Canakinumab
(Synonyms: Ilaris; ACZ 885) 目录号 : GC66328
Canakinumab (ACZ885) 是一种重组的人抗 IL-1β 单克隆抗体。Canakinumab 显示出对人类和绒猴 IL-1β 的 IC50 值为分别为 43.6 和 40.8 pM。Canakinumab 的作用模式是基于对 IL-1β 信号的中和，从而抑制与自身免疫性疾病相关的炎症。
Cas No.:914613-48-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 43.6 pM (human IL-1β), 40.8 pM (marmoset IL-1β)[2]
Canakinumab (ACZ885) is a recombinant human anti-IL-1β monoclonal antibody. Canakinumab shows IC50 values of 43.6 and 40.8 pM for human and marmoset IL-1β, respectively. The mode of action of canakinumab is based on the neutralization of IL-1β signaling, resulting in suppression of inflammation related to disorders of autoimmune origin[1][2].
Canakinumab (0-7 nM) dose dependently represses IL-6 production in marmoset peripheral blood mononuclear cells with IC50s of 43.6 and 40.8 pM for human and marmoset IL-1β[2].Canakinumab effectively competes with IL-1RI and IL-1RII for binding to IL-1b[2].
| Cas No. | 914613-48-2 | SDF | Download SDF |
| 别名 | Ilaris; ACZ 885 | ||
| 分子式 | 分子量 | 145.5 kDa | |
| 溶解度 | 储存条件 | Store at -20°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。 |
||
| 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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 6.8729 mL | 34.3643 mL | 68.7285 mL |
| 5 mM | 1.3746 mL | 6.8729 mL | 13.7457 mL |
| 10 mM | 0.6873 mL | 3.4364 mL | 6.8729 mL |
| 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。
Canakinumab for the Treatment of Autoinflammatory Recurrent Fever Syndromes
N Engl J Med 2018 May 17;378(20):1908-1919.PMID:29768139DOI:10.1056/NEJMoa1706314.
Background: Familial Mediterranean fever, mevalonate kinase deficiency (also known as the hyperimmunoglobulinemia D syndrome), and the tumor necrosis factor receptor-associated periodic syndrome (TRAPS) are monogenic autoinflammatory diseases characterized by recurrent fever flares. Methods: We randomly assigned patients with genetically confirmed colchicine-resistant familial Mediterranean fever, mevalonate kinase deficiency, or TRAPS at the time of a flare to receive 150 mg of Canakinumab subcutaneously or placebo every 4 weeks. Patients who did not have a resolution of their flare received an add-on injection of 150 mg of Canakinumab. The primary outcome was complete response (resolution of flare and no flare until week 16). In the subsequent phase up to week 40, patients who had a complete response underwent a second randomization to receive Canakinumab or placebo every 8 weeks. Patients who underwent a second randomization and had a subsequent flare and all other patients received open-label Canakinumab. Results: At week 16, significantly more patients receiving Canakinumab had a complete response than those receiving placebo: 61% vs. 6% of patients with colchicine-resistant familial Mediterranean fever (P<0.001), 35% versus 6% of those with mevalonate kinase deficiency (P=0.003), and 45% versus 8% of those with TRAPS (P=0.006). The inclusion of patients whose dose was increased to 300 mg every 4 weeks yielded a complete response in 71% of those with colchicine-resistant familial Mediterranean fever, 57% of those with mevalonate kinase deficiency, and 73% of those with TRAPS. After week 16, an extended dosing regimen (every 8 weeks) maintained disease control in 46% of patients with colchicine-resistant familial Mediterranean fever, 23% of those with mevalonate kinase deficiency, and 53% of those with TRAPS. Among patients who received Canakinumab, the most frequently reported adverse events were infections (173.3, 313.5, and 148.0 per 100 patient-years among patients with colchicine-resistant familial Mediterranean fever, those with mevalonate kinase deficiency, and those with TRAPS, respectively), with a few being serious infections (6.6, 13.7, and 0.0 per 100 patient-years). Conclusions: In this trial, Canakinumab was effective in controlling and preventing flares in patients with colchicine-resistant familial Mediterranean fever, mevalonate kinase deficiency, and TRAPS. (Funded by Novartis; CLUSTER ClinicalTrials.gov number, NCT02059291 .).
Canakinumab
MAbs 2010 Jan-Feb;2(1):3-13.PMID:20065636DOI:10.4161/mabs.2.1.10328.
Canakinumab (ACZ885, Ilaris) is a human anti-IL-1beta monoclonal antibody developed by Novartis. Its mode of action is based on the neutralization of IL-1beta signaling, resulting in suppression of inflammation in patients with disorders of autoimmune origin. In June 2009 the drug was approved by the US Food and Drug Administration for the treatment of familial cold auto-inflammatory syndrome and Muckle-Wells syndrome, which are inflammatory diseases related to cryopyrin-associated periodic syndromes. The drug is currently being evaluated for its potential in the treatment of rheumatoid arthritis, systemic-onset juvenile idiopathic arthritis, chronic obstructive pulmonary disease, type 1 and 2 diabetes and ocular diseases. Reports from clinical trials suggest that Canakinumab is well-tolerated in most patients, and no serious adverse effects have been reported. The drug provides significant advantages over existing competitive therapies, including bimonthly administration and approved use in children.
Canakinumab for secondary prevention of coronary artery disease
Future Cardiol 2021 May;17(3):427-442.PMID:33533289DOI:10.2217/fca-2020-0211.
Cardiovascular disease manifestations (CVD) are the world's leading cause of death, and their impact on morbidity requires effective prevention strategies of recurrent adverse events. For decades, inflammation has been proposed as a key promoter for atherosclerosis and its complications. However, studies on the use of drugs to target the excess inflammation in CVD are limited. In 2017, the Canakinumab Anti-inflammatory Thrombosis Outcome Study (CANTOS) trial confirmed the key role of inflammation on atherosclerotic disease. Canakinumab is a monoclonal antibody that blocks an inflammatory pathway mediated by IL-1β. The results of the CANTOS trial opened a new era of investigating new therapeutics targeting inflammation for CVD secondary prevention. This review presents the Canakinumab's pharmacology, current clinical development status and regulatory perspectives.
Canakinumab for the treatment of adult-onset Still's disease
Expert Rev Clin Immunol 2020 Feb;16(2):129-138.PMID:31957508DOI:10.1080/1744666X.2019.1707664.
Introduction: Adult-onset Still's disease (AOSD) is a rare multisystem autoinflammatory disorder of unknown etiology, with clinical and biological similarities with the juvenile form (sJIA).The pivotal role of interleukin (IL)-1 gives rise to the use of IL-1 inhibitors in treating resistant cases.Areas covered: This review focuses on Canakinumab, a fully human anti-IL-1β antibody, as treatment for AOSD. The data obtained from case reports and case series on AOSD and two double-blind, randomized, placebo-controlled Phase III trial on sJIA are analyzed. Efficacy and safety profiles of Canakinumab are discussed.Expert opinion: There is no unanimous consensus on how to treat with IL-1 inhibitors. Many reviews have focused primarily on anakinra, but the accumulating data for Canakinumab have emerged. The choice of treatment is a relevant issue for patients and the national health services. The available data for Canakinumab indicate that this drug in AOSD patients is effective and well tolerated.
Canakinumab in gout
Expert Opin Biol Ther 2012 Sep;12(9):1265-75.PMID:22784099DOI:10.1517/14712598.2012.705825.
Introduction: Gout is a painful inflammatory arthritis with a prevalence of approximately 4% in the United States, affecting an estimated 8.3 million adults. The past 20 years have shown significant increases in the number of patients with gout and its incidence may still be increasing. Current treatment options to control the pain and inflammation of acute gout include nonsteroidal anti-inflammatory drugs, colchicine and corticosteroids, although patients are often unresponsive to, intolerant of, or have contraindications for, these therapies. Additional treatment options are therefore needed for this population with difficult-to-treat gout. Areas covered: Currently available and investigational anti-inflammatory agents for acute and chronic gout will briefly be reviewed. Canakinumab , a fully human monoclonal anti-interleukin (IL)-1β antibody that selectively blocks IL-1β and that is being investigated for the treatment of gout, will be discussed in greater detail. Expert opinion: Canakinumab has been found to be superior to triamcinolone acetonide in acute gout and to colchicine in gout attack prophylaxis in reducing pain and risk of new gout attacks. Canakinumab's long half-life contributes to its prolonged anti-inflammatory effects.