Avacopan CAS# 1346623-17-3 (2R,3S)-2-[4-(环戊基氨基)苯基]-1-(2-氟-6-甲基苯甲酰基)-N-[4-甲基3-(三氟甲基)苯基]哌啶-3-甲酰胺

Avacopan, also known as CCX168, is an orally active, selective and potent C5aR inhibitor. CCX168 blocked the C5a binding, C5a-mediated migration, calcium mobilization, and CD11b upregulation in U937 cells as well as in freshly isolated human neutrophils. CCX168 retains high potency when present in human blood. CCX168 effectively blocked migration in in vitro and ex vivo chemotaxis assays, and it blocked the C5a-mediated neutrophil vascular endothelial margination. Avacopan was approved in 10/7/2021 for to treat severe active anti-neutrophil cytoplasmic autoantibody-associated vasculitis (granulomatosis with polyangiitis and microscopic polyangiitis) in combination with standard therapy, including glucocorticoids