英文药名：EYLEA solution for IVT inj.(aflibercept[Genetical Recombination])

中文药名：阿普西柏IVT注射溶液剂

生产厂家：日本拜耳

アイリーア硝子体内注射液40mg/mL

治疗类别名称
眼科※VEGF）抑制剂
※），VEGF：血管内皮生长因子（血管内皮生长因子）审批等。
商標名
EYLEA solution for IVT inj. 40mg/mL
一般名
アフリベルセプト（遺伝子組換え）
Aflibercept（Genetical Recombination）
分子式
C4330H6812N1168O1306S32
（蛋白質部分，2量体）
分子量
約115,000
本質
亚单位组成的人VEGF受体1，人VEGF第一3 Ig结构域受体2，和基因工程融合糖蛋白的两个Ig结构域组成人IgG1的Fc结构域的432个氨基酸残基2分子
操作注意事项
为了维持光屏蔽，此剂可以被存储在考虑到外箱的状态。
条件批准
在建立药品风险管理计划的顶部，要正确使用
药效药理
1.作用机序
Aflibercept（遗传重组）是人VEGF受体1和2的细胞外结构域是结合于人IgG1的Fc结构域的重组融合糖蛋白，作为用于溶解，渗出性年龄相关性黄斑一个诱饵受体于VEGF-a和胎盘生长因子病理性血管发生，并在被认为参与眼疾，如改性（PIGF）发现血管渗漏，通过用比原受体的高亲和力结合，抑制其作用。同样地，也结合到眼病的VEGF-B的参与已报道。人VEGF-A165，VEGF-A121，结合的VEGF-B和PlGF的-2（K D）的解离常数的Aflibercept分别下午12点05分，下午12点36，下午1点09和39pM（体外）。
2. 在动物模型中的作用
在小鼠，大鼠和眼病的动物模型的猴，aflibercept抑制在眼病理性血管发生和血管渗漏的发生。在猴子的激光诱导脉络膜血管新生模型，通过aflibercept的玻璃体内给药，脉络膜新生血管形成的激光损伤后形成（CNV）被抑制，也改善了上形成的CNV病变已经血管渗漏。
适应病症
年龄相关性黄斑变性与凹下脉络膜新生血管
黄斑水肿，由于视网膜静脉阻塞
在病理性近视脉络膜新生血管
糖尿病性黄斑水肿
用法与用量
＊年龄相关性黄斑变性与凹下脉络膜新生血管
为2毫克（为0.05mL）每月，连续三次（诱导期）玻璃体内给药。在随后的维持阶段，通常，每两个月一次，玻璃体内给药。应当指出的是，虽然由症状适当调整给药间隔。
＊黄斑水肿是由于视网膜静脉阻塞，病理性近视脉络膜新生血管
每2毫克的（为0.05mL），用于玻璃体内给药作为aflibercept（基因重组）。给药间隔为一个月或更开的时间。
＊糖尿病性黄斑水肿
2毫克（为0.05mL），每月给五连冠体内施用。在此之后，通常，每两个月一次，是玻璃体内给药。应当指出的是，虽然由症状适当调整给药间隔。
包装规格
玻璃体内注射液40毫克/毫升  1瓶（带针Toeki一头连着专用过滤器）
制造厂商
拜耳药品社有限公司
完整处方资料附件：http://www.info.pmda.go.jp/go/pack/1319405A1027_1_10/

EYLEA solution for IVT inj 40 mg/mL
VEGF inhibitor "Ilea" acquired additional approval for diabetic macular edema-Bayer and Santen
Diabetic macular edema expressed in 3% of all diabetic patients
Bayer Yakuhin Co., Ltd. and Santen Pharmaceutical Co., Ltd. announced on November 18, "Age-related macular degeneration accompanying choroidal neovascularization (exudative age-related macular degeneration)", "Macular edema associated with central retinal vein occlusion" "40 mg/mL Eyre® (R) intravitreal injection solution for ophthalmic use" 40 mg/mL for intravitreal injection for eyelashes "used in the treatment of" choroidal neovascularization in pathologic myopia ", and newly" diabetic macula Edema "to be approved for adaptation announced.
Diabetic macular edema, along with diabetic retinopathy in which retinal blood vessels are impaired, is a common microvascular complication in diabetic patients. Plasma components leak into central fovea of the macular region, which may cause high vision disorder and blindness. Diabetic macular edema accounts for the highest percentage of blindness in young and middle age adults in many developed countries and is estimated to be expressed in about 3% of total diabetic patients in combination with vision impairment.
To the great gospel for patients with diabetes
This approval was conducted based on data of the first year of the VIVID - DME test and the VISTA - DME test, which is a Phase III clinical trial for a total of 862 patients. In the VIVID-DME study conducted in Europe and Japan, we compared allocated to Afrivelescept 2 mg every 5 weeks every 4 weeks and every 8 weeks and group to be subjected to macular laser photocoagulation .
In the group administered every 8 weeks, BCVA at week 52 improved by an average of 10.7 characters compared to baseline. In the laser treatment group, there was an average improvement of 1.2 letters. In the VISTA-DME study conducted in the United States under the same conditions, the Afribelcept dose group improved by an average of 10.7 characters compared to the baseline. In the laser treatment group the average improvement of 0.2 letters was improved.
Professor Hiroko Terasaki, ophthalmologist at Nagoya University, member of the trial coordinating committee of the VIVID-DME trial, said "Diabetic retinopathy is the second largest cause of visual disorder in Japan, of which Diabetic macular edema, which is also said to account for about 20%, has a risk of leading to a high degree of visual acuity Redua, who showed statistically significant improvement in visual acuity compared to the laser treatment group in Phase III clinical trials, We are expecting that it will be a great gospel for patients with diabetes mellitus by becoming a treatment option that can improve vision for diabetic macular edema with the approval of this time. "