Pegaptanib sodium
(Synonyms: EYE001; NX1838) 目录号 : GC64346
Pegaptanib sodium 是一种靶向血管内皮生长因子 (VEGF)-165 的 RNA适配体。 Pegaptanib 可用于新生血管型老年性黄斑变性的研究。
Cas No.:222716-86-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pegaptanib sodium is an RNA aptamer directed against vascular endothelial growth factor (VEGF)-165. Pegaptanib could be used for the study of neovascular age-related macular degeneration (AMD) [1].
Pegaptanib also inhibits VEGF165-mediated phosphorylation of VEGFR2 and phospholipase Cγ and inhibited VEGF165-induced calcium mobilization in human umbilical vein endothelial cells[1].
[1]. Eugene W M Ng, et al. Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease. Nat Rev Drug Discov. 2006 Feb;5(2):123-32.
| Cas No. | 222716-86-1 | SDF | Download SDF |
| 别名 | EYE001; NX1838 | ||
| 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。 | ||
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| 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。
Pegaptanib sodium for the treatment of neovascular age-related macular degeneration: a review
Clin Ther 2006 Jan;28(1):36-44.PMID:16490578DOI:10.1016/j.clinthera.2006.01.009.
Objective: This article reviews available information on the new selective vascular endothelial growth factor aptamer pegaptanib in the treatment of neovascular age-related macular degeneration (ARMD). The pharmacology, pharmacokinetics, pharmacodynamics, contraindications, and drug-interaction potential of pegaptanib are discussed, and the results of clinical trials evaluating its efficacy and tolerability are summarized. Methods: Relevant articles were identified through searches of MEDLINE (1966-June 2005) and International Pharmaceutical Abstracts (1970-June 2005). The search terms included Pegaptanib sodium, Macugen, age-related macular degeneration, and choroidal neovascularization. The reference lists of identified articles were reviewed for additional publications, and further information was obtained from the manufacturer of pegaptanib. Included studies were review articles and Phase II, III, and IV clinical trials, with preference given to available Phase III studies. Results: Only 1 research group has evaluated the tolerability and efficacy of pegaptanib in patients with neovascular ARMD. The VEGF Inhibition Study in Ocular Neovascularization involved 2 concurrent randomized trials of intravitreous injections of pegaptanib 0.3 mg (n = 294), 1 mg (n = 300), and 3 mg (n = 296) compared with sham injections (n = 296) every 6 weeks for 54 weeks in patients with neovascular ARMD. Assessments were conducted at 6, 12, 18, 24, 30, 42, 48, and 54 weeks. The primary end point was the proportion of patients losing <15 letters on the study eye chart at 54 weeks. This end point was achieved in 70%, 71%, and 65% of patients who received pegaptanib 0.3 (P < 0.001), 1 (P < 0.001), and 3 mg (P = 0.03), respectively, compared with 55% of those receiving the sham injections. Significant improvements in visual acuity with pegaptanib compared with the sham-injection group were seen at all time points (0.3 and 1 mg: P < 0.002; 3 mg: P < 0.05). The sham-injection group was twice as likely to have severe vision loss (loss of > or =30 letters or 6 lines on the eye chart) compared with those receiving pegaptanib 0.3 or 1 mg (P < 0.001). Adverse events reported significantly more often in the pegaptanib group compared with the sham-injection group included vitreous floaters (33% vs 28%, respectively; P < 0.001), vitreous opacities (18% vs 10%; P < 0.001), and anterior-chamber inflammation (14% vs 6%; P = 0.001). Injection-related adverse events during the first year of pegaptanib treatment included endophthalmitis in 12 (1.3%) patients, retinal detachment in 6 (0.7%) patients, and traumatic injury to the lens in 5 (0.6%) patients. Conclusions: There are few published clinical data on pegaptanib. In 2 clinical comparisons with sham injections, pegaptanib was well tolerated and effective in slowing the decline in visual acuity in patients with neovascular ARMD. This agent may be considered an option for the treatment of neovascular ARMD.
Pegaptanib sodium for ocular vascular disease
Indian J Ophthalmol 2007 Nov-Dec;55(6):427-30.PMID:17951898DOI:10.4103/0301-4738.36476.
Pegaptanib sodium (Macugen) is a selective RNA aptamer that inhibits vascular endothelial growth factor (VEGF) 165 , the VEGF isoform primarily responsible for pathologic ocular neovascularization and vascular permeability, while sparing the physiological isoform VEGF 121 . After more than 10 years in development and preclinical study, pegaptanib was shown in clinical trials to be effective in treating choroidal neovascularization associated with age-related macular degeneration. Its excellent ocular and systemic safety profile has also been confirmed in patients receiving up to three years of therapy. Early, well-controlled studies further suggest that pegaptanib may provide therapeutic benefit for patients with diabetic macular edema, proliferative diabetic retinopathy and retinal vein occlusion. Notably, pegaptanib was the first available aptamer approved for therapeutic use in humans and the first VEGF inhibitor available for the treatment of ocular vascular diseases.
Pegaptanib sodium for the treatment of neovascular age-related macular degeneration
Expert Opin Investig Drugs 2005 May;14(5):671-82.PMID:15926872DOI:10.1517/13543784.14.5.671.
This article reviews Pegaptanib sodium, a compound developed by Eyetech Pharmaceuticals Inc. and Pfizer Inc., for the treatment of neovascular age-related macular degeneration (AMD). Traditional treatment approaches to neovascular AMD have included destructive therapies such as thermal laser photocoagulation and photodynamic therapy; the use of Pegaptanib sodium heralds a new treatment approach that is a non-destructive therapy based on the inhibition of vascular endothelial growth factor activity in the eye. This diminishes the neovascular drive in the pathologically hyperpermeable state of the diseased eye. Pegaptanib sodium is one of the first therapeutics belonging to the class of compounds known as aptamers. The chemistry, mechanism of action, pharmacokinetics and rationale for the clinical use of the drug are reviewed. The article highlights and summarises the results of the multi-centre, randomised, sham-controlled clinical trials with Pegaptanib sodium to treat subfoveal choroidal neovascularisation in AMD. In addition, the safety profile is reviewed.
Pegaptanib sodium for the treatment of age-related macular degeneration
Expert Opin Pharmacother 2008 Feb;9(3):499-508.PMID:18220500DOI:10.1517/14656566.9.3.499.
Background: Pegaptanib sodium, the first aptamer therapeutic approved for use and the first antiangiogenic agent used to treat ocular neovascular disease, acts by inhibiting the 165 isoform of vascular endothelial growth factor believed primarily responsible for pathologic ocular neovascularization and vascular permeability. Objective: To briefly present the pharmacology, clinical efficacy and safety, and role of pegaptanib in treating ocular neovascular diseases. Methods: A systematic literature review and synopsis. Results/conclusion: After more than 10 years in development, clinical trials have shown pegaptanib efficacy in treating choroidal neovascularization of age-related macular degeneration. Its excellent ocular and systemic safety profiles have been confirmed in up to 3 years of experience. Early phase, well-controlled studies also suggest therapeutic benefit in diabetic retinopathy and retinal vein occlusion.
Pegaptanib sodium for the treatment of proliferative diabetic retinopathy and diabetic macular edema
Curr Diabetes Rev 2009 Feb;5(1):33-8.PMID:19199896DOI:10.2174/157339909787314158.
Diabetes mellitus is a growing health concern world-wide. Patients with this disease present with a variety of health conditions, including a number of sight-threatening ocular pathologies. Proliferative diabetic retinopathy (PDR) and diabetic macula edema (DME) are common diseases that cause substantial vision impairment in diabetic patients. There has been a strong focus on studying the epidemiology and treatment of these diseases. The recent discovery of vascular endothelial growth factor (VEGF) and its role in the development of proliferative disease, has led to a movement towards treating PDR and DME with anti-angiogenic medications in conjunction with the standard of care. In this review we present a summary of the origination and progression of PDR and DME. This will be followed by a review of clinical data surrounding new anti-angiogenic treatment modalities.