Swedish Orphan Biovitrum AB, 171 65 Stockholm, Sweden.
Apellis Pharmaceuticals, Inc., Waltham, MA 02451, USA.
Int J Mol Sci. 2024 Aug 9;25(16):8698. doi: 10.3390/ijms25168698.
Paroxysmal nocturnal hemoglobinuria (PNH) is a rare disease characterized by complement-mediated hemolysis and potentially life-threatening complications. Pegcetacoplan, an inhibitor of complement components C3 and C3b, was approved by the US Food and Drug Administration (FDA) and European Medicines Agency (EMA) in 2021. A recent expansion to its indication by the EMA has made pegcetacoplan available for the treatment of both complement inhibitor-naïve and -experienced patients with PNH who have hemolytic anemia, a similarly broad patient population as in the US. This approval was based on results from the Phase 3 PEGASUS study, where pegcetacoplan showed superiority over the C5 inhibitor eculizumab with regard to improving the hemoglobin level in patients with anemia despite eculizumab treatment, and the Phase 3 PRINCE study, where pegcetacoplan showed superiority over supportive care with regard to hemoglobin stabilization and improving the lactate dehydrogenase level in complement inhibitor-naïve patients. In light of this recent indication expansion by the EMA, this article describes how the strong efficacy of pegcetacoplan is linked to its mechanism of action, which provides broad hemolysis control over both intravascular and extravascular hemolysis to improve a range of disease markers and enhance patients' quality of life. Furthermore, additional data and learnings obtained from over 3 years of experience with pegcetacoplan are summarized, including long-term efficacy and safety results, real-world clinical experiences, pharmacokinetic characteristics, and extensive practical guidance for the first-to-market proximal complement inhibitor for PNH.
阵发性睡眠性血红蛋白尿症(PNH)是一种罕见疾病,其特征为补体介导的溶血,并可能导致危及生命的并发症。Pegcetacoplan 是一种补体成分 C3 和 C3b 的抑制剂,于 2021 年获得美国食品药品监督管理局(FDA)和欧洲药品管理局(EMA)的批准。EMA 最近扩大了其适应证,使 pegcetacoplan 可用于治疗补体抑制剂初治和经治的 PNH 伴溶血性贫血患者,患者人群与美国相似。此次批准是基于 PEGASUS 研究和 PRINCE 研究的结果,与 C5 抑制剂依库珠单抗相比,Pegcetacoplan 可改善正在接受依库珠单抗治疗的贫血患者的血红蛋白水平,在 PEGASUS 研究中具有优越性;与支持治疗相比,Pegcetacoplan 可稳定血红蛋白水平,并降低补体抑制剂初治患者的乳酸脱氢酶水平,在 PRINCE 研究中具有优越性。鉴于 EMA 最近扩大了适应证,本文将描述 Pegcetacoplan 的强大疗效与其作用机制之间的关联,该作用机制可广泛控制血管内和血管外溶血,从而改善一系列疾病标志物并提高患者的生活质量。此外,还总结了 Pegcetacoplan 上市 3 年来获得的额外数据和经验,包括长期疗效和安全性结果、真实世界的临床经验、药代动力学特征,以及对 PNH 的首个上市的近端补体抑制剂的广泛实用指导。