美国FDA和瑞士批准来尼珠单抗注射液（ranibizumab，Lucentis）上市，突破性治疗造成50岁以上主要由失明引起的老年渗出性视网膜黄斑变性(AMD)患者，推荐一月1次玻璃体内注射0.5mg/0.05mL。本品剂量规格：来尼珠单抗10mg/mL。 美国FDA批准本品是基于2项大规模Ⅲ期临床研究结果：以本品治疗95％患者保持视力达1年，高达40％患者的视力有了改善。 本品的作用机制：来尼珠单抗结合于并抑制形成新血管起着关键作用的蛋白质VEGF-A活性受体部位和此分子生物活性裂解型VEGF110。在眼血管形成模型上，VEGF-A造成新血管形成和渗漏，增加了老年视网膜黄斑变性新血管的形成。在渗出性AMD中，这些血管在视网膜下生长，渗漏血液和液体造成快速损伤形成斑点，影响精细和详细的中心视力。来尼珠单抗结合于内皮细胞表面的VEGF-A1和VEGF-A2受体，减少内皮细胞增生、血管渗漏和新血管形成。 来尼珠单抗最常见的不良反应是结膜出血、眼痛、飞蚊症、眼内压升高和眼内炎症。 通用名称 ranibizumab injection,兰尼单抗注射液 商品名 Lucentis (R) 性状 无色或微黄色无菌注射液 药理作用 [1]本品为一种重组人源化单克 隆抗体,为肠道杆菌(E.coli)在含四环素的培养液中的产物.其受体结合部位是血管内皮生长因子A(VEGF-A),相对分子质量为48 000,包括有生物活性的裂解片段VEGF110.VEGF-A可促进新生血管生成和渗漏,被认为是导致湿性老年黄斑病变的原因.这种结合防止并阻碍了血管受体(VEGFR1和VEGFR2)在血管内皮细胞表面的的相互作用,阻止血管内皮增生,减少了视黄斑区血管的渗漏和视网膜新血管(CNV)的生成.   适应症 Lucentis是表明对于患者的治疗： 新生血管（湿）年龄相关性黄斑变性（AMD） 黄斑水肿的视网膜静脉阻塞（RVO）   剂量和用法 眼科玻璃体腔注射 新生血管（湿）年龄相关性黄斑变性（AMD） Lucentis的0.5毫克（0.05毫升）建议将体内注射每月一次（约28天）管理。 虽然治疗效果较差，可能会减少到每3个月后的前四个注射的注射，如果每月注射是不可行的。相比继续每月给药，剂量每3个月将导致约5个字母（1线）丧失视力的好处，在接下来的9个月，平均，。患者应定期对待。 黄斑水肿视网膜静脉阻塞（RVO） Lucentis的0.5毫克（0.05毫升）建议管理体内注射每月一次（约28天）。 RVO的临床研究中，患者接受6个月，每月注射Lucentis的。尽管光学相干断层扫描和视力再处理标准，然后平均经历的第6个月不治疗的患者，在第7个月的视力损失，指导，而没有人在第6个月治疗的患者。患者应被视为每月。 剂型和优势 10毫克/毫升的解决方案，在玻璃体内注射单用小瓶 禁忌 眼或眼周感染 超敏反应   注意事项： 玻璃体内注射后眼内炎和视网膜脱离，可能会出现。应监测患者在一周后注射。 体内注射60分钟内，人们已经注意到，眼压增加。   不良反应 （Lucentis的治疗的受试者比对照组更频繁报道）最常见的不良反应是结膜出血，眼痛，玻璃体飞蚊症，眼压增高，眼内发炎。 生产商：Genentech公司 更新日期：04/2011 Lucentis (Ranibizumab) Lucentis (ranibizumab) is an eye medication used for a rare disease called the wet type of macular degeneration. It affects the eyes only, by creating new blood vessels right behind the retina. The retina is the most important component of the eye. New blood vessels cause a crowded system behind the eye, resulting in fluids and blood leaking. The active substance – ranibizumab – is actually an antibody that should naturally be produced by the organism. The patients who suffer from this unpleasant disease cannot produce enough of it to prevent it. Other than that, Lucentis (ranibizumab) is prescribed for the treatment of macular edema too, but only when it implies the blood vessels under the retina. The drug can be prescribed after the patient’s eyes are analyzed. It is rarely used as a prevention method, since the disease is unpredictable. Administration Lucentis (ranibizumab) is administered by an injection taken right into your eye. It is a risky procedure that can only be performed by a specialist doctor. Therefore, it is not the type of injection you can get at home, but only in a clinic or a hospital. Prior to getting it, you will have to get a different medication for local anesthesia. The anesthesia is not powerful enough to cause any severe reactions, but just enough to lose any discomfort you might encounter. The injection is normally taken monthly. The treatment may differ from the general instructions though, according to your situation. Normally you will need to take four injections in four months, then you must be reevaluated. In the fortunate case, the injections will go on, but at three months one from another. They will go on like this until the disease is entirely cured. Make sure you don’t miss any appointments or consultations. After getting the Lucentis (ranibizumab) injections, you will be monitored for 30 to 60 minutes, for the doctor to ensure that you are not experiencing any unpleasant secondary effects. Contraindications There are not any contraindications regarding food or beverages. However, you should avoid driving immediately after having a Lucentis (ranibizumab) injection. One of the side effects implies blurry vision. If you have any other eye infections, they must be cured before going on with this treatment. The treatment is also contraindicated in the sufferers who are sensitive to ranibizumab or other ingredients. Adverse reactions The most common adverse reactions to Lucentis (ranibizumab) consist of blurry vision, runny nose, dry or watery eyes or numbness. 罗氏眼疾药Lucentis获准治疗黄斑水肿 近日，美国食品药品管理局（FDA）已批准其Lucentis 用于治疗由于视网膜静脉阻塞（RVO）导致的黄斑水肿。这是该药获准的最新适应证，此前它已获准用于治疗湿性老年黄斑病变。 该药新适应证获准的重要依据是两项临床试验数据：其中一项名为BRAVO，受试者人数为397人；另外一项研究名为CRUISE，受试人数为392人。在BRAVO试验中，患者接受为期6个月的治疗之后，Lucentis（0.5毫克）受试组在最佳矫正视力（BCVA）检测时，在视力检测表中比原来多辨认15个字母以上的人数比例达到61%，而对照组仅为29%。在CRUISE试验中，Lucentis受试组达到上述效果的人数比例达到48%，而对照组仅为17%。 罗氏相关负责人表示：“Lucentis新适应证的获准让这类患者多了一种治疗选择，而且临床试验结果也已显示患者用药后视力能得到很大的改善并能够保持，其中有人用药7天后就能看到效果。” 在美国，深受RVO困扰的人超过100万，是由于视网膜血管病而导致视力丧失的第二大原因。 III期临床研究显示：ranibizumab疗效优于维替泊芬 基因技术公司（Genentech）的III期临床研究显示，其在研药物ranibizumab（Lucentis）治疗年龄相关性视力减退的疗效优于诺华公司的维替泊芬（verteporfin，Visudyne）。在为期2年研究的头年，94%的0.3mg本品组患者和96%的0.5mg本品组患者视力水平改善或维持，而维替泊芬光动力疗法组仅64%的患者达到该水平。 基因技术公司计划于2005年12月递交本品的上市申请，届时将争取使本品取得优先审批权。在2项关键的III期临床研究中，本品是首个改善湿性年龄相关性黄斑变性（AMD）患者视力的潜力药物，与光动力疗法的“肉搏式”对照研究亦证实本品临床效益更佳。基于这些富有竞争力的临床结论和当前尚未满足的市场需求，所有患者在临床研究的剩余期间均可以接受本品治疗。 Lucentis approved for visual impairment due to retinal vein occlusion Lucentis (ranibizumab) is now approved to treat visual impairment due to macular oedema secondary to retinal vein occlusion (including branch RVO or central RVO). Retinal vein occlusion (RVO) is the second most common retinal vascular disorder after diabetic retinopathy. Occlusion of the outflow channel of the retinal circulation markedly increases intraluminal venous pressure, resulting in haemorrhage, oedema and loss of vision. There are two basic types of vein occlusion:  Branch RVO, in which one of the branches of the main retinal vein is blocked, and central RVO, in which the main vein is blocked. Ranibizumab is a monoclonal antibody fragment which prevents binding of vascular endothelial growth factor (VEGF) to its receptors, with effect on vessel permeability. The new approval follows the BRAVO1 and CRUISE2 studies which tested ranibizumab in patients with visual impairment due to macular oedema secondary to branch RVO (n=397) and central RVO (n=392), respectively. Study design BRAVO and CRUISE were randomised, double-masked, controlled studies that recruited 397 subjects with branch RVO and 392 subjects with central RVO, respectively. In both studies, participants received either ranibizumab 0.3mg or 0.5mg for 12 months or sham injections for 6 months followed by ranibizumab 0.5mg for the next 6 months. 18 letter gains achieved by branch RVO Lucentis-treated patients at 1 year Mean increase in visual acuity at 6 months was significantly greater in the ranibizumab-only group than the sham/ranibizumab group in both studies (Figures 1 and 2; p<0.0001). Gains of 18 letters and 14 letters were achieved by Lucentis-treated patients in the BRAVO and CRUISE studies, respectively.  Overall, 60.3% of ranibizumab patients with branch RVO (BRAVO) and 50.8% of those with central RVO (CRUISE) experienced a gain of 15 or more letters by 12 months, compared with 43.9% and 33.1%, of sham/ranibizumab patients respectively. Lucentis-treated patients experienced a rapid response, with a 7.5 and 9.3 letter gain by day 7, in the BRAVO and CRUISE studies respectively. Figure 1: Mean change of best-corrected visual acuity over time in branch RVO patients (BRAVO) 18 letter gain sustained at 12 months Marked reduction in central foveal thickness In both studies, the improvement of vision was accompanied by a continuous and significant reduction in the macular oedema as measured by central retinal thickness. In sham/ranibizumab patients, the reduction in central foveal thickness was marked after the first as-needed ranibizumab injection and sustained through month 12. The improvement in visual acuity observed with ranibizumab treatment at 6 and 12 months was accompanied by patient-reported benefits as measured by the National Eye Institute Visual Function Questionnaire (VFQ-25) sub-scales related to near and distance activity. No new ocular or nonocular safety events were identified. In both studies, there was a low incidence of serious arterial thromboembolic events (0.7-2.3%) after 12-month ranibizumab treatment and 1 case of death in each of the treatment groups. Conclusion Altogether, these results show that intraocular injections of VEGF-targeting antibody Lucentis provide an effective treatment for macular oedema after retinal vein occlusion, including both branch and central RVO. Lucentis is also licensed for neovascular (wet) age-related macular degeneration and visual impairment due to diabetic macular oedema. Dosing for the new indication is the same as for the other indications: 0.5mg given monthly as a single intravitreal injection until maximum visual acuity is achieved (i.e. visual acuity stable for three consecutive months).