Center for Retina & Macular Disease, Winter Haven, Florida 33880, USA.
Surv Ophthalmol. 2011 Mar-Apr;56(2):95-113. doi: 10.1016/j.survophthal.2010.08.006.
The treatment of ocular neovascular diseases is being revolutionized by intravitreal therapies targeting vascular endothelial growth factor (VEGF). Two agents are approved for treating neovascular age-related macular degeneration and are being evaluated for other retinal conditions: the RNA aptamer pegaptanib and the monoclonal antibody antigen-binding fragment ranibizumab. Bevacizumab, a related antibody, is being used similarly, although its use is off-label. Pegaptanib selectively binds to a VEGF isoform identified as being especially pathogenic in the eye and spares other isoforms, whereas the other two agents nonselectively bind all VEGF isoforms. Because VEGF is involved in a wide variety of physiologic processes, the ocular and systemic safety of anti-VEGF agents is of paramount concern. I provide an overview of safety data for intravitreal anti-VEGF therapies, focusing primarily on randomized, controlled trials. For pegaptanib, an accumulation of data from pivotal trials and a dedicated systemic safety study have revealed no ocular or systemic safety concerns. For ranibizumab, the principal ocular adverse event detected in clinical trials was a low frequency of ocular inflammation, and systemic adverse events included a slightly elevated risk of nonocular hemorrhage and stroke. Safety data from properly designed randomized controlled trials for bevacizumab are not available.
针对血管内皮生长因子 (VEGF) 的眼内治疗正在彻底改变眼部新生血管疾病的治疗方法。有两种药物被批准用于治疗新生血管性年龄相关性黄斑变性,并正在评估其他视网膜疾病的应用:RNA 适体 pegaptanib 和单克隆抗体抗原结合片段 ranibizumab。类似地,相关抗体 bevacizumab 也在被使用,尽管其用途是超适应证的。Pegaptanib 选择性地结合一种在眼部特别具有致病性的 VEGF 亚型,而其他两种药物则非选择性地结合所有 VEGF 亚型。由于 VEGF 参与了广泛的生理过程,因此抗 VEGF 药物的眼部和全身安全性至关重要。我提供了眼内抗 VEGF 治疗的安全性数据概述,主要关注随机对照试验。对于 pegaptanib,主要试验和专门的系统安全性研究的数据积累表明没有眼部或全身安全性问题。对于 ranibizumab,临床试验中检测到的主要眼部不良事件是眼部炎症的低频率,全身不良事件包括非眼部出血和中风的风险略有升高。贝伐单抗的设计合理的随机对照试验的安全性数据尚不可用。