GSK-2981278

GSK-2981278 is a small molecule drug developed by GSK for the topical treatment of plaque psoriasis. It acts as a highly potent and selective inverse agonist of the nuclear receptor subfamily 1 group F member 3 (RORγ, also known as RORC or RORγt). By inhibiting the transcriptional activity of RORγt, it suppresses Th17 signature cytokine production, which is implicated in the pathogenesis of psoriasis. Despite promising preclinical data showing inhibition of cytokine expression in vitro and ex vivo human tissue models, clinical trials did not demonstrate significant improvement in psoriatic lesions. Development for plaque psoriasis was discontinued after phase II trials[1][4][7].

Other names

N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide1474110-21-8