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International Journal of Ophthalmology(English edition) 2013年第2期6卷 136-140页

作者： Ebru Eren Akar Veysi ner Cem Küükerdnmez Yonca Aydin Akova Department of Ophthalmology Artvin State Hospital Department of Ophthalmology Recep Tayyip Erdogan University Medical School Department of Ophthalmology Izmir University Medical School Kavaklidere Bayindir Hospital

AIM: To compare the efficacies of subconjunctival bevacizumab, ranibizumab, and pegaptanib sodium injections for the inhibition of corneal neovascularization in an experimental rat model. METHODS: Sixteen corneas of 16 rats were chemically cauterized and randomized into four groups: bevacizumab group that treated with 0.05mL/1.25mg bevacizumab, ranibizumab group that treated with 0.05mL/0.5mg ranibizumab, pegaptanib group that treated with 0.05mL/0.15mg pegaptanib sodium, and control group that treated with 0.05mL saline solution. Digital photographs of the corneas were taken and analyzed using an image analysis software program. All corneas were excised and examined histologically on the 15 th day. RESULTS: Each treatment group had significantly less neovascularized corneal areas and fewer blood vessels than the control group (all P pegaptanib groups (both P pegaptanib groups regarding percentage of neovascularized corneal areas and number of blood vessels (both P >0.05). CONCLUSION: Subconjunctival bevacizumab, ranibiz-umab, and pegaptanib sodium were effective with no corneal epitheliopathy for inhibiting corneal neovascularization after corneal burn in rats .Bevacizumab was more effective than ranibizumab and pegaptanib sodium.

关键词： corneal neovascularization bevacizumab ranibizumab pegaptanib subconjunctival injection

pegaptanib治疗湿性年龄相关性黄斑变性的临床研究

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国际眼科杂志 2006年第4期6卷 829-832页

作者：李夏王雨生第四军医大学西京医院眼科全军眼科研究所中国陕西省西安市710032

年龄相关性黄斑变性(age-relatedmaculardegeneration,AMD)是发达国家老年人的主要致盲眼病,脉络膜新生血管(choroidalneovascularization,CNV)的形成是湿性AMD患者丧失视力的主要原因。CNV的发生机制尚不清楚,已证实血管内皮生长因子(v... 详细信息

年龄相关性黄斑变性(age-relatedmaculardegeneration,AMD)是发达国家老年人的主要致盲眼病,脉络膜新生血管(choroidalneovascularization,CNV)的形成是湿性AMD患者丧失视力的主要原因。CNV的发生机制尚不清楚,已证实血管内皮生长因子(vascularendothelialgrowthfac-tor,VEGF)是诱发CNV的关键因素之一。pegaptanib作为眼科领域应用的第一种VEGF抑制剂,通过抑制CNV形成和血管渗漏,对湿性AMD已初步显示出较传统疗法更优越的治疗效果。随着对CNV发生机制的深入研究,针对病因进行治疗,将有可能更加有效的防治湿性AMD等CNV相关疾病。

关键词：年龄相关性黄斑变性 VEGF抑制剂 pegaptanib Macugen EYE001 NX1838

pegaptanib治疗湿性老年性黄斑变性后视网膜色素上皮脱离

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世界核心医学期刊文摘（眼科学分册） 2006年第10期2卷 61-62页

作者： Singh R.P. Sears J.E. 许娜 Cole Eye Center Cleveland Clinic FoundationCleveland Clinic Lerner Col-lege of MedicineClevelandOHUnited States Dr.

Purpose:To report two cases of retinal pigment epithelium(RPE)tears following intravitreal pegaptanib injections for occult choroidal ***:Noncomparative case ***:The charts of two patients with pigment epithelial tears after receiving intravitreal pegaptanib were *** from the institutional review board and informed consent were obtained before chart *** photos,intravenous fluorescein angiograms,and optical coherence tomography(OCT)were obtained before and after therapy confirmed the ***:Two patients had turbid pigment epithelial detachments(PEDs)and occult choroidal neovascular membranes(CNVMs)treated with intravitreal *** patients developed RPE tears weeks following one intravitreal pegaptanib ***:This report describes the development of RPE tears after intravitreal pegaptanib *** should be taken in cases of turbid pigment epithelial detachments in the monocular patient when treatment with intravitreal pegaptanib is *** studies should be performed to evaluate which subtypes of lesions are most susceptible to this devastating visual complication.

关键词：视网膜色素上皮 pegaptanib 老年性黄斑变性脉络膜新生血管眼底照相荧光素腔内注射隐

pegaptanib治疗新生血管性老年性黄斑变性

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世界核心医学期刊文摘（眼科学分册） 2005年第5期1卷 8-8页

作者： Gragoudas E.S. Adamis A.P. Cunningham Jr. E.T. 陈立军 Ret ina Service Massachusetts Eye and Ear Infirmary Harvard Medical School 243 Ch arles St. Boston MA 02114 United States Dr.

BACKGROUND: pegaptanib, an anti-vascular endothelial growth factor therapy, w as evaluated in the treatment of neovascular age-related macular degeneration. METHODS: We conducted two concurrent, prospective, randomized, double-blind, mu lticenter, dose-ranging, controlled clinical trials using broad entry criteria. Intravitreous injection into one eye per patient of pegaptanib (at a dose of 0. 3 mg, 1.0 mg, or 3.0 mg) or sham injections were administered every 6 weeks over a period of 48 weeks. The primary end point was the proportion of patients who had lost fewer than 15 letters of visual acuity at 54 weeks. RESULTS: In the com bined analysis of the primary end point (for a total of 1186 patients), efficacy was demonstrated, without a dose-response relationship, for all three doses of pegaptanib (Ppegaptanib at 0.3 mg, 70 per cent of patients lost fewer than 15 letters of visual acuity, as compared with 5 5 percent among the controls (P pegaptanib (P pegaptanib (0.3 mg), as compared with sham injection, m aintained their visual acuity or gained acuity (33 percent vs. 23 percent; P=0.0 03). As early as six weeks after beginning therapy with the study drug, and at a ll subsequent points, the mean visual acuity among patients receiving 0.3 mg of pegaptanib was better than in those receiving sham injections (P < 0.002). Among the adverse events that occurred, endophthalmitis (in 1.3 percent of patients), traumatic injury to the lens (in 0.7 percent), and retinal detachment (in 0.6 p ercent) were the most serious and required vigilance. These events were assoc

关键词：老年性黄斑变性 pegaptanib 玻璃体腔注射组视网膜脱离晶体损伤临床试验周给眼内炎并行性

FDA批准pegaptanib用于治疗渗出型年龄相关性黄斑变性

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世界临床药物 2005年第2期26卷 66-66页

2004年12月，FDA批准Eyetech和辉瑞公司的pegaptanib(商品名Macugen)治疗渗出型年龄相关性黄斑变性(AMD)。AMD是发达国家50岁以上老年人视力严重丧失的主要原因。

关键词： FDA pegaptanib 治疗渗出型年龄相关性黄斑变性

呼吸系统、特殊感官及皮肤用药 Eyetech／Pfizer公司的pegaptanib首次获准

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国外药讯 2005年第3期 17-17页

作者：张宇

Eyetech／Pfizer公司的第一个抗VEGF适体类药物Mactlgen(pegaptanib Na)(Ⅰ)获美国FDA批准，用于所有湿性年龄相关性视黄斑变性(wAMD)亚型的治疗。这是此产品首次获准和首次批准一个抗VEGF药物用于此适应症。

关键词：呼吸系统用药特殊感官用药皮肤用药 Eyetech/Pfizer公司 pegaptanib 获批准

Progress of anti-vascular endothelial growth factor therapy for ocular neovascular disease： benefits and challenges

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Chinese Medical Journal 2014年第8期127卷 1550-1557页

作者： Xu Jianjiang Li Yimin Hong Jiaxu Department of Ophthalmology Eye Ear Nose and Throat Hospital School of Shanghai Medicine Fudan University Shanghai 200031 China

publication. Study selection Clinical trials and case studies presented at medical conferences and published in peer-reviewed literature in the past decade were reviewed. Results Anti-VEGF agents have manifested great potential and promising outcomes in treating ocular neovascularization, though some of them are still used as off-label drugs. Intravitrea~ injection of anti-VEGF agents could be accompanied by devastating ocular or systemic complications, and intimate monitoring in both adult and pediatric population are warranted. Future directions should be focused on carrying out more well-designed large-scale controlled trials, promoting sustained duration of action, developing safer and more efficient generation of anti-VEGF agents. Conclusions Anti-VEGF treatment has proved to be beneficial in treating both anterior and posterior neovascular ocular diseases. However, more safer and affordable antiangiogenic agencies and regimens are warranted to be explored.

关键词： vascular endothelial growth factor," anti-vascular endothelial growth factor therapy," ranibizumab bevacizumab aflibercept pegaptanib neovascularization angiogenesis safety

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RNA药物研发最新进展

中国药科大学学报 2007年第6期38卷 576-576页

RNA药物研究还处于初级阶段。唯一获得批准的RNA反义药物是诺华、Isis制药的福米韦生(fomivirsen、Vitra-vene),该药主要用来治疗艾滋病人的巨细胞病毒性视网膜炎。另一个是辉瑞、OSI制药的哌加他尼(pegaptanib,Macu-gen),用于治疗老年... 详细信息

RNA药物研究还处于初级阶段。唯一获得批准的RNA反义药物是诺华、Isis制药的福米韦生(fomivirsen、Vitra-vene),该药主要用来治疗艾滋病人的巨细胞病毒性视网膜炎。另一个是辉瑞、OSI制药的哌加他尼(pegaptanib,Macu-gen),用于治疗老年湿性黄斑变性(AMD)。◆反义RNA反义RNA药物ISIS301012由Isis制药开发,用于治疗肿瘤、多发性硬化症、眼部疾病、艾滋病和肌萎缩性脊髓侧索硬化,目前已进入Ⅱ期临床试验阶段。Genta公司的反义药物oblimersen已经向美国和欧洲分别提交了用于治疗复发性慢性淋巴球性白血病和转移性黑色素瘤的申请。用于治疗晚期黑色素瘤的为期3年的Ⅲ期临床试验也将开始。◆RNA干扰治疗AMD的短干扰RNA药物Bevasiranib(Opko健康公司)进入了Ⅲ期临床试验;AGN211745(Allergan公司,治疗AMD)正进入了Ⅱ期临床试验;此外,由辉瑞、Silence Therapeutics公司和夸克生物技术公司共同研发的第3个用于治疗AMD的短干扰RNA药物RTP801i目前也已进入I期临床试验。ALN-RSV01(Alnylam制药公司...

关键词：药物研发 RNA fomivirsen 巨细胞病毒性视网膜炎 pegaptanib Macugen 反义药物福米韦生