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编 号:F747874
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CAS No: 1917321-26-6
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生物活性:
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2?nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research.
体内研究:
Crovalimab (SKY59; RO7112689; 20?mg/kg; 静脉注射; 仅第 0 天一次) 完全防止食蟹猴体内血浆 C5 的积累。Crovalimab-IgG1 (SG115) 显示出较慢的清除率:1.87mL/day/kg。Crovalimab (20?mg/kg; 静脉注射; 单剂量) 稳定抑制血浆中的补体活性 8 周。Crovalimab (第 0 天静脉注射 5mg/kg; 第 7、21、35、49 和 63 天皮下注射 2mg/kg) 在 cRBC 裂解试验中导致超过 20% 的血清溶血活性,吞咽困难和乳酸脱氢酶 (LDH) 和丙氨酸转氨酶 (ALT) 水平急剧升高。
体外研究:
Crovalimab (SKY59; RO7112689; 0-100 μg/mL) 抑制经典途径和反应性裂解系统中的溶血。