药品信息 Lucentis治疗湿性老年黄斑变性 近日，英国国家卫生和临床医疗优选研究所推荐Lucentis（雷珠单抗注射液）作为治疗所有湿性老年黄斑变性（AMD）的有效方法，湿性老年黄斑变性是50岁以上人群主要致盲原因。诺丁汉大学医学院眼科副教授Winfried Amoaku说："湿性AMD是一种退行性病变，它能导致患者视力迅速下降，患者会因此丧失自理能力，生活质量也会因此下降。Lucentis能帮助那些有维护或改善视力需求的患者。" Lucentis是专门针对眼科疾病研制的药物，是唯一获得批准的能提高绝大多数湿性老年黄斑变性患者的视力和视力相关功能的治疗药物。7000多名患者参与的临床实验表明，接受Lucentis治疗的患者比未接受治疗的患者视力提高4行（21个字母），这种状况可稳定2年。 处方新修改：批准日期：2013年2月6日；公司：Genentech LUCENTIS(兰尼单抗[ranibizumab]注射剂) 玻璃体内注射 美国初次批准：2006 一般描述 LUCENTIS®(兰 尼单抗[ranibizumab]注射剂)是一种重组人源化IgG1 κ同工型单克隆抗体碎片被设计成为玻璃体注射使用。兰尼单抗结合至和抑制人血管内皮生长因子A (VEGF-A)生物活性。兰尼单抗，缺乏Fc区，有分子量约48 kda和是由大肠杆菌表达系统在营养介质含抗菌素四环素内生产。最终产品中不能检测到四环素。 LUCENTIS是一种在单次使用玻璃小瓶中无菌，无色至浅黄色溶液。LUCENTIS作为无防腐剂，无菌溶液在单次使用玻璃小瓶中供应被设计输送0.05 mL的10 mg/mL LUCENTIS (0.5 mg 剂量小瓶)或6 mg/mL LUCENTIS (0.3 mg剂量小瓶)水溶液有10 mM盐酸组氨酸，10% α,α-海藻糖二水合物，0.01% 聚山梨醇20，pH 5.5。 作用机制 兰尼单抗结合至VEGF-A的活性形式的受体结合部位，包括生物学活性，这个分子的裂解形式，VEGF110。在眼血管生成和血管闭塞模型中曾显示 VEGF-A至心血管形成和渗漏和被认为新生血管年龄相关黄斑变性(AMD)被认为对RVO，和DME后黄斑水肿的病理生理学有贡献。兰尼单抗与 VEGF-A的结合防止VEGF-A与内皮细胞表面其受体(VEGFR1和VEGFR2)相互作用，减低内皮细胞增生，血管渗漏，和新生血管形成。 适应证和用途 LUCENTIS适用于治疗以下患者： （1）新生血管(湿)年龄相关黄斑退行性变性(AMD) （2）视网膜血管闭塞(RVO)后黄斑水肿。 （3）糖尿病黄斑水肿(DME) 剂量和给药方法 只为眼科玻璃体内注射。 新生血管(湿)年龄相关黄斑变性(AMD) 推荐LUCENTIS 0.5mg(0.05mL)玻璃体内注射1月1次(约28天)。 尽管不一样有效，患者可用三次每月剂量治疗接着用较低频数给药与有规则评估。在3次初始每月剂量后9个月，较低频数给药用4-5剂平均是期望维持视力而每月给药可能预期导致得到平均增加1-2字母。患者应定期评估。 尽管不一样有效，患者也可以4次每月剂量后每3个月用1次剂量治疗。与继续每月给药比较，在下9个月每3个月给药将导致平均约5-字母(1-行)视力丧失获益。患者应定期评估。 视网膜血管闭塞(RVO)后黄斑水肿。 （1） 建议玻璃体内注射1个月1次(约28天)LUCENTIS 0.5mg(0.05mL)给药。在RVO临床研究中，患者每月接收LUCENTIS注射共6个月。尽管正是通过光学相干断层扫描[optical coherence tomography]和视力再-治疗标准，据经验患者然后在平均第6个月不治疗，而患者在第6个月不治疗在第7月丧失视力。患者应每个月被治疗。 糖尿病黄斑水肿(DME)。 （1）建议玻璃体内注射1个月1次(约28天)LUCENTIS 0.3mg (0.05mL)给药。 剂型和规格 （1）10mg/mL溶液(LUCENTIS 0.5mg) （2）6mg/mL溶液(LUCENTIS 0.3mg) 禁忌证 （1）眼或眼周围感染。 （2）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离。注射后应监视患者. （2）玻璃体内注射前和后均曾注意到眼内压增加(IOP)。 （3）使用VEGF抑制剂玻璃体后有动脉血栓栓塞事件潜在风险。 （4）在糖尿病黄斑水肿(DME)每个月用LUCENTIS治疗患者比对照组更频繁发生致命性事件. 不良反应 （1）最常见不良反应(LUCENTIS-治疗受试者比对照受试者报道更频繁)是结膜出血，眼痛，玻璃体飞蚊症，和IOP增加。 Lucentis® (ranibizumab injection) is a prescription medicine for the treatment of patients with neovascular (wet) age-related macular degeneration (AMD) and macular edema following retinal vein occlusion (RVO). Status AMD In June 2006, the U.S. Food and Drug Administration (FDA) approved Lucentis for the treatment of neovascular wet AMD after a Priority Review (six-month). The FDA approval of Lucentis in wet AMD is based on data from two large prospective, randomized, masked sham-injection controlled Phase III clinical trials (MARINA and ANCHOR) and one Phase IIIb study (PIER). In the Phase III studies: •Nearly all patients (approximately 95 percent) treated with Lucentis (0.5 mg) maintained (defined as the loss of less than 15 letters in visual acuity) and up to 40 percent improved (defined as the gain of 15 letters or more in visual acuity) vision at one year, as measured on the Early Treatment of Diabetic Retinopathy (ETDRS) eye chart. •On average, patients treated with Lucentis in the MARINA study experienced an improvement from baseline of 6.6 letters at two years compared to a loss of 14.9 letters in the sham group. In the ANCHOR study, patients treated with Lucentis, on average, experienced a 10.7 letter gain from baseline at two years compared to a loss of 9.8 letters in the Visudyne® photodynamic therapy (PDT) control group. •Up to 40 percent of patients treated with Lucentis achieved vision of 20/40 or better. •The most common eye-related side effects were red eye, eye pain, small specks in vision, the feeling that something is in the eye, and increased tears. The most common non-eye-related side effects were nose and throat infection, headache, and respiratory and urinary tract infections. In addition to data from the two pivotal studies, data from the Phase I/II FOCUS and Phase IIIb PIER studies were included in the FDA review. RVO Lucentis was approved by the FDA for macular edema following RVO on June 22, 2010 after a Priority Review (six-month). Lucentis was studied in two prospective, randomized, masked sham-injection controlled Phase III clinical trials — BRAVO and CRUISE: •The BRAVO study assessed the safety and efficacy profile of Lucentis in a total of 397 patients with macular edema following branch-RVO. The percentage of patients in the Lucentis 0.5 study arm who gained 15 or more letters in best-corrected visual acuity (BCVA) from baseline at month six was 61 percent, compared to 29 percent in the sham injection arm. At month six, patients who received 0.5 mg of Lucentis had a mean gain of 18.3 letters compared to 7.3 letters in patients receiving sham injections. •The CRUISE study assessed the safety and efficacy profile of Lucentis in a total of 392 patients with macular edema following central-RVO. The percentage of patients in the Lucentis 0.5 mg study arm who gained 15 or more letters in BCVA from baseline at month six was 48 percent, compared to 17 percent in the sham injection arm. At month six, patients who received 0.5 mg of Lucentis had a mean gain of 14.9 letters, compared to 0.8 letters for patients receiving sham injections. •The adverse events reported in BRAVO and CRUISE were similar to previous studies, and no new safety events were observed. Important Safety Information •Lucentis® (ranibizumab injection) is a prescription medication given by injection into the eye, and it has side effects. Some Lucentis patients have had detached retinas and serious eye infections.  Lucentis should not be used in patients who have an infection in or around the eye or are allergic to Lucentis or any of its ingredients. •Although not uncommon, Lucentis patients have had eye- and non-eye related blood clots (heart attacks, strokes and death). •Some patients have had increases in eye pressure within one hour of an injection. •Serious side effects also include inflammation inside the eye, and rarely, problems related to the injection procedure, such as developing a cataract. These can make a patient’s vision worse. •The most common side effects to a patient’s eye are increased redness in the whites of the eye, eye pain, small specks in vision, and the feeling that something is in the eye. The most common non-eye-related side effects are nose and throat infections, headache, and respiratory (lung) infections. •If a patient's eye becomes red, sensitive to light, painful, or has a change in vision, they should call or visit their eye doctor right away. •Please visit www.lucentis.com for the Lucentis full prescribing information, and additional important safety information. Proposed Mechanism of Action  Lucentis is designed to bind and inhibit vascular endothelial growth factor (VEGF)-A, a protein that is believed to play a critical role in the formation of new blood vessels (angiogenesis) and the hyperpermeability (leakiness) of the vessels. In wet AMD, these blood vessels grow under the retina and leak blood and fluid, causing rapid damage to the macula, the portion of the eye responsible for fine, detailed central vision. In RVO, angiogenesis and hyperpermeability can lead to macular edema, the swelling and thickening of the macula, which is the portion of the eye responsible for fine, detailed central vision. Age-Related Macular Degeneration (AMD)  AMD is a major cause of gradual or sudden, painless, central visual loss in the elderly, brought on by deterioration of the macula and is a leading cause of vision loss in people age 60 and older. There are two forms of AMD — wet and dry. All cases begin as the dry form, but 10 percent to 15 percent progress to the wet form, which can result in sudden and severe central vision loss. More than 1.7 million Americans have the advanced form of this condition. Retinal Vein Occlusion (RVO) RVO affects more than 1 million people in the United States and is the second-most common cause of vision loss due to retinal vascular disease, which can develop over a long period of time or occur suddenly. It occurs when the normal blood flow through a retinal vein becomes blocked, causing swelling (edema) and hemorrhages in the retina, which may result in vision loss. RVO is commonly caused by a clot in the retinal vein. Sudden blurring or vision loss in all or part of one eye is common with RVO, although loss of vision can develop over a long period of time. RVO typically affects patients who are more than 50 years old, and the incidence increases with age. People with a history of high blood pressure, hypertension, diabetes and atherosclerosis are at an increased risk for developing RVO. There are two main types of RVO: branch-RVO, which affects an estimated 887,000 people, and central-RVO, which affects an estimated 265,000 people in the United States. Branch-RVO, which is three times more common than central-RVO, occurs when one of the smaller veins emptying into the main vein of the eye becomes blocked. Usually, the blockage occurs at the site where an artery and a vein cross, and affects only a portion of the retina. Central-RVO, the less common form of RVO, occurs when the main vein of the eye (located at the optic nerve) becomes blocked. 雷珠单抗(Lucentis)-治疗糖尿病黄斑水肿再添新证 最新消息报道称，两项评价用于评价雷珠单抗注射液(Lucentis)对糖尿病患者黄斑水肿（DME）作用的3期试验中的第二项已实现了其主要终点。 此项名为RIDE的研究的主要终点显示，经过24个月的治疗后，雷珠单抗注射液组比开始时多阅读视力表上15个字母以上的患者明显多于对照组。药品安全性也与先前的Lucentis3期试验一致。RIDE研究的结果将于2011年5月29日在伦敦召开的欧洲视网膜大会上公布。 早在今年二月，基因泰克公司宣布雷珠单抗注射液对黄斑水肿患者作用的3期试验中的第一项——RISE研究——已实现了主要终点。研究结果显示，接受雷珠单抗注射液治疗的黄斑水肿患者，用药后第七天开始并且维持24个月的快速持久的视力改善。RISE研究结果于3月10日在黄斑学会会议上公布。 黄斑水肿是一种以眼睛视网膜肿胀为特点的病变，是I型或II型糖尿病患者最常见并发症之一，可引起视力模糊、严重的视力丧失和失明。在发达国家，黄斑水肿是人口致盲的最主要原因之一，目前尚没有获美国FDA批准专治药物。RIDE及RISE研究是相同的三期试验，均是为向美国食品及药品管理局申请上市而设计，即将Lucentis用于治疗黄斑水肿的潜在新适应症的支持性研究。 RISE与RIDE这2项研究结果均证实，雷珠单抗注射液治疗的黄斑水肿患者视力能获得明显改善，雷珠单抗注射液有望为临床治疗黄斑水肿的提供了一种潜在新选择。 附件： 201041222295922.pdf -------------------------------------------------------------- 注：以下产品不同规格和不同价格，购买以咨询为准！ -------------------------------------------------------------- 产地国家: 西班牙 原产地英文商品名: LUCENTIS 10mg/Vial 原产地英文药品名: RANIBIZUMAB 中文参考商品译名: 乐明睛 10毫克/瓶 中文参考药品译名: 雷珠单抗 生产厂家中文参考译名: 诺华制药 生产厂家英文名: NOVARTIS FARMACEUTICA -------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: LUCENTIS 0.3mg/Vial 原产地英文药品名: RANIBIZUMAB 中文参考商品译名: 乐明睛 0.3毫克/瓶 中文参考药品译名: 雷珠单抗 生产厂家中文参考译名: 基因技术公司 生产厂家英文名: GENENTECH -------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: LUCENTIS 3mg/Vial 原产地英文药品名: RANIBIZUMAB 中文参考商品译名: 乐明睛 3毫克/瓶 中文参考药品译名: 雷珠单抗 生产厂家中文参考译名: 基因技术公司 生产厂家英文名: GENENTECH -------------------------------------------------------------- 产地国家: 美国 原产地英文商品名: LUCENTIS 10mg/ml 0.23ml/vial 原产地英文药品名: RANIBIZUMAB 中文参考商品译名: 乐明睛 10毫克/毫升 0.23毫升/瓶 中文参考药品译名: 雷珠单抗 生产厂家中文参考译名: 基因技术公司 生产厂家英文名: GENENTECH 该药品相关信息网址1: http://www.lucentis.com 该药品相关信息网址2: http://www.drugs.com/lucentis.html 该药品相关信息网址3: http://www.medilexicon.com/drugs/lucentis.php