LNP023 (hydrochloride)

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A CFB inhibitor (IC50 = 10 nM); selective for CFB over a panel of 41 human proteases and 110 other enzymes, receptors, and ion channels (IC50s = >30 µM for all); inhibits zymosan A-induced formation of the membrane attack complex in isolated human blood (IC50 = 150 nM); blocks hemolysis of erythrocytes isolated from patients with paroxysmal nocturnal hemoglobinuria (IC50 = 400 nM); reduces levels of complement factor Ba, -C3d, and -C5a in the joints, levels of inflammatory cell infiltration in joint tissue, and arthritis disease severity in a K/BxN serum transfer-induced mouse model of inflammatory arthritis at 60 mg/kg twice per day; decreases proteinuria and serum levels of urea and creatine and prevents hair loss and kidney damage in an MRL-lpr mouse model of lupus nephritis at 30 mg/kg per day