Eculizumab
(Synonyms: 依库珠单抗; Anti-Human C5, Humanized Antibody) 目录号 : GC64796
Eculizumab (Anti-Human C5, Humanized Antibody) 是一种针对补体 C5 (complement C5) 的长效人源化单克隆抗体。Eculizumab 抑制 C5 裂解为 C5a 和 C5b，因此抑制末端补体系统的部署，包括膜攻击复合物 (MAC) 的形成。Eculizumab 具有用于溶血研究的潜力。
Cas No.:219685-50-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
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Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Eculizumab (Anti-Human C5, Humanized Antibody) is a long-acting humanized monoclonal antibody targeted against complement C5. Eculizumab inhibits the cleavage of C5 into C5a and C5b and hence inhibits deployment of the terminal complement system including the formation of membrane attack complex (MAC). Eculizumab has the potential for haemolysis research[1].
[1]. Eline A Dubois,et al. Eculizumab. Br J Clin Pharmacol. 2009 Sep;68(3):318-9.
| Cas No. | 219685-50-4 | SDF | Download SDF |
| 别名 | 依库珠单抗; Anti-Human C5, Humanized Antibody | ||
| 分子式 | 分子量 | ||
| 溶解度 | 储存条件 | Store at -80°C | |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pegcetacoplan versus Eculizumab in Paroxysmal Nocturnal Hemoglobinuria
N Engl J Med 2021 Mar 18;384(11):1028-1037.PMID:33730455DOI:10.1056/NEJMoa2029073.
Background: Paroxysmal nocturnal hemoglobinuria (PNH) is a rare, acquired disease characterized by chronic complement-mediated hemolysis. C5 inhibition controls intravascular hemolysis in untreated PNH but cannot address extravascular hemolysis. Pegcetacoplan, a pegylated peptide targeting proximal complement protein C3, potentially inhibits both intravascular and extravascular hemolysis. Methods: We conducted a phase 3 open-label, controlled trial to assess the efficacy and safety of pegcetacoplan as compared with Eculizumab in adults with PNH and hemoglobin levels lower than 10.5 g per deciliter despite Eculizumab therapy. After a 4-week run-in phase in which all patients received pegcetacoplan plus Eculizumab, we randomly assigned patients to subcutaneous pegcetacoplan monotherapy (41 patients) or intravenous Eculizumab (39 patients). The primary end point was the mean change in hemoglobin level from baseline to week 16. Additional clinical and hematologic markers of hemolysis and safety were assessed. Results: Pegcetacoplan was superior to Eculizumab with respect to the change in hemoglobin level from baseline to week 16, with an adjusted (least squares) mean difference of 3.84 g per deciliter (P<0.001). A total of 35 patients (85%) receiving pegcetacoplan as compared with 6 patients (15%) receiving Eculizumab no longer required transfusions. Noninferiority of pegcetacoplan to Eculizumab was shown for the change in absolute reticulocyte count but not for the change in lactate dehydrogenase level. Functional Assessment of Chronic Illness Therapy-Fatigue scores improved from baseline in the pegcetacoplan group. The most common adverse events that occurred during treatment in the pegcetacoplan and Eculizumab groups were injection site reactions (37% vs. 3%), diarrhea (22% vs. 3%), breakthrough hemolysis (10% vs. 23%), headache (7% vs. 23%), and fatigue (5% vs. 15%). There were no cases of meningitis in either group. Conclusions: Pegcetacoplan was superior to Eculizumab in improving hemoglobin and clinical and hematologic outcomes in patients with PNH by providing broad hemolysis control, including control of intravascular and extravascular hemolysis. (Funded by Apellis Pharmaceuticals; PEGASUS ClinicalTrials.gov, NCT03500549.).
Eculizumab in atypical hemolytic uremic syndrome: strategies toward restrictive use
Pediatr Nephrol 2019 Nov;34(11):2261-2277.PMID:30402748DOI:10.1007/s00467-018-4091-3.
With the introduction of the complement C5-inhibitor Eculizumab, a new era was entered for patients with atypical hemolytic uremic syndrome (aHUS). Eculizumab therapy very effectively reversed thrombotic microangiopathy and reduced mortality and morbidity. Initial guidelines suggested lifelong treatment and recommended prophylactic use of Eculizumab in aHUS patients receiving a kidney transplant. However, there is little evidence to support lifelong therapy or prophylactic treatment in kidney transplant recipients. Worldwide, there is an ongoing debate regarding the optimal dose and duration of treatment, particularly in view of the high costs and potential side effects of Eculizumab. An increasing but still limited number of case reports and small cohort studies suggest that a restrictive treatment regimen is feasible. We review the current literature and focus on the safety and efficacy of restrictive use of Eculizumab. Our current treatment protocol is based on restrictive use of Eculizumab. Prospective monitoring will provide more definite proof of the feasibility of such restrictive treatment.
Eculizumab and aHUS: to stop or not
Blood 2021 May 6;137(18):2419-2420.PMID:33956069DOI:10.1182/blood.2020010234.
In this issue of Blood, Fakhouri et al provide evidence in a prospective phase 4, multicentric, noncontrolled study that discontinuing Eculizumab is safe in most patients with atypical hemolytic uremic syndrome (aHUS) once they achieve complete remission. Risk of relapse was <25% overall, but as high as 50% in patients with a rare variant in at least 1 complement gene.
Eculizumab treatment for myasthenia gravis subgroups: 2021 update
J Neuroimmunol 2022 Jan 15;362:577767.PMID:34823117DOI:10.1016/j.jneuroim.2021.577767.
Eculizumab is a recombinant humanized monoclonal antibody that targets the complement protein C5, inhibiting its cleavage into C5a and C5b and ultimately preventing the formation of C5b-9 membrane attack complex (MACs), thereby protecting the neuromuscular junction from the damage of complement activation. In 2017, Eculizumab became the second FDA-approved medication for AchR-positive generalized myasthenia gravis (gMG) patients based on the successful results of a randomized, double-blinded, placebo-controlled, phase 2, phase 3 study (the REGAIN trial) and its open-label extension study. Despite the efficacy of Eculizumab in treating AchR antibody-positive refractory gMG was demonstrated in the REGAIN study, there is few information on its efficacy in other subgroup of MG patients including seronegative MG, thymoma-associated MG and MG crisis. This narrative review summarizes current clinical studies of Eculizumab in these refractory gMG patients, with a focus on the therapeutic efficacy and tolerability in different subgroup of MG.
Ravulizumab (ALXN1210) vs Eculizumab in C5-inhibitor-experienced adult patients with PNH: the 302 study
Blood 2019 Feb 7;133(6):540-549.PMID:30510079DOI:10.1182/blood-2018-09-876805.
Ravulizumab, a new complement component C5 inhibitor administered every 8 weeks, was noninferior to Eculizumab administered every 2 weeks in complement-inhibitor-naive patients with paroxysmal nocturnal hemoglobinuria (PNH). This study assessed noninferiority of ravulizumab to Eculizumab in clinically stable PNH patients during previous Eculizumab therapy. In this phase 3, open-label, multicenter study, 195 PNH patients on labeled-dose (900 mg every 2 weeks) Eculizumab for >6 months were randomly assigned 1:1 to switch to ravulizumab (n = 97) or continue Eculizumab (n = 98). Primary efficacy end point was percentage change in lactate dehydrogenase (LDH) from baseline to day 183. Key secondary end points included proportion of patients with breakthrough hemolysis, change in Functional Assessment of Chronic Illness Therapy (FACIT)-Fatigue score, transfusion avoidance, and stabilized hemoglobin. In 191 patients completing 183 days of treatment, ravulizumab was noninferior to Eculizumab (P inf < .0006 for all end points), including percentage change in LDH (difference, 9.21% [95% confidence interval (CI), -0.42 to 18.84], P = .058 for superiority), breakthrough hemolysis (difference, 5.1 [95% CI, -8.89 to 18.99]), change in FACIT-Fatigue score (difference, 1.47 [95% CI, -0.21 to 3.15]), transfusion avoidance (difference, 5.5 [95% CI, -4.27 to 15.68]), and stabilized hemoglobin (difference, 1.4 [95% CI, -10.41 to 13.31]). The most frequently reported adverse event was headache (26.8%, ravulizumab; 17.3%, Eculizumab). No meningococcal infections or discontinuations due to adverse events occurred. Patients with PNH may be safely and effectively switched from labeled-dose Eculizumab administered every 2 weeks to ravulizumab administered every 8 weeks. This trial was funded by Alexion Pharmaceuticals, Inc., and is registered at www.clinicaltrials.gov as #NCT03056040.