Golimumab
(Synonyms: CNTO-148) 目录号 : GC66345
Golimumab (CNTO-148) 是一种有效的人 IgG1 TNFα 拮抗剂单克隆抗体。Golimumab 具有抗炎活性，并抑制 IL-6 和 IL-1β 的产生。Golimumab 通过靶向和中和 TNF 来防止炎症发生和软骨或骨骼的破坏。Golimumab 具有抗癌活性并诱导细胞凋亡 (apoptosis)。Golimumab 可用于类风湿关节炎、克罗恩病和癌症研究。
Cas No.:476181-74-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Golimumab (CNTO-148) is a potent human IgG1 TNFα antagonist monoclonal antibody. Golimumab has anti-inflammation activitity and inhibits IL-6 and IL-1β production. Golimumab acts via targeting and neutralizing TNF to prevent inflammation and destruction of cartilage and bone. Golimumab has the anticancer activity and induces cell apoptosis. Golimumab can be used for rheumatoid arthritis, Crohn's disease and cancer research[1][2][3].
Golimumab (CNTO-148) (0.1-10 μg /mL; 24-72 hours; transmembrane TNFα-transfected Jurkat cells) induces reductions in the viability of transmembrane TNFα-expressing cells[1].
Golimumab (CNTO-148) (10 μg /mL; 48 hours; transmembrane TNFα-transfected Jurkat cells) induces apoptosis, increase the levels of active caspase-3 and induces apoptotic DNA fragmentation[1].
Cell Viability Assay[1]
| Cell Line: | Transmembrane TNFα-transfected Jurkat cells |
| Concentration: | 0.1, 1 and 10 μg/mL |
| Incubation Time: | 24, 48 and 72 hours |
| Result: | Reduced cell viability in a dose- and time-dependent manner. |
Apoptosis Analysis[1]
| Cell Line: | Transmembrane TNFα-transfected Jurkat cells |
| Concentration: | 10 μg /mL |
| Incubation Time: | 48 hours |
| Result: | Had the percentage of apoptotic cells for 30.29%. |
Western Blot Analysis[1]
| Cell Line: | Transmembrane TNFα-transfected Jurkat cells |
| Concentration: | 10 μg /mL |
| Incubation Time: | 48 hours |
| Result: | Increased the levels of active caspase-3 and induces apoptotic DNA fragmentation. |
Golimumab (CNTO-148) (24 mg/kg; i.h.; daily, for 7 days; swiss-albino healthy male mice) inhibits oxidative stress, apoptotic cell death inflammatory response, thus improving renal function. Golimumab reduces all markers of kidney injury and attenuates cell death[2].
Golimumab (CNTO-148) (1-10 mg/kg; i.p.;daily; for 4 weeks; Tg197 transgenic mouse model) relieves TNFα-induced arthritis in a mouse model of human[3].
| Animal Model: | Swiss-albino healthy male mice[2] |
| Dosage: | 24 mg/kg |
| Administration: | Subcutaneous injection; daily, for 7 days |
| Result: | Reduced serum parameters like BUN, NGAL creatinine, cystatin C, and urinary parameters like KIM-1, NAG, albumin clusterin. |
| Animal Model: | Swiss-albino healthy male mice[2] |
| Dosage: | 24 mg/kg |
| Administration: | Subcutaneous injection; daily, for 7 days |
| Result: | Inhibited oxidative stress, reduces MDA concentrations and increases the GSH and catalase levels. |
| Animal Model: | Swiss-albino healthy male mice[2] |
| Dosage: | 24 mg/kg |
| Administration: | Subcutaneous injection; daily, for 7 days |
| Result: | Inhibitd cisplatin-induced inflammation, decreased TNF-α, including IL-6, IL-1β, MCP-1, ICAM-1, and TGF-β1 levels and increases IL-10 concentrations, reduced caspase 3 in cisplatin injected mice kidneys. |
| Animal Model: | Tg197 transgenic mouse model[3] |
| Dosage: | 1 and 10 mg/kg |
| Administration: | Intraperitoneal injection;for 4 weeks |
| Result: | Reduced the arthritic index. |
| Cas No. | 476181-74-5 | SDF | Download SDF |
| 别名 | CNTO-148 | ||
| 分子式 | 分子量 | ||
| 溶解度 | 储存条件 | Store at -20°C | |
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Golimumab (anti-TNF monoclonal antibody): where we stand today
Hum Vaccin Immunother 2021 Jun 3;17(6):1586-1598.PMID:33369527DOI:10.1080/21645515.2020.1836919.
Tumor necrosis factor (TNF) is a pro-inflammatory cytokine and its overexpression has been implicated in the pathophysiology of several chronic immune-mediated inflammatory diseases. Biological therapies, like TNF inhibitors, have been revolutionizing the course of these disorders. Golimumab is a transgenic anti-TNF monoclonal antibody that acts primarily by targeting and neutralizing TNF, thus preventing inflammation. It is approved for the treatment of Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, Nonradiographic axial Spondyloarthritis, Juvenile Idiopathic Arthritis, and Ulcerative Colitis. Clinical trials are also being conducted in other conditions. This review charts the clinical development of Golimumab and outlines the data that support its potential use across several Immune-mediated inflammatory diseases.
[Golimumab]
Nihon Rinsho 2013 Jul;71(7):1227-31.PMID:23961671doi
Golimumab is one of the TNF-inhibitors, having an efficacy and safety profile comparable to other TNF-inhibitors. In addition, Golimumab is a fully human monoclonal antibody, has several unique features, such as neutralizing antibodies are difficult to generate. In clinical trials carried out in Japan, the efficacy and safety of administration of Golimumab 100 mg every 4 weeks is shown, and Golimumab blood concentration related to efficacy have been pointed out. From these, Golimumab is considered a useful drug in every step of the treatment of rheumatoid arthritis. This section reviews the clinical trials of Golimumab, and consider the useful use of Golimumab.
Golimumab
MAbs 2009 Sep-Oct;1(5):422-31.PMID:20065639DOI:10.4161/mabs.1.5.9286.
Golimumab, a human anti-TNFalpha IgG1kappa monoclonal antibody, was approved in the US and Canada in April 2009 as a treatment for rheumatoid arthritis, psoriatic arthritis and ankylosing spondylitis, and is undergoing regulatory review in the EU for these indications. The product was developed by Centocor and Janssen Pharmaceutical KK (Johnson & Johnson subsidiaries), in collaboration with Schering-Plough and Mitsubishi Tanabe Pharma. Golimumab faces numerous protein therapeutic competitors on the market, but, as the first patient-administered, once-monthly dosed anti-TNFalpha drug, it will likely be an attractive option for patients.
Golimumab and Beta-Cell Function in Youth with New-Onset Type 1 Diabetes
N Engl J Med 2020 Nov 19;383(21):2007-2017.PMID:33207093DOI:10.1056/NEJMoa2006136.
Background: Type 1 diabetes is an autoimmune disease characterized by progressive loss of pancreatic beta cells. Golimumab is a human monoclonal antibody specific for tumor necrosis factor α that has already been approved for the treatment of several autoimmune conditions in adults and children. Whether Golimumab could preserve beta-cell function in youth with newly diagnosed overt (stage 3) type 1 diabetes is unknown. Methods: In this phase 2, multicenter, placebo-controlled, double-blind, parallel-group trial, we randomly assigned, in a 2:1 ratio, children and young adults (age range, 6 to 21 years) with newly diagnosed overt type 1 diabetes to receive subcutaneous Golimumab or placebo for 52 weeks. The primary end point was endogenous insulin production, as assessed according to the area under the concentration-time curve for C-peptide level in response to a 4-hour mixed-meal tolerance test (4-hour C-peptide AUC) at week 52. Secondary and additional end points included insulin use, the glycated hemoglobin level, the number of hypoglycemic events, the ratio of fasting proinsulin to C-peptide over time, and response profile. Results: A total of 84 participants underwent randomization - 56 were assigned to the Golimumab group and 28 to the placebo group. The mean (±SD) 4-hour C-peptide AUC at week 52 differed significantly between the Golimumab group and the placebo group (0.64±0.42 pmol per milliliter vs. 0.43±0.39 pmol per milliliter, P<0.001). A treat-to-target approach led to good glycemic control in both groups, and there was no significant difference between the groups in glycated hemoglobin level. Insulin use was lower with Golimumab than with placebo. A partial-remission response (defined as an insulin dose-adjusted glycated hemoglobin level score [calculated as the glycated hemoglobin level plus 4 times the insulin dose] of ≤9) was observed in 43% of participants in the Golimumab group and in 7% of those in the placebo group (difference, 36 percentage points; 95% CI, 22 to 55). The mean number of hypoglycemic events did not differ between the trial groups. Hypoglycemic events that were recorded as adverse events at the discretion of investigators were reported in 13 participants (23%) in the Golimumab group and in 2 (7%) of those in the placebo group. Antibodies to Golimumab were detected in 30 participants who received the drug; 29 had antibody titers lower than 1:1000, of whom 12 had positive results for neutralizing antibodies. Conclusions: Among children and young adults with newly diagnosed overt type 1 diabetes, Golimumab resulted in better endogenous insulin production and less exogenous insulin use than placebo. (Funded by Janssen Research and Development; T1GER ClinicalTrials.gov number, NCT02846545.).
Golimumab for the treatment of axial spondyloarthritis
Expert Opin Biol Ther 2017 Jan;17(1):129-133.PMID:27817204DOI:10.1080/14712598.2017.1256387.
Anti-TNF drugs have represented an epochal revolution in the treatment of rheumatoid arthritis and spondyloarthritis. In the field of axial spondyloarthritis, Golimumab, a fully human monoclonal anti-TNFα administered subcutaneously every 4 weeks, has shown significant efficacy and good safety in patients with ankylosing spondylitis. More recently, it was also indicated as an effective treatment for patients suffering from non-radiographic axial spondyloarthitits. Areas covered: A systematic literature search was completed, using the largest electronic databases (Medline, Embase and Cochrane), with the aim to review all data concerning the administration of Golimumab in patients suffering from axial spondyloartritis. Expert opinion: In the 16-week GO-AHEAD study, Golimumab was effective in patients with non-radiographic spondyloarthritis with high levels of CRP and/or positive MRI findings, but not in subjects with both negative CRP and MRI. This finding allows for the addressing the of anti-TNF treatment more specifically. Preliminary data concerning an open-label extension of the GO-AHEAD study outlined the high retention-rate of the drug at 52 weeks. The production of antibodies against Golimumab is rare and it seems to exert scarce influence on the drug performances. In conclusion, Golimumab appears as a very useful and well tolerated anti-TNF agent.