拜耳（Bayer）2月10日公布了眼科药物Eylea（aflibercept，阿柏西普注射液）III期VISTA-DME研究的2年期积极数据。该研究在糖尿病性黄斑水肿（DME）患者中开展，数据表明，与激光光凝相比，2种不同的Eylea给药方案，均使最佳矫正视力（BCVA）得到了持续改善。

在VISTA-DME研究中，患者随机接受每月2mg Eylea（n=155）、每2个月2mg Eylea（完成最初5个月每月2mg Eylea治疗后，n=152）或激光光凝治疗（n=154）。数据表明，治疗100周后，每月2mg Eylea治疗组，最佳矫正视力（BCVA）相对基线增加了11.5个字母（52周时为12.5个字母）；每2个月2mg Eylea治疗组，BCVA相对基线增加了11.1个字母（52周时为10.7个字母）；激光光凝治疗组，BCVA相对基线增加了0.9个字母（52周时为0.2个字母）。

此前，拜耳已于2013年8月公布了Eylea治疗DME的2个III期试验VISTA-DME和VISTA-DME的1年期数据（主要分析）。VISTA-DME研究的2年期数据将提交至即将举行的科学会议。VIVID-DME研究的2年期数据预计将于2014年晚些时候获得。这2项研究均将按计划继续开展至148周。

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分别于今年8月和11月获欧盟（EC）和日本批准，用于治疗视网膜中央静脉阻塞(CRVO)继发黄斑水肿（ME）所致的视力损害，同时已获美国及亚洲、非洲特定国家批准用于治疗CRVO继发ME。此外，拜耳已向美国、欧盟及其他国家提交了Eylea治疗糖尿病性黄斑水肿（DME）的监管文件，并在日本提交了Eylea治疗病理性近视继发脉络膜新生血管（mCNV）的监管文件。

关于

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。

英文原文：

Berlin, February 10, 2014 – Bayer HealthCare and Regeneron Pharmaceuticals, Inc. today announced positive two-year results from the Phase III VISTA-DME trial with VEGF Trap-Eye (aflibercept solution for injection) for the treatment of diabetic macular edema (DME). The results demonstrated a sustained improvement with VEGF Trap-Eye in best-corrected visual acuity (BCVA) in two different dosing regimens, compared to laser photocoagulation.

Patients in the VISTA-DME trial were randomized to receive either VEGF Trap-Eye 2 milligrams (mg) monthly (n=155), VEGF Trap-Eye 2 mg every two months (after 5 initial monthly injections) (n=152), or the comparator treatment of laser photocoagulation (n=154).

“DME is a leading cause of vision loss in adults under the age of 50,” said Dr. J?rg M?ller, Member of the Bayer HealthCare Executive Committee and Head of Global Development. “The two-year data confirm the safety and efficacy of VEGF Trap-Eye in treating DME, and we look forward to hopefully offer this new treatment option for DME-patients soon.”

Trial results show that after 100 weeks, patients receiving VEGF Trap-Eye 2 mg dosed monthly had a mean change from baseline in BCVA of 11.5 letters (12.5 letters at 52 weeks). Patients receiving VEGF Trap-Eye 2 mg dosed every two months (after 5 initial monthly injections) had a mean change from baseline in BCVA of 11.1 letters (10.7 letters at 52 weeks). Patients in the laser photocoagulation treatment group had a mean change from baseline in BCVA of 0.9 letters (0.2 letters at 52 weeks).

In the VISTA-DME trial, VEGF Trap-Eye was generally well tolerated with a similar overall incidence of adverse events (AEs), ocular serious AEs, and non-ocular serious AEs across the VEGF Trap-Eye treatment groups and the laser control group. AEs were typical of those seen in other studies in patients with diabetes receiving intravitreal anti-VEGF therapy. The most frequent ocular AEs observed in the VISTA-DME trials included conjunctival hemorrhage, eye pain, and vitreous floaters. The most frequent non-ocular AEs included hypertension, anemia, and urinary tract infection. Arterial thromboembolic events as defined by the Anti-Platelet Trialists' Collaboration (non-fatal stroke, non-fatal myocardial infarction, and vascular death) were similar across the treatment groups and the laser control group with events occurring in 13 out of 155 patients in the group dosed with VEGF Trap-Eye 2 mg monthly, 11 out of 152 patients in the group dosed with VEGF Trap-Eye 2 mg every 2 months (after 5 initial monthly injections), and 9 events out of 154 patients in the laser group. Eight out of 155 patients died in the group dosed with VEGF Trap-Eye 2 mg monthly, four out of 152 patients in the group dosed with VEGF Trap-Eye 2 mg every 2 months (after 5 initial monthly injections), and three out of 154 patients in the laser treatment group.

The 52-week results (primary analyses) from this study have been previously reported. Full two-year data from the VISTA-DME trial will be presented at upcoming medical conferences. Two-year results for the similarly designed VIVID-DME trial will become available later in 2014. Both the VISTA-DME and VIVID-DME trials will continue as planned up to 148 weeks.

VEGF Trap-Eye (aflibercept solution for injection) has been approved under the brand name EYLEA? in Europe, the United States, Japan, Australia, 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 CRVO as well as in the U.S., Japan and in selected countries in Asia and Latin America for the treatment of macular edema following CRVO. Regulatory submissions have also been made in the U.S., the EU, and other countries, for EYLEA for the treatment of Diabetic Macular Edema, and in Japan for the treatment of choroidal neovascularization secondary to pathologic myopia (mCNV).

Bayer HealthCare and Regeneron 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 on net sales.

About the Phase III DME Program

The global Phase III DME program consists of three double-masked trials: VIVID-DME, VISTA-DME, and VIVID-EAST-DME, 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 in the VEGF Trap-Eye groups was adjunct laser treatment, and in the laser control group, it was VEGF Trap-Eye 2mg. The primary endpoint of all 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-DME studies are ongoing.

About 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 about 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.

About 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 (aflibercept solution for injection) 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.

关键词： 拜耳 眼科药物 Eylea III期 阿柏西普注射液

免责声明： 

      本文仅供专业人士学术交流探讨，不作为诊疗及用药依据。 

      如有侵权，请联系我们删除