In vitro activity: Solcitinib (formerly GSK2586184 or GLPG0778) is a potent, selective, and orally available Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis. It has an IC50 of 9.8 nM for JAK1 and is 11-, 55- and 23-fold more selective over JAK2, JAK3 and TYK2, respectively. 12 weeks of treatment with GSK2586184 resulted in clinical improvement and was generally well tolerated in patients with moderate-to-severe plaque-type psoriasis. Overall, the incidence of adverse events (AEs) was similar across treatment groups, and no relationship between frequency of AE and GSK2586184 dose was identified. Differential gene expression was observed in involved and uninvolved skin at baseline and in involved skin after 2 weeks of treatment with GSK2586184.

Kinase Assay: Solcitinib (formerly GSK2586184 or GLPG0778) is a potent, selective, and orally available Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis. It has an IC50 of 9.8 nM for JAK1 and is 11-, 55- and 23-fold more selective over JAK2, JAK3 and TYK2, respectively.