培克珠单抗(Pexelizumab) - 药物靶点：C5_专利_临床

概要

基本信息

药物类型

单克隆抗体

别名

Anti-C5 monoclonal antibody 5G1-1-SC、Monoclonal antibody 5G1.1-SC、Pexelizumab (USAN/INN)

+ [3]

靶点

C5

作用方式

抑制剂

作用机制

C5抑制剂(补体C5抑制剂)

治疗领域

心血管疾病其他疾病

在研适应症-

非在研适应症

急性心肌梗塞冠心病心肌梗塞+ [1]

原研机构

Stanford University

在研机构-

非在研机构

Procter & Gamble, Inc.

Alexion Pharmaceuticals, Inc.

Stanford University

权益机构

Alexion Pharmaceuticals, Inc.

Procter & Gamble Co.

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

Sequence Code 561758592

来源: *****

关联

3

项与培克珠单抗相关的临床试验

NCT00088179

/ Completed临床3期

A Multicenter, Randomized, Double-Blind, Parallel-group, Placebo-Controlled Study of Pexelizumab in Patients Undergoing Coronary Artery Bypass Grafting With Cardiopulmonary Bypass (PRIMO-CABG II)

During a heart bypass procedure, a substance called "complement" is activated by the body. This "complement activation" causes an inflammatory response that can lead to side affects such as chest pain, heart attacks, stroke, heart failure, or death. The purpose of this study is to find out if the study drug (pexelizumab), that blocks "complement activation," can reduce such side effects and be given safely to patients requiring the bypass procedure with the use of the heart-lung machine.

开始日期2004-07-01

申办/合作机构

Alexion Pharmaceuticals, Inc.

[+1]

NCT00091637

/ Completed临床3期

APEX-AMI - Pexelizumab in Conjunction With Angioplasty

In the setting of reperfusion therapy in an acute myocardial infarction using primary percutaneous intervention (PCI), the body's own inflammatory system involving the complement cascade may be harmful. This study will test the safety and efficacy of a novel complement inhibitor, pexelizumab to reduce mortality at 30 days.

开始日期2004-04-01

申办/合作机构

Procter & Gamble, Inc.

NCT00048308

/ Completed临床3期

Effect of Pexelizumab on All-Cause Mortality and Myocardial Infarction in Patients Undergoing Coronary Artery Bypass Graft Surgery With Cardio-Pulmonary Bypass

During a heart bypass procedure, a substance called "complement" is released by the body. This complement causes inflammation, which can lead to side effects such as chest pain, heart attacks, heart failure, or impairment of memory, language and motor skills. The purpose of this study is to find out if the study drug (pexelizumab), which blocks complement release, can reduce such side effects and be taken safely.

开始日期2002-01-01

申办/合作机构

Alexion Pharmaceuticals, Inc.

100 项与培克珠单抗相关的临床结果

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100 项与培克珠单抗相关的转化医学

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100 项与培克珠单抗相关的专利（医药）

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75

项与培克珠单抗相关的文献（医药）

2025-09-01·ATHEROSCLEROSIS

Early anti-inflammatory therapy in acute myocardial infarction: A network meta-analysis of timing-dependent effects in 23 randomized trials and 28,220 patients

Article

作者: Saldaña-García, Jesús ; Rivero-Santana, Borja ; Jurado-Román, Alfonso ; Cantolla-Pablo, Paula ; Moreno, Raúl ; Gil-Fernández, Marta ; Tardif, Jean-Claude ; Fernández-Velasco, María ; López-Sendón, José

BACKGROUND AND AIMS:

The timing of anti-inflammatory therapy in acute myocardial infarction (AMI) may be critical, yet has not been systematically assessed. While several agents have shown benefit in secondary prevention, their efficacy during the early inflammatory phase of AMI remains uncertain. This study evaluated the effectiveness of anti-inflammatory therapies in AMI and whether early initiation within 24 h of symptom onset modifies clinical outcomes.

METHODS:

We conducted a network meta-analysis of 23 randomized controlled trials including 28,220 patients with AMI. Interventions included colchicine, anakinra (IL-1β inhibitor), tocilizumab (IL-6 inhibitor), varespladib (PLA2 inhibitor), losmapimod (p38 MAPK inhibitor), cyclosporine (mitochondrial pore inhibitor), and pexelizumab (complement C5 inhibitor). Primary outcomes were major adverse cardiovascular events (MACE), heart failure (HF), and ischemic events. Treatment effects were summarized as incidence rate ratios (IRRs), defined as the ratio of incidence rates between intervention and control groups. Subgroup analyses stratified trials by treatment initiation ≤24 h vs > 24 h from symptom onset.

RESULTS:

Colchicine significantly reduced MACE ([IRR] 0.71; 95 % confidence interval [CI] 0.53-0.97) and ischemic events (IRR 0.65; 95 % CI 0.43-0.98). Anakinra reduced HF events (IRR 0.38; 95 % CI 0.16-0.89). These effects were observed exclusively when treatment was initiated within 24 h. No benefit was seen with delayed therapy, and no other intervention showed clinical efficacy. Safety outcomes, including infection risk, were neutral across treatments.

CONCLUSIONS:

This network meta-analysis demonstrates that anti-inflammatory therapy improves outcomes in AMI only when initiated early. Colchicine and anakinra were the only effective agents, highlighting a narrow therapeutic window and supporting a time-sensitive approach to inflammation-targeted treatment in AMI.

2025-01-01·Acta Medica Indonesiana

Anti-inflammatory Therapy Before Reperfusion Therapy in Patients with Ischemic Vascular Disease on the Incidence of Ischemic Reperfusion Injury: An Evidence-Based Case Report.

Review

作者: Utami, Nindya P B S ; Antono, Dono ; Gautama, Ade

BACKGROUND:

Reperfusion serves as a mainstay therapy in almost all ischemic vascular diseases (IVD), but reperfusion may enhance cell damage after an ischemic period time. Increased ROS and inflammatory markers, decreasing organ function parameters, along with systemic inflammatory response and multi-organ damage may occur in ischemic reperfusion injury (IRI). Unfortunately, this series of events is unpredictable and sudden, causing high mortality in patients with IRI. Due to the significant role of inflammation in IRI, how is the effectiveness of anti-inflammatory agents administered before reperfusion therapy to prevent IRI? To know the efficacy of anti-inflammatory agents administered before reperfusion therapy to prevent IRI.

METHODS:

A systematic search was conducted in databases (Pubmed, EMBASE, Scopus) and was later selected according to predetermined inclusion and exclusion criteria. Studies included later critically appraised using the CEBM Oxford questionnaire for randomized control trials and systematic review.

RESULTS:

Seven studies were included among 1072 studies found in early searching. Six of the studies are randomized control trials, and one is a meta-analysis of randomized control trials. Methylprednisolone, pexelizumab, tirilazad mesylate, and N-acetylcysteine are known anti-inflammatory agents applicable in humans. The highest effectiveness of anti-inflammatory agents is methylprednisolone, with a relative risk reduction (RRR) of 75-85%. Besides that, pexelizumab also had an RRR of 27%, and tirilazad-mesylate had an RRR of 18%. N-acetylcysteine is not effective in preventing IRI. IL-6 levels postoperatively also decreased significantly in patients given anti-inflammatory agents before reperfusion therapy. There are no side effects of the intervention reported.

CONCLUSION:

Anti-inflammatory agent administration before reperfusion therapy effectively prevents IRI. The choices of anti-inflammatory agents recommended are methylprednisolone, pexelizumab, and tirilazad-mesylate. Anti-inflammatory agent administration before reperfusion therapy is recommended.

2022-06-01·BMJ open

Examining anti-inflammatory therapies in the prevention of cardiovascular events: protocol for a systematic review and network meta-analysis of randomised controlled trials

Article

作者: Geejo, Aishwarya ; Pearson, Alexander Liam ; Shin, Sheojung ; Beanlands, Rob ; Wells, George A ; Fehlmann, Christophe A ; Shahab, Saba ; Visintini, Sarah ; Bezzina, Kathryn A ; Boczar, Kevin Emery

Introduction:

Inflammation is emerging as an important risk factor for atherosclerotic cardiovascular disease and has been a recent target for many novel therapeutic agents. However, comparative evidence regarding efficacy of these anti-inflammatory treatment options is currently lacking.

Methods and analysis:

This systematic review will include randomised controlled trials evaluating the effect of anti-inflammatory agents on cardiovascular outcomes in patients with known cardiovascular disease. Studies will be retrieved from Medline, Embase, the Cochrane Central Register of Controlled Trials, as well as clinical trial registry websites, Europe PMC and conference abstract handsearching. No publication date or language restrictions will be imposed. Eligible interventions must have some component of anti-inflammatory agent. These include (but are not limited to): non-steroidal anti-inflammatory drugs (NSAIDs), colchicine, prednisone, methotrexate, canakinumab, pexelizumab, anakinra, succinobucol, losmapimod, inclacumab, atreleuton, LP-PLA 2 (darapladib) and sPLA 2 (varespladib). The primary outcomes will include major adverse cardiac events (MACE), and each individual component of MACE (myocardial infarction, stroke and cardiovascular death). Key secondary outcomes will include unstable angina, heart failure, all-cause mortality, cardiac arrest and revascularisation. Screening, inclusion, data extraction and quality assessment will be performed independently by two reviewers. Network meta-analysis based on the random effects model will be conducted to compare treatment effects both directly and indirectly. The quality of the evidence will be assessed with appropriate tools including the Grading of Recommendations, Assessment, Development and Evaluation profiler or Confidence in Network Meta-Analysis tool.

Ethics and dissemination:

Ethics approval is not required for this systematic review. The findings will be disseminated through a peer-reviewed journal.

PROSPERO registration number:

CRD42022303289.

1

项与培克珠单抗相关的新闻（医药）

2025-12-22

·医心向学

炎症，心血管疾病的“残余风险”：权威综述深度解读抗炎药物治疗新进展

心血管疾病（CVD）依然是全球范围内导致发病和死亡的首要原因，给医疗体系带来了沉重负担。除了高血压、高胆固醇血症和糖尿病等传统的危险因素外，越来越多的证据表明，炎症在心血管疾病的发生、发展和并发症中扮演着核心角色。血液中升高的炎性生物标志物（如高敏C反应蛋白、白介素等）与疾病严重程度和不良预后密切相关。近日，《European Heart Journal ‐ Cardiovascular Pharmacotherapy》杂志发表了一篇权威综述，对心血管疾病患者的抗炎药物治疗进行了系统性梳理和深入解读。这篇综述认为，随着证据的积累，炎症可能正从心血管疾病管理的辅助靶点，转变为一个中心焦点。抗炎药物在心血管疾病中的药代动力学和药效学综述核心内容：靶向炎症的实践与争议一、稳定冠心病：秋水仙碱的肯定与生物制剂的局限在稳定型冠状动脉疾病（CAD）患者中，即使接受了优化标准的降脂、抗血栓和抗缺血治疗，残余心血管风险依然存在。持续的低度慢性血管炎症被认为是推动动脉粥样硬化进展及其血栓并发症的关键因素。秋水仙碱（Colchicine）：秋水仙碱因其抑制中性粒细胞功能和更广泛的细胞抗炎作用，受到了广泛关注。确切的临床益处： LoDoCo2等大型随机对照试验（RCTs）证实，对于稳定型CAD患者，每日服用低剂量秋水仙碱（0.5 mg）可以显著降低主要心血管事件（MACE）的风险，这主要归因于自发性心肌梗死（MI）和缺血驱动的血运重建发生率的降低。指南推荐：基于多项试验结果，欧洲指南已将低剂量秋水仙碱（0.5 mg/天）纳入IIa类推荐，用于降低稳定型CAD患者的心肌梗死、卒中和血运重建风险。挑战：约11%至15%的患者因胃肠道不耐受而中止治疗，但总体的Meta分析显示其在这一剂量下安全性良好。白介素抑制剂（IL Inhibitors）与甲氨蝶呤： Canakinumab（抗IL-1β）：在CANTOS试验中，该药在不影响低密度脂蛋白胆固醇水平的情况下，独立降低了高风险患者（高敏C反应蛋白≥2 mg/L）的MACE风险。这被认为是第一个直接支持动脉粥样硬化炎症假说的里程碑式证据。然而，由于其高昂的成本以及试验中观察到的败血症和致命感染发生率增加，Canakinumab尚未获批用于心肌梗死后的二级预防。甲氨蝶呤（Methotrexate）：这种叶酸拮抗剂在CIRT试验中未能显示出心血管益处，暗示抗炎治疗之间并不存在明确的“类效应”。这可能与甲氨蝶呤未能充分调节动脉粥样硬化中的关键炎症通路有关。新兴的靶向策略——IL-6抑制：目前研究正转向更具选择性的抗炎策略，如靶向白介素-6（IL-6）的抑制剂Ziltivekimab。IL-6被认为是动脉粥样硬化相关炎症的核心介质。该药已在慢性肾脏病（CKD）和持续炎症的高危人群（RESCUE试验）中显示出剂量依赖性的高敏C反应蛋白显著降低，且安全性良好，这为正在进行的大型III期临床试验（如ZEUS试验）提供了理论基础。二、急性冠脉综合征（ACS）：时机与剂量引发的争议在急性冠脉综合征（ACS）中，斑块破裂会引发急性和持续的炎症级联反应，促进血栓形成和心肌损伤。寻找在急性期有效的抗炎疗法极具挑战性。秋水仙碱的复杂证据：早期积极结果： COLCOT试验（纳入近期心梗患者）显示，秋水仙碱显著降低了主要复合终点，主要归因于卒中和因心绞痛进行紧急血运重建的减少。近期大型试验的冲突：然而，CLEAR试验（纳入7062名急性心肌梗死患者，大部分为ST段抬高型心肌梗死）的结果是中性的，秋水仙碱对主要复合疗效终点没有显著影响，尽管它确实降低了C反应蛋白水平。未解决的疑问：试验结果的冲突可能与用药时机（过早用药可能干扰急性修复机制）和剂量（0.5 mg/天的方案可能在ACS高炎症负荷下不足）有关。欧洲指南根据COLCOT试验的结果，允许选择性地考虑使用秋水仙碱（IIb类推荐），但预计在CLEAR试验发布后，指南可能会更加严格，至少对于ST段抬高型心肌梗死患者如此。其他靶点探索的失败：针对补体成分C5的Pexelizumab和p38丝裂原活化蛋白激酶抑制剂Losmapimod等抗炎策略在ACS试验中均未能持续显示出显著的临床益处。 IL-6抑制剂的希望：与IL-1抑制（可能影响广泛的免疫细胞并增加感染风险）不同，IL-6抑制被认为更具选择性。目前，大型III期ARTEMIS试验正在评估IL-6抑制剂Ziltivekimab在近期急性心肌梗死患者中的临床效果。研究人员热切期待ARTEMIS试验结果，它可能揭示IL-6的下游抑制是否能在ACS中提供安全性和有效性的理想平衡。三、心力衰竭与其他疾病谱：靶向炎症的漫长征程心力衰竭（HF）：炎症通过驱动心肌纤维化、肥大和功能障碍，在心力衰竭（HF）的发生和进展中起着重要作用。尽管存在强烈的机制理论支持，但针对心力衰竭的抗炎治疗试验（包括靶向肿瘤坏死因子-α或TNF-α的英夫利昔单抗/依那西普，以及非选择性药物秋水仙碱和甲氨蝶呤）大多得到了阴性或不确定的结果，甚至有些治疗（如高剂量TNF-α抑制剂）还与更高的死亡率相关。目前，IL-6抑制剂Ziltivekimab的HERMES和ATHENA等大型III期试验正在进行中，旨在明确更具针对性的方法是否能为射血分数保留性心力衰竭（HFpEF）患者带来临床益处。瓣膜性心脏病：炎症是主动脉瓣狭窄（AS）发病机制的关键因素。尽管目前尚无获批的药物，但遗传学数据表明，通过Tocilizumab实现的遗传学上的IL-6抑制与主动脉狭窄风险降低有关。秋水仙碱的小型试验（如CHIANTI和COPAS试验）正在探索其是否能延缓轻度至中度AS患者的瓣膜钙化和疾病进展。心包炎与心肌炎：与上述疾病不同，炎症在心包炎的治疗中具有明确的核心地位。非甾体抗炎药和秋水仙碱是急性和复发性心包炎的一线治疗基石。对于难治性病例，IL-1α/β抑制剂Rilonacept等新型生物制剂已显示出显著减少复发的作用。对于心肌炎，治疗方案仍多基于专家共识，针对病因学的特异性靶向治疗是未来的研究方向。结论：个性化、多靶点与选择性抑制的未来炎症作为心血管疾病的中心致病机制，这一范式转变正推动治疗从广谱药物（如秋水仙碱）向更具选择性、路径特异性的干预措施发展。当前，秋水仙碱是唯一被推荐用于CAD二级预防的抗炎药，但在ACS中的地位仍存在不确定性，未来的指南可能会调整。其他广谱或早期的靶向治疗（如Canakinumab、TNF-α抑制剂）因安全性和成本效益等问题而面临局限。未来心血管抗炎策略将朝着以下方向发展：选择性靶向：以IL-6抑制剂Ziltivekimab为代表的靶向策略，因其在安全性和有效性之间可能提供更好的平衡，成为目前最受期待的进展。个性化与时机优化：识别最可能受益的患者亚组，并确定最佳的给药剂量和时机，以避免干扰炎症在某些情境下的生理修复作用。多靶点联合干预：未来的方法可能采纳整合炎症控制与降脂、抗血栓治疗的个性化、多靶点方案。随着ARTEMIS、ZEUS、HERMES等大型关键试验结果的公布，抗炎药物有望在心血管疾病管理中发挥更清晰、更重要的作用。参考文献： Simone Finocchiaro, Placido Maria Mazzone, Nicola Ammirabile, et al., and Davide Capodanno. Anti-inflammatory pharmacotherapy in patients with cardiovascular disease. European Heart Journal ‐ Cardiovascular Pharmacotherapy (2025) 11, 712–728. 免责声明：本文内容旨在介绍医学研究进展，文章中提及的所有药物和治疗方案，其临床应用均应遵循最新的医学指南，并在专业医师指导下进行。本文不构成任何医疗建议或诊疗指导。关键词： # #心血管疾病# #炎症# #抗炎药# #秋水仙碱# #白介素抑制剂# #冠心病# #心力衰竭#

100 项与培克珠单抗相关的药物交易

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D10023	培克珠单抗	-	DB04949

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
急性心肌梗塞	临床3期	美国	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	澳大利亚	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	奥地利	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	比利时	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	加拿大	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	捷克	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	丹麦	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	法国	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	德国	Procter & Gamble, Inc.	2004-04-01
急性心肌梗塞	临床3期	意大利	Procter & Gamble, Inc.	2004-04-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00091637 (APEX-AMI, Pubmed \| Am Heart J)	临床3期	ST段抬高心肌梗死	5,745	Pexelizumab (LVEDP ≤ 22 mm Hg)	鏇遞鬱遞鑰襯餘鹽製鬱(獵窪壓餘願鹽範鏇壓選) = 鏇獵觸願壓艱夢遞糧壓襯獵製膚膚廠製獵膚鹹 (鑰遞製糧築選築淵蓋製 )	-	2013-11-01
NCT00091637 (APEX-AMI, Pubmed \| Am Heart J)	临床3期	心肌梗塞	5,745	Pexelizumab (Aborted MI)	艱築觸網糧築壓繭網衊(淵壓積鑰築簾淵糧憲積) = 醖觸廠獵網築醖夢齋鬱簾鬱鑰鬱齋願觸積簾淵 (觸餘衊選繭壓廠艱選憲 ) 更多	-	2013-02-01
				Pexelizumab (MI)	艱築觸網糧築壓繭網衊(淵壓積鑰築簾淵糧憲積) = 選繭鏇鑰餘遞鹹膚夢餘簾鬱鑰鬱齋願觸積簾淵 (觸餘衊選繭壓廠艱選憲 ) 更多
NCT00088179 (PRIMO-CABG I and II, Pubmed \| J Thorac Cardiovasc Surg) 人工标引	临床3期	心血管疾病	4,254	Pexelizumab (The PRIMO-CABG II trial)	襯廠鏇糧膚艱遞選襯願(簾蓋鬱夢選範夢壓醖鏇) = The PRIMO-CABG II trial did not meet its prespecified primary endpoint of death or MI at 30 days 鏇夢範網築衊蓋廠蓋艱 (製壓鹽顧構網壓鬱範鏇 ) 未达到更多	不佳	2011-07-01
				Placebo (The PRIMO-CABG II trial)
NCT00091637 (Assessment of Pexelizumab in Acute Myocardial Infarction, Pubmed \| Circ Cardiovasc Qual Outcomes)	临床3期	急性心肌梗塞	5,745	Pexelizumab (Symptom onset-to-balloon time)	窪網積鹽鹹範觸夢簾願(鹽製鬱積醖簾觸獵糧鬱) = 憲膚獵鏇衊鹽繭網襯壓醖獵糧衊糧窪鑰壓範製 (製淵餘鹹鏇夢艱鏇選壓 )	-	2011-03-01
				Pexelizumab (Door-to-balloon time)	夢鏇衊構鬱遞鬱衊膚範(鹹齋艱襯積顧膚範夢襯) = 窪構窪製網築願鏇鹽膚網鏇艱餘壓鹹夢餘製鏇 (範蓋願簾窪醖艱製夢餘 )
NCT00091637 (APEX-AMI, Pubmed \| JACC Cardiovasc Imaging)	临床3期	急性心肌梗塞	5,745	Pexelizumab	膚鹽鑰蓋壓憲鏇壓簾鑰(繭鏇鏇遞齋獵積獵製網) = 夢窪選鹹鹹廠餘選選淵築獵夢遞鹽鬱鏇觸淵窪 (繭齋窪艱範網願蓋餘積 ) 更多	-	2010-01-01
				Placebo	膚鹽鑰蓋壓憲鏇壓簾鑰(繭鏇鏇遞齋獵積獵製網) = 鑰齋壓簾築膚簾觸鹹窪築獵夢遞鹽鬱鏇觸淵窪 (繭齋窪艱範網願蓋餘積 ) 更多
NCT00091637 (APEX-AMI, Pubmed \| Am Heart J)	临床3期	ST段抬高心肌梗死	5,745	Pexelizumab (Angiographic reperfusion)	製構淵襯鬱觸憲艱鬱鑰(範襯獵齋構鑰選鏇顧簾) = 淵壓願襯願鹹襯構築淵憲壓網夢膚鏇積醖壓範 (艱壓鏇顧窪膚築鏇積觸 )	-	2009-11-01
NCT00091637 (Pubmed \| JAMA) 人工标引	临床3期	ST段抬高心肌梗死	5,745	Pexelizumab	鹹艱艱構鹽鹹築窪膚淵(觸糧繭膚蓋廠壓膚蓋顧) = 鹹壓廠淵鹽鏇鬱遞選鏇繭積鹽獵壓齋壓獵夢選 (築壓網膚醖壓築壓淵網 ) 更多	不佳	2007-01-03
				Placebo	鹹艱艱構鹽鹹築窪膚淵(觸糧繭膚蓋廠壓膚蓋顧) = 壓醖衊繭壓繭餘齋顧鹹繭積鹽獵壓齋壓獵夢選 (築壓網膚醖壓築壓淵網 ) 更多