Etanercept
(Synonyms: 依那西普) 目录号 : GC34579
Etanercept(Enbrel)是一种肿瘤坏死因子(TNF)抑制剂，用于治疗类风湿性关节炎，强直性脊柱炎，银屑病关节炎和斑块状银屑病。
Cas No.:185243-69-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Purity: >98.00%
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Etanercept (Enbrel) is a tumor necrosis factor (TNF) inhibitor used for treating rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis and plaque psoriasis. TNF[1]
[1]. Burness CB, et al. Etanercept (SB4): A Review in Autoimmune Inflammatory Diseases. BioDrugs. 2016 Aug;30(4):371-8.
Etanercept (Enbrel) 是一种肿瘤坏死因子 (TNF) 抑制剂，用于治疗类风湿性关节炎、强直性脊柱炎、银屑病关节炎和斑块状银屑病。肿瘤坏死因子[1]
[1]。 Burness CB 等人。依那西普 (SB4):自身免疫性炎症疾病综述。生物药物。 2016 年 8 月；30(4):371-8。
| Cas No. | 185243-69-0 | SDF | |
| 别名 | 依那西普 | ||
| Canonical SMILES | [Etanercept] | ||
| 分子式 | C2224H3475N621O698S36 | 分子量 | 51234.33 |
| 溶解度 | Soluble in water | 储存条件 | Store at 4°C, Do not freeze |
| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.0195 mL | 0.0976 mL | 0.1952 mL |
| 5 mM | 0.0039 mL | 0.0195 mL | 0.039 mL |
| 10 mM | 0.002 mL | 0.0098 mL | 0.0195 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。
Etanercept for the treatment of rheumatoid arthritis
Immunotherapy 2018 Mar 1;10(6):433-445.PMID:29482402DOI:10.2217/imt-2017-0155.
Etanercept was the first specific anticytokine therapy approved for the treatment of rheumatoid arthritis (RA). Its clinical efficacy and safety has been demonstrated by several clinical trials in early as well as established disease. Etanercept, along with other TNF inhibitors, have revolutionized management of RA and dramatically improved disease activity, function, quality of life and mortality for these patients. It is structurally distinct from other TNF inhibitors and thus has desirable profiles for immunogenicity, drug survival and infection rate. With the increasing number of Etanercept biosimilars, there will likely be a resurgence of their prescription. This article reviews the pharmacology, efficacy and safety of the Etanercept reference product, and its biosimilars, in the context of RA treatment.
Etanercept or Methotrexate Withdrawal in Rheumatoid Arthritis Patients in Sustained Remission
Arthritis Rheumatol 2021 May;73(5):759-768.PMID:33205906DOI:10.1002/art.41589.
Objective: Patients with rheumatoid arthritis (RA) in whom remission is achieved following combination therapy with methotrexate plus Etanercept face an ongoing medication burden. This study was undertaken to investigate whether sustained remission achieved on combination therapy can be maintained with either methotrexate or Etanercept monotherapy, as assessed following discontinuation of one or the other medication from the combination. Methods: Of the 371 adult patients with RA who received combination therapy with methotrexate plus Etanercept, remission (defined as a Simplified Disease Activity Index [SDAI] score of ≤3.3) was sustained in 253 patients through a 24-week open-label period. These 253 patients then entered a 48-week, double-blind period and were randomized to receive either 1) methotrexate monotherapy (n = 101), 2) Etanercept monotherapy (n = 101), or 3) methotrexate plus Etanercept combination therapy (n = 51). Patients who subsequently experienced disease-worsening received rescue therapy with the combination regimen at the same dosages as used in the initial run-in period. The primary end point was the proportion of patients in whom SDAI-defined remission was maintained without disease-worsening at week 48 in the Etanercept monotherapy group as compared to the methotrexate monotherapy group. Secondary end points included time to disease-worsening, and the proportion of patients in whom SDAI-defined remission was recaptured after initiation of rescue therapy. Results: Baseline demographic and clinical characteristics of the RA patients were similar across the treatment groups. At week 48, SDAI-defined remission was maintained in significantly more patients in the Etanercept monotherapy group than in the methotrexate monotherapy group (49.5% versus 28.7%; P = 0.004). Moreover, as a secondary end point, sustained SDAI-defined remission was achieved in significantly more patients who received combination therapy than in those who received methotrexate monotherapy (52.9% versus 28.7%; P = 0.006). Time to disease-worsening was shorter in those who received methotrexate monotherapy than in those who received Etanercept monotherapy or those who received combination therapy (each P < 0.001 versus methotrexate monotherapy). Among the patients who received rescue therapy, SDAI-defined remission was recaptured in 70-80% in each treatment group. No new safety signals were reported. Conclusion: The efficacy of Etanercept monotherapy was superior to that of methotrexate monotherapy and similar to that of combination therapy in maintaining remission in patients with RA. SDAI-defined remission was recaptured in most of the patients who were given rescue therapy. These data could inform decision-making when withdrawal of therapy is being considered to reduce treatment burden in patients with well-controlled RA.
Etanercept biosimilar SB-4
Expert Opin Biol Ther 2019 Mar;19(3):173-179.PMID:30616405DOI:10.1080/14712598.2019.1566456.
Biosimilars are highly similar molecules to other biological medicines that have already been authorized for use. Etanercept (ETN) was the first anti-tumor necrosis factor inhibitor (TNFi) approved by the Food and Drug Administration for the treatment of moderate to severe rheumatoid arthritis (RA) in November 1998 and in February 2000 by the European Medicines Agency. Twenty years later, the first ETN biosimilar has come of age. Areas covered: In this review we examined SB-4 as a biosimilar candidate to ETN, focusing on the available data. Current data indicate that SB-4 is a highly similar alternative to ETN in terms of safety, efficacy, tolerability, and immunogenicity. SB-4 has already been approved by health authorities in Europe, South Korea, Australia, and Canada, as a subcutaneous therapy option for the treatment of patients with RA but also for the full spectrum approved for its bio-originator ETN. Expert opinion: The current body of evidence suggests that all biologic activities have been demonstrated to be equivalent between SB-4 and the originator, including pharmacodynamic and pharmacokinetic activities. In some areas, and more specifically when it comes to immunogenicity, SB-4 showed lower incidents. Therefore, it is fully expected to have same efficacy and safety in all indications.
Etanercept and Methotrexate as Monotherapy or in Combination for Psoriatic Arthritis: Primary Results From a Randomized, Controlled Phase III Trial
Arthritis Rheumatol 2019 Jul;71(7):1112-1124.PMID:30747501DOI:10.1002/art.40851.
Objective: To examine the efficacy of methotrexate monotherapy relative to Etanercept monotherapy and the value of combining methotrexate and Etanercept for the treatment of patients with psoriatic arthritis (PsA). Methods: In this double-blind study, 851 patients with PsA were randomized to 1 of 3 treatment arms, as follows: oral methotrexate (20 mg) plus subcutaneous placebo given weekly (n = 284), subcutaneous Etanercept (50 mg) plus oral placebo given weekly (n = 284), or subcutaneous Etanercept (50 mg) plus oral methotrexate (20 mg) given weekly (combination therapy; n = 283). The American College of Rheumatology 20% improvement (ACR20) response and Minimal Disease Activity (MDA) response at week 24 were the primary end point and key secondary end point, respectively. Other measures of inflammatory arthritis, radiographic progression, and nonarticular disease manifestations were also assessed. Results: Patients with PsA had a mean ± SD age of 48.4 ± 13.1 years, and the mean ± SD duration of PsA was 3.2 ± 6.3 years (median 0.6 years). ACR20 and MDA response rates at week 24 were significantly greater in patients who received Etanercept monotherapy compared with those who received methotrexate monotherapy (ACR20, 60.9% versus 50.7% of patients [P = 0.029]; MDA, 35.9% versus 22.9% of patients [P = 0.005]), and both were significantly greater in the combination therapy group compared with the methotrexate monotherapy group at week 24 (ACR20, 65.0% versus 50.7% of patients [P = 0.005]; MDA, 35.7% versus 22.9% of patients [P = 0.005]). Other secondary outcomes (ACR50 and ACR70 response rates, proportions of patients achieving a Very Low Disease Activity score, and PsA disease activity scores) showed between-group differences that were consistent with the primary and key secondary end point results. Furthermore, patients in both Etanercept treatment arms showed less radiographic progression at week 48 compared with patients who received methotrexate monotherapy. Outcomes were similar in the combination therapy and Etanercept monotherapy groups, except for some skin end points. No new safety signals were seen. Conclusion: Etanercept monotherapy and combination therapy with Etanercept and methotrexate showed greater efficacy than methotrexate monotherapy in patients with PsA, according to the ACR and MDA response rates and extent of radiographic progression at follow-up. Overall, combining methotrexate and Etanercept did not improve the efficacy of Etanercept.
Evaluation of Combination Therapy With Etanercept and Systemic Corticosteroids for Stevens-Johnson Syndrome and Toxic Epidermal Necrolysis: A Multicenter Observational Study
J Allergy Clin Immunol Pract 2022 May;10(5):1295-1304.e6.PMID:35131514DOI:10.1016/j.jaip.2022.01.038.
Background: Stevens-Johnson syndrome-toxic epidermal necrolysis (SJS-TEN) are fatal severe cutaneous adverse reactions, without consensus on the medical treatment. The use of systemic corticosteroids or intravenous immunoglobulin (IVIG) remains debatable. Tumor necrosis factor-alpha inhibitors are potentially effective. Objective: To evaluate the effectiveness and safety of combination therapy using Etanercept combined with corticosteroids or IVIG combined with corticosteroids versus corticosteroid monotherapy for patients with SJS-TEN. Methods: We retrospectively enrolled SJS-TEN patients from Taiwan and the Chinese mainland, during 2014 to 2019. Patients enrolled were treated with corticosteroid monotherapy, or combinations with IVIG or Etanercept. We analyzed the clinical characteristics, skin healing time, mortality, and adverse events among these treatment groups. Results: Among the 242 patients (187 with SJS or SJS-TEN overlapping and 55 with TEN), patients who received combination therapy with Etanercept and corticosteroids had lower actual mortality than those with corticosteroid monotherapy and those with IVIG combined with corticosteroids, respectively (0% vs 6.63% and 4.76%). There was a tendency of reducing standardized (observed/predicted) mortality rate (SMR) based on the Score of Toxic Epidermal Necrolysis in Etanercept combined with corticosteroids compared with corticosteroid monotherapy and IVIG combined with corticosteroids therapy (SMR [95% CI] 0 [1.80-3.59], 0.71 [0.83-2.64], 0.30 [0.68-6.22]; P = .006). Etanercept combined with corticosteroids showed a reduced skin healing time (12.0 [8.5-14.0], median days [interquartile range]), compared with corticosteroid monotherapy (13.0 [10.0-18.0]) and IVIG combined with corticosteroids therapy (13.5 [10.0-19.5]); P = .004 and P = .012, respectively). Etanercept combined with corticosteroids also showed a lower incidence of adverse event with gastrointestinal hemorrhage than corticosteroid monotherapy, especially in patients with TEN (P = .001). Conclusions: The tumor necrosis factor-alpha inhibitors and corticosteroids combination therapy was effective and safer than corticosteroid monotherapy for SJS-TEN, and may be considered as an alternative therapy for SJS-TEN patients who responded poorly to conventional corticosteroid therapy.