Repurposing an old drug to improve the use and safety of tissue plasminogen activator for acute ischemic stroke: minocycline.
Repurposing an old drug to improve the use and safety of tissue plasminogen activator for acute ischemic stroke: minocycline.
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DOI：
10.1592/phco.30.pt2.55s
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发表时间：
2010-07
期刊：
影响因子：
4.1
通讯作者：
Fagan SC
中科院分区：
文献类型：
--
作者：
Hess DC;Fagan SC
只有一种美国食品和药物管理局批准用于急性缺血性卒中的药物：组织纤溶酶原激活剂（tPA）。由于时间窗口短和对脑出血（ICH）的恐惧，tPA仍未得到充分利用。开发与tPA联合使用的药物以提高有利恢复的几率并降低脑出血的风险是非常有兴趣的。米诺环素是一种广谱抗生素，在临床前缺血性脑卒中模型中被发现是一种神经保护剂。二甲胺四环素抑制基质金属蛋白酶-9，这是与tPA使用相关的脑出血的生物标志物。二甲胺四环素也是一种抗炎剂和抑制多聚腺苷核糖聚合酶- 1。米诺环素在迄今为止进行的临床试验中是安全且耐受性良好的。
There is only 1 US Food and Drug Administration-approved drug for acute ischemic stroke: tissue plasminogen activator (tPA). Due to a short time window and fear of intracerebral hemorrhage (ICH), tPA remains underutilized. There is great interest in developing combination drugs to use with tPA to improve the odds of a favorable recovery and to reduce the risk of ICH. Minocycline is a broad spectrum antibiotic that has been found to be a neuroprotective agent in preclinical ischemic stroke models. Minocycline inhibits matrix metalloproteinase-9, a biomarker for ICH associated with tPA use. Minocycline is also an anti-inflammatory agent and inhibits poly (ADP-ribose) polymerase- 1. Minocycline has been safe and well tolerated in the clinical trials conducted to date.