Drug intelligence / Profile preview

SB-705498

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intranasal, Rectal
01

Overview

SB-705498 is a potent and selective small molecule antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel, also known as the vanilloid receptor 1. TRPV1 is a nonselective cation channel highly expressed in sensory neurons and plays a key role in detecting noxious stimuli such as capsaicin (the active component of chili peppers), acid, and heat. By blocking TRPV1 activation by these stimuli, SB-705498 inhibits pain signaling associated with tissue injury and inflammation. The drug was developed by GlaxoSmithKline for investigational use in conditions such as rhinitis (including non-allergic rhinitis), chronic cough, migraine, and various pain states. It demonstrated efficacy in preclinical models of pain and showed pharmacodynamic activity in human studies but did not progress beyond phase II clinical trials; its development has since been terminated[2][3][4][6][8].

Other names
501951-42-4UNII-T74V9O0Y2WUNII-T-74V9O0Y2WUNII-T 74V9O0Y2W
02

Targets

TRPV1 (Transient receptor potential cation channel subfamily V member 1)

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