Obinutuzumab
(Synonyms: 奥滨尤妥珠单抗; GA101; Anti-Human CD20 type II, Humanized Antibody) 目录号 : GC61143
Obinutuzumab (anti-CD20) (Gazyva, GA101, Gazyvaro, Afutuzumab) is a novel, type II, glycoengineered, humanized anti-CD20 monoclonal antibody that has been developed for lymphocytic leukemia and lymphoma of B-cell origin. MW : 146.1 kD.
Cas No.:949142-50-1
Sample solution is provided at 25 µL, 10mM.
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Purity: >99.00%
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Obinutuzumab (anti-CD20) (Gazyva, GA101, Gazyvaro, Afutuzumab) is a novel, type II, glycoengineered, humanized anti-CD20 monoclonal antibody that has been developed for lymphocytic leukemia and lymphoma of B-cell origin. MW : 146.1 kD.
GA101 is the first Fc-engineered, type II humanized IgG1 antibody against CD20. Relative to rituximab, GA101 has increased direct and immune effector cell-mediated cytotoxicity and exhibits superior activity in cellular assays and whole blood B-cell depletion assays.[3]
In human lymphoma xenograft models, GA101 exhibits superior antitumor activity, resulting in the induction of complete tumor remission and increased overall survival. In nonhuman primates, GA101 demonstrates superior B cell–depleting activity in lymphoid tissue, including in lymph nodes and spleen.[3]
[1] Kensei Tobinai, et al. Adv Ther . 2017 Feb;34(2):324-356. [2] Frank Herting, et al. Leuk Lymphoma. 2014 Sep;55(9):2151-5160. [3] Ekkehard M?ssner, et al. Blood. 2010 Jun 3;115(22):4393-402.
| Cas No. | 949142-50-1 | SDF | |
| 别名 | 奥滨尤妥珠单抗; GA101; Anti-Human CD20 type II, Humanized Antibody | ||
| Canonical SMILES | [Obinutuzumab] | ||
| 分子式 | 分子量 | 146298.97 | |
| 溶解度 | 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 | 0.0068 mL | 0.0342 mL | 0.0684 mL |
| 5 mM | 0.0014 mL | 0.0068 mL | 0.0137 mL |
| 10 mM | 0.0007 mL | 0.0034 mL | 0.0068 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 | ||||||||||
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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。
Obinutuzumab for the First-Line Treatment of Follicular Lymphoma
N Engl J Med 2017 Oct 5;377(14):1331-1344.PMID:28976863DOI:10.1056/NEJMoa1614598.
Background: Rituximab-based immunochemotherapy has improved outcomes in patients with follicular lymphoma. Obinutuzumab is a glycoengineered type II anti-CD20 monoclonal antibody. We compared rituximab-based chemotherapy with obinutuzumab-based chemotherapy in patients with previously untreated advanced-stage follicular lymphoma. Methods: We randomly assigned patients to undergo induction treatment with obinutuzumab-based chemotherapy or rituximab-based chemotherapy. Patients with a response received maintenance treatment for up to 2 years with the same antibody that they had received in induction. The primary end point was investigator-assessed progression-free survival. Results: A total of 1202 patients with follicular lymphoma underwent randomization (601 patients in each group). After a median follow-up of 34.5 months (range, 0 to 54.5), a planned interim analysis showed that obinutuzumab-based chemotherapy resulted in a significantly lower risk of progression, relapse, or death than rituximab-based chemotherapy (estimated 3-year rate of progression-free survival, 80.0% vs. 73.3%; hazard ratio for progression, relapse, or death, 0.66; 95% confidence interval [CI], 0.51 to 0.85; P=0.001). Similar results were seen with regard to independently reviewed progression-free survival and other time-to-event end points. Response rates were similar in the two groups (88.5% in the Obinutuzumab group and 86.9% in the rituximab group). Adverse events of grade 3 to 5 were more frequent in the Obinutuzumab group than in the rituximab group (74.6% vs. 67.8%), as were serious adverse events (46.1% vs. 39.9%). The rates of adverse events resulting in death were similar in the two groups (4.0% in the Obinutuzumab group and 3.4% in the rituximab group). The most common adverse events were infusion-related events that were considered by the investigators to be largely due to Obinutuzumab in 353 of 595 patients (59.3%; 95% CI, 55.3 to 63.2) and to rituximab in 292 of 597 patients (48.9%; 95% CI, 44.9 to 52.9; P<0.001). Nausea and neutropenia were common. A total of 35 patients (5.8%) in the Obinutuzumab group and 46 (7.7%) in the rituximab group died. Conclusions: Obinutuzumab-based immunochemotherapy and maintenance therapy resulted in longer progression-free survival than rituximab-based therapy. High-grade adverse events were more common with obinutuzumab-based chemotherapy. (Funded by F. Hoffmann-La Roche; GALLIUM ClinicalTrials.gov number, NCT01332968 .).
Venetoclax and Obinutuzumab in Patients with CLL and Coexisting Conditions
N Engl J Med 2019 Jun 6;380(23):2225-2236.PMID:31166681DOI:10.1056/NEJMoa1815281.
Background: The BCL2 inhibitor venetoclax has shown activity in patients with chronic lymphocytic leukemia (CLL), but its efficacy in combination with other agents in patients with CLL and coexisting conditions is not known. Methods: In this open-label, phase 3 trial, we investigated fixed-duration treatment with venetoclax and Obinutuzumab in patients with previously untreated CLL and coexisting conditions. Patients with a score of greater than 6 on the Cumulative Illness Rating Scale (scores range from 0 to 56, with higher scores indicating more impaired function of organ systems) or a calculated creatinine clearance of less than 70 ml per minute were randomly assigned to receive venetoclax-obinutuzumab or chlorambucil-obinutuzumab. The primary end point was investigator-assessed progression-free survival. The safety of each regimen was also evaluated. Results: In total, 432 patients (median age, 72 years; median Cumulative Illness Rating Scale score, 8; median creatinine clearance, 66.4 ml per minute) underwent randomization, with 216 assigned to each group. After a median follow-up of 28.1 months, 30 primary end-point events (disease progression or death) had occurred in the venetoclax-obinutuzumab group and 77 had occurred in the chlorambucil-obinutuzumab group (hazard ratio, 0.35; 95% confidence interval [CI], 0.23 to 0.53; P<0.001). The Kaplan-Meier estimate of the percentage of patients with progression-free survival at 24 months was significantly higher in the venetoclax-obinutuzumab group than in the chlorambucil-obinutuzumab group: 88.2% (95% CI, 83.7 to 92.6) as compared with 64.1% (95% CI, 57.4 to 70.8). This benefit was also observed in patients with TP53 deletion, mutation, or both and in patients with unmutated immunoglobulin heavy-chain genes. Grade 3 or 4 neutropenia occurred in 52.8% of patients in the venetoclax-obinutuzumab group and in 48.1% of patients in the chlorambucil-obinutuzumab group, and grade 3 or 4 infections occurred in 17.5% and 15.0%, respectively. All-cause mortality was 9.3% in the venetoclax-obinutuzumab group and 7.9% in the chlorambucil-obinutuzumab group. These differences were not significant. Conclusions: Among patients with untreated CLL and coexisting conditions, venetoclax-obinutuzumab was associated with longer progression-free survival than chlorambucil-obinutuzumab. (Funded by F. Hoffmann-La Roche and AbbVie; ClinicalTrials.gov number, NCT02242942.).
B-cell depletion with Obinutuzumab for the treatment of proliferative lupus nephritis: a randomised, double-blind, placebo-controlled trial
Ann Rheum Dis 2022 Jan;81(1):100-107.PMID:34615636DOI:10.1136/annrheumdis-2021-220920.
Objective: Randomised trials of type I anti-CD20 antibodies rituximab and ocrelizumab failed to show benefit in proliferative lupus nephritis (LN). We compared Obinutuzumab, a humanised type II anti-CD20 monoclonal antibody that induces potent B-cell depletion, with placebo for the treatment of LN in combination with standard therapies. Methods: Patients with LN receiving mycophenolate and corticosteroids were randomised to Obinutuzumab 1000 mg or placebo on day 1 and weeks 2, 24 and 26, and followed through week 104. The primary endpoint was complete renal response (CRR) at week 52. Exploratory analyses through week 104 were conducted. The prespecified alpha level was 0.2. Results: A total of 125 patients were randomised and received blinded infusions. Achievement of CRR was greater with Obinutuzumab at week 52 (primary endpoint, 22 (35%) vs 14 (23%) with placebo; percentage difference, 12% (95% CI -3.4% to 28%), p=0.115) and at week 104 (26 (41%) vs 14 (23%); percentage difference, 19% (95% CI 2.7% to 35%), p=0.026). Improvements in other renal response measures, serologies, estimated glomerular filtration rate and proteinuria were greater with Obinutuzumab. Obinutuzumab was not associated with increases in serious adverse events, serious infections or deaths. Non-serious infusion-related reactions occurred more frequently with Obinutuzumab. Conclusions: Improved renal responses through week 104 were observed in patients with LN who received Obinutuzumab plus standard therapies compared with standard therapies alone. Obinutuzumab was well tolerated and no new safety signals were identified. Trial registration number: NCT02550652.
Venetoclax plus Obinutuzumab versus chlorambucil plus Obinutuzumab for previously untreated chronic lymphocytic leukaemia (CLL14): follow-up results from a multicentre, open-label, randomised, phase 3 trial
Lancet Oncol 2020 Sep;21(9):1188-1200.PMID:32888452DOI:10.1016/S1470-2045(20)30443-5.
Background: Venetoclax plus Obinutuzumab has been established as a fixed-duration treatment regimen for patients with chronic lymphocytic leukaemia. We compared the long-term efficacy after treatment cessation of the combination of venetoclax plus Obinutuzumab with chlorambucil plus Obinutuzumab in patients with previously untreated chronic lymphocytic leukaemia. Methods: CLL14 is a multicentre, randomised, open-label, phase 3 trial done at 196 sites in 21 countries. Eligible patients were aged 18 years or older, had untreated chronic lymphocytic leukaemia, and coexisting conditions with a cumulative illness rating scale greater than 6, a creatinine clearance of 30-69 mL/min, or both. Patients were randomly assigned (1:1) via a web and voicemail system with allocation concealment and based on a computer-generated randomisation schedule with a block size of six and stratified by Binet stage and geographical region. Patients received either venetoclax plus Obinutuzumab (oral venetoclax initiated on day 22 of cycle 1 [28-day cycles], with a 5-week dose ramp-up [20 mg, 50 mg, 100 mg, and 200 mg, then 400 mg daily for 1 week], thereafter continuing at 400 mg daily until completion of cycle 12; combined with intravenous Obinutuzumab for six cycles starting with 100 mg on day 1 and 900 mg on day 2 [or 1000 mg on day 1], 1000 mg on days 8 and day 15 of cycle 1, and subsequently 1000 mg on day 1 of cycles 2 through 6) or chlorambucil plus Obinutuzumab (oral chlorambucil at 0·5 mg/kg bodyweight on days 1 and 15 of each cycle for 12 cycles combined with the same Obinutuzumab regimen). The primary endpoint was investigator-assessed progression-free survival in the intention-to-treat population. Safety was assessed in all patients who received at least one dose of study treatment. Patient enrolment is complete, and the study is registered with ClinicalTrails.gov, NCT02242942. Findings: Between Aug 7, 2015, and Aug 4, 2016, 432 patients were enrolled and randomly assigned to receive either venetoclax plus Obinutuzumab (n=216) or chlorambucil plus Obinutuzumab (n=216). All patients had been off treatment for at least 24 months at data collection. At a median follow-up of 39·6 months (IQR 36·8-43·0), patients given venetoclax plus Obinutuzumab had a significantly longer progression-free survival than did patients given chlorambucil plus Obinutuzumab (HR 0·31, 95% CI 0·22-0·44; p<0·0001). Median progression-free survival was not reached (95% CI not estimable to not estimable) in the venetoclax plus Obinutuzumab group vs 35·6 months (33·7-40·7) in the chlorambucil plus Obinutuzumab group. The most common grade 3 or 4 adverse event in both groups was neutropenia (112 [53%] of 212 patients in the venetoclax plus Obinutuzumab group versus 102 [48%] of 214 patients in the chlorambucil plus Obinutuzumab group). Serious adverse events occurred in 115 (54%) of 212 patients in the venetoclax plus Obinutuzumab group and 95 (44%) of 214 patients in the chlorambucil plus Obinutuzumab group. Venetoclax or chlorambucil treatment-related deaths were reported in one (1%) of 212 patients in the venetoclax plus Obinutuzumab group (n=1 sepsis) and two (1%) of 214 patients in the chlorambucil plus Obinutuzumab group (n=1 septic shock, n=1 metastatic skin squamous carcinoma). Interpretation: 2 years after treatment cessation, venetoclax plus Obinutuzumab continues to significantly improve progression-survival compared with chlorambucil plus Obinutuzumab, thereby providing a limited duration treatment option for patients with previously untreated chronic lymphocytic leukaemia. Funding: F Hoffmann-La Roche and AbbVie.
Obinutuzumab as treatment for ANCA-associated vasculitis
Rheumatology (Oxford) 2022 Aug 30;61(9):3814-3817.PMID:34958343DOI:10.1093/rheumatology/keab916.
Objectives: Rituximab is a standard of care therapy for patients with ANCA-associated vasculitis. When rituximab is contraindicated, or in the case of refractory disease, other treatments are needed. Obinutuzumab is another anti-CD20 antibody for the treatment of haematological malignancies that may induce a deeper B cell depletion compared with rituximab. This article reviews three cases of patients with ANCA-associated vasculitis who were treated with Obinutuzumab due to their history of anaphylactic reactions to rituximab. Methods: Case series of three patients with ANCA-associated vasculitis treated with Obinutuzumab. Results: One female patient with microscopic polyangiitis and two male patients with granulomatosis with polyangiitis received Obinutuzumab. The treatment was well-tolerated in all patients despite previous anaphylactic reaction to rituximab. Treatment with Obinutuzumab was effective in (i) inducing disease remission, (ii) inducing total B cell depletion, and (iii) resulting in undetectable serum titres of ANCA. All three patients were re-treated with Obinutuzumab for maintenance of remission. Conclusion: Obinutuzumab appears to be a safe and efficacious therapy for patients with ANCA-associated vasculitis who have had refractory disease or a history of anaphylaxis to rituximab. Prospective studies comparing rituximab to Obinutuzumab in ANCA-associated vasculitis patients are warranted.