拜耳（Bayer）3月3日宣布，已向日本卫生劳动福利部（MHLW）提交了眼科药物Eylea（aflibercept，阿柏西普注射液）上市许可申请（MAA），寻求批准用于糖尿病性黄斑水肿（DME）患者的治疗。Eylea MAA的提交，是基于III期VISTA-DME和VIVID-DME研究的数据。去年11月，拜耳也向MHLW提交了Eylea新适应症申请，寻求批准用于病理性近视继发脉络膜新生血管（myopic CNV，mCNV）的治疗。

目前，Eylea已获欧洲、美国、日本、澳大利亚及其他国家批准，用于新生血管性年龄相关性黄斑变性（wet-AMD）的治疗。此外，Eylea已获美国、欧盟、日本及亚洲和非洲特定国家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。

Berlin, March 3, 2014 – Bayer HealthCare today announced that Bayer Yakuhin, Ltd., Osaka, Japan, has submitted an application for marketing authorization for VEGF Trap-Eye (aflibercept solution for injection) for the treatment of patients with diabetic macular edema (DME) to the Ministry of Health, Labour and Welfare (MHLW) in Japan.

“Clinically significant DME is a leading cause of vision loss in the working age population suffering from diabetes. The number of patients suffering from diabetes on a worldwide basis continues to increase, and with it the need for new treatment options. Whatever a person`s age, vision impairment impacts everyday tasks and has a detrimental effect on quality of life”, said Dr. Joerg Moeller, Member of the Bayer HealthCare Executive Committee and Head of Global Development. “With this filing, we hope to make a significant contribution towards alleviating the impact of this disease for the future in Japan.”

The submission of VEGF Trap-Eye (aflibercept solution for injection) for DME in Japan is based on data from VISTA-DME and VIVID-DME studies. In the Phase 3 VIVID-DME and VISTA-DME trials, VEGF Trap-Eye 2 milligrams (mg) dosed monthly and VEGF Trap-Eye 2 mg dosed every two months (after 5 initial monthly injections), achieved the primary endpoint of significantly greater improvements in best-corrected visual acuity (BCVA) from baseline compared to laser photocoagulation at 52 weeks. One-year data from the VIVID-DME and VISTA-DME trials were already presented at medical congresses in the U.S. and Europe. Both trials are planned to continue up to 148 weeks.

VEGF Trap-Eye has been approved under the brand name EYLEA? in Europe, Japan, Australia, the United States, and in many other countries for the treatment of patients with neovascular age-related macular degeneration (wet AMD). EYLEA has also been approved in Europe for the treatment of visual impairment due to macular edema secondary to central retinal vein occlusion (CRVO) as well as in Japan, in selected countries in Asia, Latin America and the U.S. for the treatment of macular edema following CRVO. Regulatory submissions have also been made in the EU, the U.S., and other countries, for EYLEA for the treatment of Diabetic Macular Edema, and in Japan additionally for the treatment of choroidal neovascularization secondary to pathologic myopia (mCNV).

Bayer HealthCare and Regeneron Pharmaceuticals, Inc. are collaborating on the global development of EYLEA. Regeneron maintains exclusive rights to EYLEA in the United States. Bayer HealthCare licensed the exclusive marketing rights outside the United States, where the companies share equally the profits from sales of EYLEA, except for Japan where Regeneron receives a percentage of net sales.

ab0ut the Phase 3 DME Program

The Phase 3 DME program consists of three double-masked trials: VIVID-DME, VISTA-DME, and VIVID-EAST, and one open label single arm safety trial in Japanese patients (VIVID-Japan). All three double masked studies have three treatment arms, where patients are randomized to receive either VEGF Trap-Eye 2 mg monthly, VEGF Trap-Eye 2 mg every two months (after 5 initial monthly injections), or the comparator treatment of laser photocoagulation. Based on protocol specified criteria, patients were eligible to receive rescue treatment from week 24 onwards. Rescue treatment was adjunct laser treatment for both VEGF Trap-Eye arms and VEGF Trap-Eye 2mg for the laser group. The primary endpoint of these three studies is the mean change in best-corrected visual acuity from baseline, as measured on the Early Treatment Diabetic Retinopathy Scale (ETDRS) eye chart, a standard chart used in research to measure visual acuity. The VIVID-DME, VISTA-DME and VIVID-EAST studies are ongoing.

ab0ut Diabetic Macular Edema (DME)

DME is a common complication of Diabetic Retinopathy (DR), a disease affecting the blood vessels of the retina. Clinically significant DME occurs when fluid leaks into the center of the macula, the light-sensitive part of the retina responsible for sharp, direct vision. Fluid in the macula can cause severe vision loss or blindness.

DME is the most frequent cause of blindness in young and mid-aged adults. The treatable population for DME globally is estimated at ab0ut 6.2 million people. According to the American Diabetes Association, over 18 million Americans currently suffer from diabetes, and many more are at risk for developing diabetes. The incidence of diabetes is steadily climbing and it is projected that up to seven percent of all patients with diabetes will develop DME during their lifetime.

ab0ut VEGF and VEGF Trap-Eye (aflibercept solution for injection)

Vascular Endothelial Growth Factor (VEGF) is a naturally occurring protein in the body. Its normal role in a healthy organism is to trigger formation of new blood vessels (angiogenesis) supporting the growth of the body's tissues and organs. It is also associated with the growth of abnormal new blood vessels in the eye, which exhibit abnormal increased permeability that leads to edema.

VEGF Trap-Eye is a recombinant fusion protein, consisting of portions of human VEGF receptors 1 and 2 extracellular domains fused to the Fc portion of human IgG1 and formulated as an iso-osmotic solution for intravitreal administration. VEGF Trap-Eye acts as a soluble decoy receptor that binds VEGF-A and placental growth factor (PlGF) and thereby can inhibit the binding and activation of their cognate VEGF receptors.

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