IOBA, Campus Miguel Delibes., Universidad deValladolid, Spain.
Curr Pharm Biotechnol. 2011 Mar 1;12(3):386-91. doi: 10.2174/138920111794480606.
To review current data regarding protein Kinase C beta (PKCß) inhibitors and its efficacy in reducing the burden of diabetic retinopathy (DR) and diabetic macular edema (DME).
MEDLINE search (1980-2009) and presentations to major meetings.
DR and DME have emerged as the main cause of visual impairment in working age population. Treatments for DR and DME include good metabolic control, laser photocoagulation and vitrectomy. However, current therapeutic regimes have not yet provided satisfactory visual results. PKC is an intracellular signalling molecule and its activation plays an important role in the development of ocular complications and has become a field of great interest. Several PKC inhibitors have been investigated. Ruboxistaurin, an orally PKCβ inhibitor has demonstrated in vitro and in vivo benefits in dimisnish cell and blood flow alterations related to hyperglycemia and has a potential use as a therapy for DR and DME. The beneficial effect of Ruboxistaurin in them has been demonstrated in preclinical and clinical studies and controlled trials have been conducted during the last decade. The ability of Ruboxistaurin in reducing visual loss in patients with DR has been demonstrated in the PKC DRS2 trial and DME seems to respond to Ruboxistaurin with both anatomic and functional benefits. The manufacturer, Eli Lilly, has received an approvable letter from the FDA for the prevention of vision loss in patients with DR with Ruboxistaurin, but at this time the medication is not available for clinical use pending results of additional trials for this indication.
回顾蛋白激酶 Cβ（PKCβ）抑制剂的现有数据及其在减轻糖尿病视网膜病变（DR）和糖尿病黄斑水肿（DME）负担方面的疗效。
MEDLINE 检索（1980-2009 年）和主要会议的演讲。
DR 和 DME 已成为工作年龄人群视力损害的主要原因。DR 和 DME 的治疗包括良好的代谢控制、激光光凝和玻璃体切除术。然而，目前的治疗方案尚未提供令人满意的视力结果。PKC 是一种细胞内信号分子，其激活在眼部并发症的发展中起着重要作用，已成为一个极具吸引力的研究领域。已经研究了几种 PKC 抑制剂。Ruboxistaurin，一种口服 PKCβ抑制剂，已证明在体外和体内均能改善与高血糖相关的细胞和血流改变，具有作为 DR 和 DME 治疗药物的潜力。Ruboxistaurin 在这些疾病中的有益作用已在临床前和临床研究中得到证实，并且在过去十年中进行了对照试验。PKC DRS2 试验证明了 Ruboxistaurin 可降低 DR 患者的视力丧失，DME 似乎对 Ruboxistaurin 有反应，具有解剖和功能上的益处。制造商 Eli Lilly 已收到 FDA 的批准信，可将 Ruboxistaurin 用于预防 DR 患者的视力丧失，但在等待该适应症的其他试验结果的同时，该药物尚未可供临床使用。
