Girentuximab
(Synonyms: G250; cG250) 目录号 : GC66360
Girentuximab (G250) 是一种嵌合单克隆抗体，可与碳酸酐酶 IX (CAIX) 结合，碳酸酐酶 IX 是一种在透明细胞肾细胞癌 (ccRCC) 中广泛表达的细胞表面糖蛋白。
Cas No.:916138-87-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
- Datasheet
Girentuximab (G250) is a chimeric monoclonal antibody that binds carbonic anhydrase IX (CAIX), a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC)[1].
Girentuximab is an IgG1 κ light chain chimeric version of a murine monoclonal antibody (mAb) and recognizes the antigen CAIX[1].
| Cas No. | 916138-87-9 | SDF | Download SDF |
| 别名 | G250; cG250 | ||
| 分子式 | 分子量 | ||
| 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。 |
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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。
Targeted PET/CT imaging for clear cell renal cell carcinoma with radiolabeled antibodies: recent developments using Girentuximab
Curr Opin Urol 2021 May 1;31(3):249-254.PMID:33742975DOI:10.1097/MOU.0000000000000872.
Purpose of review: Conventional imaging is unable to differentiate clear cell renal cell carcinoma (ccRCC) from other more indolent and benign renal tumors. Positron emission tomography/computed tomography (PET/CT) using radiolabeled antibodies may aid in detecting both localized and metastatic ccRCC. The purpose of this review is to summarize recent literature regarding the use of radiolabeled antibodies for imaging of ccRCC. Recent findings: Two recent studies evaluated the use of radiolabeled anticarbonic anhydrase IX antibody Girentuximab for the imaging of ccRCC. PET/CT with 89zirconium-labeled Girentuximab (89Zr-girentuximab PET/CT) was used to guide clinical decision making in 16 patients with localized disease. It had a high specificity for detecting ccRCC with 6/6 resected lesions with uptake proven to be ccRCC, all lesion without uptake showed to be indolent during follow-up. Clinical management was changed in 36% (5/14) of patients with the metastatic disease based on outcomes of the scan. Furthermore, in 42 patients 89Zr-girentuximab PET/CT combined with CT outperformed CT alone or combined with 18F fludeoxyglucose PET for detection of metastasis. Summary: 89Zr-girentuximab PET/CT has the ability to diagnose ccRCC in localized disease. In metastatic disease, it enables the differentiation of ccRCC from non-ccRCC cancers and the evaluation of disease extent. 89Zr-girentuximab PET/CT diagnostic accuracy is currently evaluated in a multicenter phase III trial.
89Zirconium-labelled Girentuximab (89Zr-TLX250) PET in Urothelial Cancer Patients (ZiPUP): protocol for a phase I trial of a novel staging modality for urothelial carcinoma
BMJ Open 2022 Apr 15;12(4):e060478.PMID:35428649DOI:10.1136/bmjopen-2021-060478.
Introduction: Bladder cancer is a lethal disease with a rising incidence on a background of limited conventional imaging modalities for staging (either CT of the chest-abdomen-pelvis or 18F-fluorodeoxyglucose positron emitting tomography (FDG-PET/CT)). CT is known to have relatively low sensitivity for detecting low volume metastatic disease, an important goal when considering surgical interventions entailing significant potential morbidity. FDG is also limited, being predominantly renally excreted and, therefore, producing intense non-specific activity in the urinary tract, which limits its utility to detect bladder and upper tract lesions, or nodal metastases in close proximity to the urinary tract. 89Zirconium-labelled Girentuximab (89Zr-TLX250) may have utility in the accurate staging of bladder and urothelial carcinomas, with less renal excretion as compared with FDG; however, this has not previously been investigated. Methods and analysis: 89Zirconium-labelled Girentuximab PET in Urothelial Cancer Patients is a single-arm phase I trial examining the feasibility of using 89Zr-TLX250-PET/CT as a staging modality for urothelial and bladder carcinomas by examining isotope uptake by the cancer. This trial will also examine the safety and utility of 89Zr-TLX250-PET/CT in patients either undergoing preoperative staging of bladder or other urothelial carcinomas for curative intent, or with known metastatic urothelial carcinomas. All participants will undergo 89Zr-TLX250-PET/CT and will need to have undergone recent FDG-PET/CT for comparison. This trial aims to recruit 10 participants undergoing preoperative staging and 10 participants with known metastatic disease. The primary endpoint is feasibility defined by the ability to recruit to the target sample size within the study duration; secondary endpoints are safety, tolerability, sensitivity and specificity in detecting lymph node metastases compared with FDG-PET/CT. Ethics and dissemination: Ethics approval has been obtained from the South Metropolitan Health Service Human Research Ethics Committee (RGS0000003940). Eligible patients will only be enrolled after providing written informed consent. Patients will be given a full explanation, in lay terms, of the aims of the study and potential risks including as a written patient information sheet. Trial registration numbers: ACTRN12621000411842, NCT05046665.
Adjuvant Weekly Girentuximab Following Nephrectomy for High-Risk Renal Cell Carcinoma: The ARISER Randomized Clinical Trial
JAMA Oncol 2017 Jul 1;3(7):913-920.PMID:27787547DOI:10.1001/jamaoncol.2016.4419.
Importance: Girentuximab is a chimeric monoclonal antibody that binds carbonic anhydrase IX, a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC). Its safety and activity in phase 2 studies prompted investigation into its use as adjuvant monotherapy in participants with high-risk ccRCC. Objective: To evaluate the safety and efficacy of adjuvant Girentuximab on disease-free survival (DFS) and overall survival (OS) in patients with localized completely resected high-risk ccRCC. Design, setting, and participants: The ARISER trial (Adjuvant Rencarex Immunotherapy Phase 3 Trial to Study Efficacy in Nonmetastatic RCC) was a randomized, double-blind, placebo-controlled phase 3 clinical trial that took place between June 10, 2004, and April 2, 2013, at 142 academic medical centers in 15 countries in North and South America and Europe. Eligible adult patients had undergone partial or radical nephrectomy for histologically confirmed ccRCC and fell into 1 of the following high-risk groups: pT3/pT4Nx/N0M0 or pTanyN+M0 or pT1b/pT2Nx/N0M0 with nuclear grade 3 or greater. Patients were assigned via central computerized double-blind 1:1 randomization to receive either a single loading dose of Girentuximab, 50 mg (week 1), followed by weekly intravenous infusions of Girentuximab, 20 mg (weeks 2-24), or placebo, stratified by risk group and region. The data were analyzed from March 31, 2012, to April 2, 2013. Main outcomes and measures: Co-primary end points were DFS and OS, based on imaging studies assessed by independent radiological review committee. Secondary end points included safety, assessed as the rate and grade of adverse events. Results: A total of 864 patients (66% male; median [interquartile range] age, 58 [51-65] years) were randomized to Girentuximab (n = 433) or placebo (n = 431). Compared with placebo, participants treated with Girentuximab had no statistically significant DFS (hazard ratio, 0.97; 95% CI, 0.79-1.18) or OS advantage (hazard ratio, 0.99; 95% CI, 0.74-1.32). Median DFS was 71.4 months (interquartile range, 3 months to not reached) for Girentuximab and never reached for placebo group. Median OS was never reached regardless of treatment. Drug-related adverse events occurred in 185 patients (21.6%), reported comparably between arms. Serious adverse events occurred in 72 patients (8.4%), reported comparably between arms. One drug-related serious adverse event occurred in a patient receiving placebo. Conclusions and relevance: Girentuximab had no clinical benefit as adjuvant treatment for patients with high-risk ccRCC. The surprisingly long DFS and OS in these patients represent a challenge to adjuvant ccRCC drug development. Trial registration: clinicaltrials.gov Identifier: NCT00087022.
Evaluation of Radiolabeled Girentuximab In Vitro and In Vivo
Pharmaceuticals (Basel) 2018 Nov 28;11(4):132.PMID:30487460DOI:10.3390/ph11040132.
Girentuximab (cG250) targets carbonic anhydrase IX (CAIX), a protein which is expressed on the surface of most renal cancer cells (RCCs). cG250 labeled with 177Lu has been used in clinical trials for radioimmunotherapy (RIT) of RCCs. In this work, an extensive characterization of the immunoconjugates allowed optimization of the labeling conditions with 177Lu while maintaining immunoreactivity of cG250, which was then investigated in in vitro and in vivo experiments. cG250 was conjugated with S-2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane tetraacetic acid (DOTA(SCN)) by using incubation times between 30 and 90 min and characterized by mass spectrometry. Immunoconjugates with five to ten DOTA(SCN) molecules per cG250 molecule were obtained. Conjugates with ratios less than six DOTA(SCN)/cG250 had higher in vitro antigen affinity, both pre- and postlabeling with 177Lu. Radiochemical stability increased, in the presence of sodium ascorbate, which prevents radiolysis. The immunoreactivity of the radiolabeled cG250 tested by specific binding to SK-RC-52 cells decreased when the DOTA content per conjugate increased. The in vivo tumor uptake was < 10% ID/g and independent of the total amount of protein in the range between 5 and 100 µg cG250 per animal. Low tumor uptake was found to be due to significant necrotic areas and heterogeneous CAIX expression. In addition, low vascularity indicated relatively poor accessibility of the CAIX target.
Indium-111-labeled Girentuximab immunoSPECT as a diagnostic tool in clear cell renal cell carcinoma
Eur Urol 2013 Jun;63(6):1101-6.PMID:23453421DOI:10.1016/j.eururo.2013.02.022.
Background: Improved and more frequent radiologic evaluation has resulted in increased identification of renal masses of unknown origin, which frequently pose a diagnostic dilemma for urologists. Objective: Carbonic anhydrase IX (CAIX) is an antigen ubiquitously expressed in clear cell renal cell carcinoma (ccRCC). The specific and high level of expression in ccRCC makes CAIX an excellent target for imaging ccRCC lesions. We present our experience with immuno-single-photon emission computed tomography (immunoSPECT) imaging with the indium-111 ((111)In)-labeled anti-CAIX antibody Girentuximab in patients presenting with either a primary renal tumor or a history of ccRCC and lesions suspect for metastases during follow-up. Design, setting, and participants: Twenty-nine patients received 100-200 MBq (111)In-labeled Girentuximab. Whole-body and single photon emission computed tomography (SPECT) images were acquired after 4-7 d. Intervention: Injection with (111)In-girentuximab and image acquisition after 4-7 d. Outcome measurements and statistical analysis: Accuracy of (111)In-girentuximab immunoSPECT. Results and limitations: Distinct uptake of (111)In-girentuximab was seen in 16 of 22 patients presenting with a renal mass. All renal masses proven to be ccRCC after resection (n=15) were detected with (111)In-girentuximab. Suspect lesions of six patients showed no uptake of (111)In-girentuximab. In these patients, ccRCC was not found, nor progression occurred. Seven patients with a history of ccRCC and possible metastatic lesions on follow-up computed tomography scans were imaged with (111)In-girentuximab. In four of these patients, the lesions showed preferential uptake of (111)In-girentuximab and local or systemic treatment was initiated. In three other cases, no (111)In-girentuximab targeting was seen. During follow-up of these three patients, one showed progression, for which systemic treatment was started. In the two other patients, no progression occurred, suggesting a benign nature. Conclusions: (111)In-girentuximab immunoSPECT can be used to detect ccRCC lesions in patients with a primary renal mass and to clarify the nature of lesions suspect for metastases in patients with a history of ccRCC.