Ranibizumab
(Synonyms: 雷珠单抗; RG-6321) 目录号 : GC19801
Ranibizumab是一种人源化的抗血管内皮生长因子（VEGF）单克隆抗体Fab片段，能够识别所有VEGF-A亚型（包括VEGF110，VEGF121，以及VEGF165）。
Cas No.:347396-82-1
Sample solution is provided at 25 µL, 10mM.
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Ranibizumab is a humanized anti-vascular endothelial growth factor (VEGF) monoclonal antibody Fab fragment that can recognize all VEGF-A isoforms (including VEGF110, VEGF121, and VEGF165)[1]. Ranibizumab inhibits pathological angiogenesis and vascular leakage by blocking the interaction between VEGF-A and receptors (VEGFR1 and VEGFR2). It is mainly used in the treatment of wet age-related macular degeneration (wAMD), diabetic macular edema (DME) and retinal vein occlusion (RVO)[2, 3]. Ranibizumab has high intraocular penetration and low immunogenicity[4].
In vitro, Ranibizumab (0.125mg/mL) treated retinal glial cells (Müller cells) for 24h inhibited the production of inter-photoreceptor compound binding protein (IRBP) in Y79 photoreceptors, without affecting cell viability, the production of neurotrophic factors and the expression of cell stress markers[5]. In vitro, Ranibizumab (0.02-5.17nM) treated human umbilical vein endothelial cells (HUVEC) inhibited rhVEGF165, rhVEGF121, and rhVEGF110-induced HUVEC proliferation in a dose-dependent manner, with IC50 values of 0.44nM, 0.56nM, and 0.23nM, respectively[6].
In vivo, Ranibizumab (2.5, 10mg/kg/day) treated newborn mice by intraperitoneal injection for 4 days had no effect on the weight gain of mice, while the weight gain of mice treated with Aflibercept was significantly impaired[7].
References:
[1] Lien S, Lowman H B. Therapeutic anti-VEGF antibodies[J]. Therapeutic antibodies, 2008: 131-150.
[2] Ferro Desideri L, Barra F, Ferrero S, et al. Clinical efficacy and safety of ranibizumab in the treatment of wet age-related macular degeneration[J]. Expert opinion on biological therapy, 2019, 19(8): 735-751.
[3] Amadio M, Govoni S, Pascale A. Targeting VEGF in eye neovascularization: What's new?: A comprehensive review on current therapies and oligonucleotide-based interventions under development[J]. Pharmacological research, 2016, 103: 253-269.
[4] Stewart M W. Intraocular drugs: pharmacokinetic strategies and the influence on efficacy and durability[J]. Expert Opinion on Drug Metabolism & Toxicology, 2024, 20(10): 977-987.
[5] Shen W, Yau B, Lee S R, et al. Effects of ranibizumab and aflibercept on human Müller cells and photoreceptors under stress conditions[J]. International journal of molecular sciences, 2017, 18(3): 533.
[6] Lowe J, Araujo J, Yang J, et al. Ranibizumab inhibits multiple forms of biologically active vascular endothelial growth factor in vitro and in vivo[J]. Experimental eye research, 2007, 85(4): 425-430.
[7] Ichiyama Y, Matsumoto R, Obata S, et al. Assessment of mouse VEGF neutralization by ranibizumab and aflibercept[J]. PloS one, 2022, 17(12): e0278951.
Ranibizumab是一种人源化的抗血管内皮生长因子（VEGF）单克隆抗体Fab片段，能够识别所有VEGF-A亚型（包括VEGF110，VEGF121，以及VEGF165）[1]。Ranibizumab通过阻断VEGF-A与受体（VEGFR1和VEGFR2）的相互作用，抑制病理性血管生成和血管渗漏，临床主要用于治疗湿性年龄相关性黄斑变性（wAMD）、糖尿病性黄斑水肿（DME）及视网膜静脉阻塞（RVO）[2, 3]。Ranibizumab具有高眼内穿透性、低免疫原性[4]。
在体外，Ranibizumab（0.125mg/mL）处理视网膜神经胶质细胞（Müller细胞）24h，抑制了Y79光感受器中光感受器间类化合物结合蛋白（IRBP）的产生，不影响细胞的活力，不影响细胞产生神经营养因子和细胞应激标志物的表达[5]。在体外，Ranibizumab（0.02-5.17nM）处理人脐静脉内皮细胞（HUVEC），以剂量依赖性方式抑制了rhVEGF165、rhVEGF121和rhVEGF110诱导的 HUVEC增殖，IC50值分别为0.44nM、0.56nM和0.23nM[6]。
在体内，Ranibizumab（2.5, 10mg/kg/day）通过腹腔注射处理新生小鼠4天，对小鼠体重增长没有影响，而用阿柏西普（Aflibercept）处理的小鼠体重增长明显受损[7]。
| Cell experiment [1]: | |
Cell lines | Müller cells (the major type of glial cells in the retina) |
Preparation Method | Clinical doses of Aflibercept (0.5mg/mL) and Ranibizumab (0.125mg/mL) were dissolved in starvation media containing 1% FCS, various concentrations of glucose along with and without CoCl2 (200µM). Müller cells and Y79 photoreceptors were incubated in 12 starvation media containing 1% FCS and other elements including: (1) low glucose (LG); (2) LG+Aflibercep; (3) LG+Ranibizumab; (4) LG+CoCl2 (200µM; (5) LG+CoCl2+Aflibercep; (6) LG+CoCl2+Ranibizumab; (7) high glucose (HG), (8) HG+Aflibercep; (9) HG+Ranibizumab; (10) HG+CoCl2; (11) HG+CoCl2+Aflibercep; (12) HG+CoCl2+Ranibizumab. The effects of Aflibercept and Ranibizumab on cell survival, differential expression of cell stress markers and the production of NT3, BDNF and PEDF as well as IRBP were assessed 24h after incubation. |
Reaction Conditions | 0.125mg/mL; 24h |
Applications | Both Aflibercept and Ranibizumab inhibited the production of IRBP in Y79 photoreceptors. Aflibercept and Ranibizumab are not toxic to Müller cells. Aflibercept and Ranibizumab did not significantly affect the production of neurotrophic factors (NT3, BDNF and PEDF) by Müller cells under the stress conditions we tested. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | PBS, 10mg/kg of Aflibercept, or 2.5mg/kg or 10mg/kg of Ranibizumab was intraperitoneally injected into C57BL/6J mouse neonates daily from P3 to P6. To minimize the effects of individual differences, littermates were divided into the above four groups. The mice were weighed at all time points of injection. At P6, eyes and kidneys were harvested 6h after the last injection. |
Dosage form | 2.5, 10mg/kg/day; i.p. |
Applications | Body weight gain in pups treated with Aflibercept was significantly impaired comparing with other three groups. The body weight gain in pups treated with 2.5mg/kg or 10mg/kg of Ranibizumab was comparable with that in PBS treated pups. |
References: | |
| Cas No. | 347396-82-1 | SDF | |
| 别名 | 雷珠单抗; RG-6321 | ||
| 分子式 | 分子量 | ||
| 溶解度 | Soluble in water | 储存条件 | -80°C, avoid multiple freeze-thaws. |
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Purity: >98.00%
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