S-777469

S-777469 is a selective and orally available small molecule agonist of the cannabinoid receptor type 2 (CB2), developed by Shionogi for the treatment of atopic dermatitis. It exhibits high selectivity for CB2 over CB1 receptors (128-fold selectivity; CB2 affinity Ki = 36 nM, CB1 affinity >4600 nM). In preclinical studies, S-777469 demonstrated anti-inflammatory and antipruritic effects by suppressing skin inflammation and itch-associated behaviors in animal models. Mechanistically, it reduces mast cell infiltration and eosinophil accumulation in inflamed skin lesions. The drug advanced to Phase II clinical trials for atopic dermatitis but development was discontinued after these studies[1][3][5][6][7].

Other names

1-[[6-Ethyl-1-[4-fluorobenzyl]-5-methyl-2-oxo-1,2-dihydropyridine-3-carbonyl]amino]-cyclohexanecarboxylic acid