甲磺酸盐鲁比前列酮水合物用于治疗糖尿病性视网膜病变。

Ruboxistaurin mesilate hydrate for diabetic retinopathy.

作者信息

Schwartz Stephen G, Flynn Harry W, Aiello Lloyd Paul

机构信息

Department of Ophthalmology, Bascom Palmer Eye Institute, University of Miami Miller School of Medicine, Naples, FL, USA.

出版信息

Drugs Today (Barc). 2009 Apr;45(4):269-74. doi: 10.1358/dot.2009.45.4.1354195.

DOI:10.1358/dot.2009.45.4.1354195

PMID:19499092

Abstract

Diabetic retinopathy remains a major worldwide cause of preventable blindness. The beta isoform of protein kinase C (PKC) may play an important role in the pathogenesis of this disorder. Ruboxistaurin mesylate hydrate is an orally bioavailable, highly-specific inhibitor of PKC beta, which has shown some efficacy in several large, multicenter, randomized clinical trials. The U.S. Food and Drug Administration issued an approvable letter for ruboxistaurin in 2006, but at this time the medication is not available for routine clinical use.

摘要

糖尿病视网膜病变仍然是全球可预防失明的主要原因。蛋白激酶C（PKC）的β亚型可能在这种疾病的发病机制中起重要作用。甲磺酸鲁索替尼水合物是一种口服生物可利用的、高度特异性的PKCβ抑制剂，在几项大型多中心随机临床试验中已显示出一定疗效。美国食品药品监督管理局于2006年发出了一封关于鲁索替尼的批准信，但目前该药物尚未用于常规临床治疗。