Avacopan

A C5a1 receptor antagonist (IC50 = 0.1 nM); selective for C5a1 over the C5a2 receptor and CMKLR2 (IC50s = >10,000 nM for both), as well as the C3a receptor, CMKLR1, and FPR1 (IC50s = >10,000 nM for all), and over panels of 18 chemokine receptors (IC50s = ≥6,700 nM for all), 54 other receptors at 10 µM, and five CYP isoforms (IC50s = >10,000 nM for all); reduces the migration of isolated cynomolgus monkey neutrophils at 50 nM; reduces C5a-induced increases in CD11b levels on neutrophils in isolated whole blood from human C5AR1 knock-in mice at 10 and 100 nM or at 0.075 and 0.15 mg/kg