inflammatory and fibrotic processes. In the context of Crohn's disease, AMTB has been shown to mitigate intestinal fibrosis by inhibiting the proliferation and activation of intestinal fibroblasts and modulating immune signaling, specifically CX3CR1+ cell populations. Research indicates that TRPM8 is upregulated in fibrotic tissues of patients with Crohn's disease, and its pharmacological inhibition with AMTB reduces extracellular matrix deposition and inflammatory markers in preclinical models.

Other names
N-(3-Aminopropyl)-2-[(3-methylphenyl)methoxy]-N-(2-thienylmethyl)benzamide
02

Targets

TRPM8 (Transient receptor potential cation channel subfamily M member 8)

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