Drug intelligence / Profile preview

GW405833

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

Overview

GW405833 is a potent and selective small molecule partial agonist of the cannabinoid receptor subtype 2 (CB2), with over 1200-fold selectivity for CB2 compared to cannabinoid receptor type 1 (CB1)[1][3][5][7]. Developed by GSK, GW405833 has been primarily studied for its anti-inflammatory, anti-hyperalgesic, and antiallodynic properties in preclinical animal models, showing efficacy in reducing pain associated with inflammatory and neuropathic conditions [1][3][6]. Although originally described as a CB2 agonist, its pharmacology is complex; it also displays partial activity at CB1, with evidence suggesting additional roles as a noncompetitive CB1 antagonist and possible inverse or protean agonist at CB2 in vitro [3]. It impacts inflammatory cytokine production and oxidative stress, and has been investigated for acute inflammation, pain, and cancer-bone interactions [2][4][5][6]. Its maximal development stage is preclinical [5].

Other names
GW-405,833L-768,242
02

Targets

CNR1 (Cannabinoid receptor 1)

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