2014年9月23日讯 /生物谷BIOON/ --导读：自2011年上市以来，拜耳眼科药物Eylea适应症个数及全球销售一再刷新。今年7-8月，Eylea先后获FDA和欧盟批准，用于糖尿病性黄斑水肿（DME）适应症，是该药在欧美市场收获的第3个适应症。近日，Eylea再次刷新记录，获全球第3大市场——日本批准，用于病理性近视继发脉络膜新生血管（mCNV）适应症。
日本获批mCNV适应症
拜耳（Bayre）和Regeneron制药本周一宣布，眼科药物Eylea（aflibercept，阿柏西普注射液）获日本卫生劳动福利部（MHLW）批准，用于治疗病理性近视继发脉络膜新生血管（myopic CNV，mCNV）所致的视力损害。在日本，病理性近视和mCNV是导致失明的第二大病因。
Eylea mCNV适应症的获批，是基于在日本mCNV患者中开展的III期MYRROP研究的利好数据，数据表明，在治疗的24周，Eylea治疗组在最佳矫正视力（BCVA）从基线平均改善12.1个字母，假注射组BCVA恶化2个字母，数据具有统计学显著差异（p＜0.0001）。
病理性近视（pathologic myopia，PM）通常影响工作年龄（working-age）的成年人，在全球范围内是导致视力丧失的一个主要原因。脉络膜新生血管（CNV）是高度近视最常见危及视力的并发症。未经治疗的myopic CNV患者，长期预后很差，约90%的患者在5年后发展为严重的视力丧失。myopic CNV所致的视力丧失通常影响年龄低于50岁的成年人，因此会对患者的生产力、财务状况、职业期望、生活质量等各个方面产生深远的影响。
适应症一再刷新
Eylea自2011年上市后，新适应症个数和全球销售额不断刷新，数度超过业界预期。今年第二季度，Eylea的表现再次超出业界预期，销售额达4.15亿美元，增长26%。而今年7-8两月，Eylea接连获FDA和欧盟批准，用于糖尿病性黄斑水肿（DME）的治疗，这是糖尿病患者中导致视力丧失的最常见病因。在DME治疗领域，Eylea落后于罗氏和诺华的眼科药物Lucentis，该药已分别于2011年和2012年获欧盟和FDA批准用于DME适应症。
目前，Eylea已获全球80多个国家批准，用于新生血管性（湿性）年龄相关性黄斑变性（wet-AMD）的治疗，已获全球60多个国家批准，用于治疗视网膜中央静脉阻塞（CRVO）继发黄斑水肿（ME）的治疗。此外，Eylea也已获全球30多个国家批准，用于糖尿病性黄斑水肿（DME）的治疗。同时，拜耳和Regeneron已向欧盟、日本、美国提交了Eylea治疗视网膜分支静脉阻塞（BRVO）继发黄斑水肿（ME）的新适应症申请，这也代表着Eylea在欧美市场的第4个新适应症申请。
DR市场将赶超罗氏Lucentis
不过，就在一周前，FDA授予Eylea令人垂涎的突破性疗法认定，用于糖尿病性视网膜病变（DR）的治疗。目前，尚未有任何药物批准用于治疗DR，因此，DR市场将是一个更广阔且非常有利可图的市场，如果Eylea获批，将成为全球首个DR治疗药物。据估计，在美国，约有770万糖尿病性视网膜病变（DR）患者，而糖尿病性黄斑水肿（DME）患者群体仅为250万人。（详见生物谷文章：《FDA授予拜耳Eylea突破性疗法认定——有望成为首个糖尿病性视网膜病变（DR）药物》）
“突破性疗法”认定，旨在加快某些重症治疗新药的开发和审评。目前，“突破性疗法”新药研发正呈上升势头，已有多个“突破性疗法”认定药物获得FDA批准上市。
关于Eylea：
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。（原文链接生物谷）
英文原文：Eylea gets yet another approval, this one in Japan
The approvals, and the sales, just keep piling up for Eylea, the blockbuster that Bayer shares with developer Regeneron ($REGN). Just weeks after getting an important nod in Europe, it has won approval in Japan, the world's third largest market, for use in myopic choroidal neovascularization (myopic CNV).
Bayer announced Monday that the approval by Japan's Ministry of Health, Labour and Welfare was based on positive data from the Phase III MYRROR study in myopic CNV in which patients' vision improved markedly in 24 weeks.
The drugmaker said that in Japan, pathologic myopia and the associated myopic CNV is the second most common cause of blindness. "Myopic CNV has a poor prognosis and more treatment options are needed to address the urgent medical need for these patients, many of whom are of working age," Dr. Joerg Moeller, Bayer's head of global development, said in a statement. "A treatment option that could not only prevent permanent vision loss but could also improve visual acuity would have great benefits for patients with pathologic myopia."
Already blowing past analysts' quarterly forecasts, Eylea keeps getting new approvals that will only add to its sales. In August, Bayer won European approval for the treatment of diabetic macular edema (DME), the most common cause of vision loss among people with diabetes. That came after the FDA approved the drug for the same condition in July. It is behind its main competition in that treatment area. Lucentis, sold by Roche ($RHHBY) and Novartis ($NVS), has been approved for DME in Europe since 2011 and the U.S. since 2012.
But just a week ago the FDA granted Eylea its coveted "breakthrough therapy" designation for treatment of diabetic retinopathy, which opens it up to a quick appraisal process. There are currently no drugs approved for the condition and it is a large and so potentially very lucrative market. The company has said an estimated 7.7 million people in the U.S. have diabetic retinopathy, compared to about 2.5 million that have DME.
Approved in November 2011, in the second quarter Eylea again topped analyst estimates with sales of $415 million, up 26%. Regeneron sells the drug in the U.S., while Bayer sells it outside of the U.S. They share profits equally in those markets, except Japan, where Regeneron gets a royalty on net sales.