GS-829845

GS-829845 is the primary active metabolite of the Janus kinase 1 (JAK1) inhibitor filgotinib. Produced by the metabolism of filgotinib via carboxylesterase 2, GS-829845 exhibits a similar JAK1 selectivity profile as the parent drug but with approximately 10-fold reduced potency. Notably, systemic exposure to GS-829845 is much higher than that of filgotinib (16–20 times greater AUC). Both filgotinib and GS-829845 act as adenosine triphosphate (ATP)-competitive, reversible inhibitors of the JAK family, modulating the JAK-STAT signaling pathway to inhibit pro-inflammatory cytokine signaling. GS-829845, as an active metabolite, contributes significantly to the pharmacodynamic effects of filgotinib therapy in conditions such as rheumatoid arthritis and ulcerative colitis[1][2][3][4][5].

Other names

GS-829845GS829845GS 829845