近日，美国食品与药物管理局（FDA）批准Eylea(阿柏西普，aflibercept) 治疗有新生血管的年龄相关性黄斑变性（AMD），该病是美国60岁以上人群视力丧失和致盲的首要原因。 两项纳入2412例成年患者的临床试验评价了Eylea的安全性和有效性。参试者接受Eylea或Lucentis（雷珠单抗注射）治疗。两研究的主要终点是治疗一年后病人视力的视敏度。 每4周或每8周，Eylea由眼科医师注入病人眼内。 研究显示，在维持或改善视敏度方面，Eylea与Lucentis同样有效。 接受Eylea病人最常见的副作用包括眼痛、结膜出血、玻璃体漂浮物、白内障和眼压增高。 FDA告诫，Eylea不应用于有活动性眼部感染或有眼内活动性炎症的病人。Eylea尚未在妊娠妇女中进行研究，所以，只有当治疗的潜在益处超过潜在风险时才能用于妊娠妇女。年龄相关的黄斑变性不出现在儿童，Eylea未在儿童中进行研究。 请参阅下文为EYLEA的部份处方资料 EYLEA™ (aflibercept)注射剂或玻璃体内注射 美国初始批准：2011 适应证和用途 EYLEA适用于治疗有新生血管(湿)年龄相关黄斑变性(AMD)患者。 剂量和给药方法 （1）只为眼科玻璃体内注射。 （2）EYLEA的推荐剂量为2mg (0.05mL)给予通过玻璃体注射每4周(每月)对头3个月，接着2mg (0.05mL)通过玻璃体内注射每8周1次(2个月)。 （3）尽管EYLEA可能频如2 mg每4周给药(每月)，当EYLEA每4周给药与每8周比较时未显示增加疗效。 剂型和规格 40mg/mL溶液在单次使用小瓶中为玻璃体内注射。 禁忌证 （1）眼或眼周感染。 （2）活动性眼内炎症。 （3）超敏性 警告和注意事项 （1）玻璃体内注射后可能发生眼内炎和视网膜脱落。应指导患者毫不延缓地报告任何提示性眼内炎或视网膜脱落和应适当处理。 （2）玻璃体内注射60分钟内曾见到眼内压增加。 不良反应 接受EYLEA患者中报道的最常见不良反应(≥5%)是结膜出血，眼疼痛，白内障，玻璃体脱落，玻璃体飞蚊症,和眼内压增加。 EYLEA  AFLIBERCEPT  40MG/ML  INJECTABLE; INJECTION Eylea approved for AMD eye disorder in older people by Sunita Kumar The U.S. Food and Drug Administration approved Eylea (aflibercept) to treat patients with wet (neovascular) age-related macular degeneration (AMD), a leading cause of vision loss and blindness in Americans ages 60 and older. AMD gradually destroys a person's sharp, central vision. It affects the macula, the part of the eye that allows people to see fine detail needed to do daily tasks such as reading and driving. There are two forms of AMD, a wet form and a dry form. The wet form of AMD includes the growth of abnormal blood vessels. The blood vessels can leak fluid into the central part of the retina, also known as the macula. When fluid leaks into the macula, the macula thickens and vision loss occurs. An early symptom of wet AMD occurs when straight lines appear to be wavy. "Eylea is an important new treatment option for adults with wet AMD," said Edward Cox, M.D., M.P.H, director of the Office of Antimicrobial Products in FDA's Center for Drug Evaluation and Research. "It is a potentially blinding disease and the availability of new treatment options is important." The safety and effectiveness of Eylea was evaluated in two clinical trials involving 2,412 adult patients. People in the study received either Eylea or Lucentis (ranibizumab injection). The primary endpoint in each study was a patient's clearness of vision (visual acuity) after one year of treatment. Eylea is injected into the eye either every four weeks or every eight weeks by an ophthalmologist. The studies showed that Eylea was as effective as Lucentis in maintaining or improving visual acuity. The most commonly reported side effects in patients receiving Eylea included eye pain, blood at the injection site (conjunctival hemorrhage), the appearance of floating spots in a person's vision (vitreous floaters), clouding of the eye lens (cataract), and an increase in eye pressure. Eylea should not be used in those who have an active eye infection or active ocular inflammation. Eylea has not been studied in pregnant women, so the treatment should be used only in pregnant women if the potential benefits of the treatment outweigh any potential risks. Age related macular degeneration does not occur in children and Eylea has not been studied in children. Other FDA-approved treatment options for wet AMD include: Visudyne (verteporfin for injection) approved in 2000, Macugen (pegaptanib sodium injection) approved in 2004, and Lucentis (ranibizumab injection) approved in 2006. Eylea is marketed by Tarrytown, N.Y.-based Regeneron Pharmaceuticals Inc. EYLEA (aflibercept) injection, solution [Regeneron Pharmaceuticals, Inc.] HIGHLIGHTS OF PRESCRIBING INFORMATION These highlights do not include all the information needed to use EYLEA safely and effectively. See full prescribing information for EYLEA. EYLEA™ (aflibercept) Injection For Intravitreal Injection Initial U.S. Approval: 2011 INDICATIONS AND USAGE EYLEA is indicated for the treatment of patients with Neovascular (Wet) Age-Related Macular Degeneration (AMD). DOSAGE AND ADMINISTRATION •For ophthalmic intravitreal injection only. •The recommended dose for EYLEA is 2 mg (0.05 mL) administered by intravitreal injection every 4 weeks (monthly) for the first 3 months, followed by 2 mg (0.05 mL) via intravitreal injection once every 8 weeks (2 months). (2.2) •Although EYLEA may be dosed as frequently as 2 mg every 4 weeks (monthly), additional efficacy was not demonstrated when EYLEA was dosed every 4 weeks compared to every 8 weeks. DOSAGE FORMS AND STRENGTHS 40 mg/mL solution for intravitreal injection in a single-use vial CONTRAINDICATIONS •Ocular or periocular infection •Active intraocular inflammation •Hypersensitivity WARNINGS AND PRECAUTIONS •Endophthalmitis and retinal detachments may occur following intravitreal injections. Patients should be instructed to report any symptoms suggestive of endophthalmitis or retinal detachment without delay and should be managed appropriately. (5.1) •Increases in intraocular pressure have been seen within 60 minutes of an intravitreal injection. ADVERSE REACTIONS The most common adverse reactions (≥5%) reported in patients receiving EYLEA were conjunctival hemorrhage, eye pain, cataract, vitreous detachment, vitreous floaters, and increased intraocular pressure. (6.2) To report SUSPECTED ADVERSE REACTIONS, contact Regeneron at 1-855-395-3248 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. See 17 for PATIENT COUNSELING INFORMATION  Storage EYLEA should be refrigerated at 2°C to 8ºC (36°F to 46ºF). Do Not Freeze. Do not use beyond the date stamped on the carton and container label. Protect from light. Store in the original carton until time of use. 17 PATIENT COUNSELING INFORMATION Patients may experience temporary visual disturbances after an intravitreal injection with EYLEA and the associated eye examinations [see Adverse Reactions (6)]. Patients should be advised not to drive or use machinery until visual function has recovered sufficiently. In the days following EYLEA administration, patients are at risk of developing endophthalmitis or retinal detachment. If the eye becomes red, sensitive to light, painful, or develops a change in vision, the patient should seek immediate care from an ophthalmologist [see Warnings and Precautions (5.1)]. 拜耳Eylea新适应症获欧盟批准 2013年8月29日，拜耳（Bayer）8月29日宣布，眼科药物Eylea（aflibercept，阿柏西普注射液）新适应症申请获欧盟委员会（EC）批准，用于治疗视网膜中央静脉阻塞(central retinal vein occlusion,CRVO)继发黄斑水肿（Macular Edema，ME）所致的视力损害。这是Eylea在欧洲获批的第二个适应症，此前，Eylea已获EC批准用于湿性年龄相关性黄斑变性（wet-AMD）的治疗。 在美国，Eylea于2011年11月获FDA批准，用于治疗新生血管性（湿性）年龄相关性黄斑变性（wet-AMD）的治疗，并于2012年9月获FDA批准用于视网膜中央静脉阻塞(CRVO)继发黄斑水肿（ME）的治疗。 Eylea也已获日本、澳大利亚及其他国家批准用于治疗wet-AMD。 Eylea是一种新型玻璃体内注射用VEGF抑制剂，是一种重组融合蛋白，由人体血管内皮细胞生长因子（VEFG）受体1和2的胞外区与人体免疫球蛋白G1的可结晶片段融合而成。 Eylea作为VEGF家族各成员（包括VEGF-A）及胎盘生长因子（PIGF）的一种可溶性诱饵受体发挥作用，与这些因子具有极高的亲和力，从而抑制这些因子与同源VEGF受体的结合，因此Eylea可抑制异常的血管生成及渗漏。 目前，拜耳和Regeneron正在合作Eylea的全球开发。Regeneron保留Eylea在美国的独家权利，拜耳则授权获得该药在美国以外国家和地区的独家销售权，这2家公司将平分Eylea在未来销售的利润。 アイリーア硝子体内注射液40mg/mL 商標名 EYLEA solution for IVT inj. 40mg/mL 一般名 アフリベルセプト（遺伝子組換え） Aflibercept（Genetical Recombination） 分子式 C4330H6812N1168O1306S32 （蛋白質部分，2量体） 分子量 約115,000 本質 ヒトVEGF受容体1の第2 Igドメイン，ヒトVEGF受容体2の第3 Igドメイン，及びヒトIgG1のFcドメインからなる432アミノ酸残基のサブユニット2分子から構成される遺伝子組換え融合糖蛋白質 取扱い上の注意 遮光を保つため，本剤は外箱に入れた状態で保存すること． 包装 アイリーア硝子体内注射液40mg/mL 1バイアル（専用フィルター付き採液針 1本添付） 製造販売元（輸入） バイエル薬品株式会社 完整处方资料附件： 1）：http://www.info.pmda.go.jp/go/pack/1319405A1027_1_05/ 2）：http://www.eylea.jp/ja/home/product/procedure/