Nielsen Vance G
Department of Anesthesiology, The University of Arizona College of Medicine, P.O. Box 245114, 1501 North Campbell Avenue, Tucson, AZ, 85724-5114, USA.
J Thromb Thrombolysis. 2016 Aug;42(2):288-93. doi: 10.1007/s11239-016-1343-6.
Fibrinogen depletion via catalysis by snake venom enzymes as a therapeutic strategy to prevent or treat thrombotic disorders was utilized for over four decades, with ancrod being the quintessential agent. However, ancrod eventually was found to not be of clinical utility in large scale stroke trial, resulting in the eventual discontinuation of the administration of the drug for any indication. It was hypothesized that ancrod, possessing thrombin-like activity, may have unappreciated robust coagulation kinetics. Using thrombelastographic methods, a comparison of equivalent tissue factor initiated thrombin generation and Calloselasma rhodostoma venom (rich in ancrod activity) on plasmatic coagulation kinetics was performed. The venom resulted in thrombi that formed nearly twice as fast compared to thrombin formed clots, and there was no difference in fibrinolytic kinetics initiated by tissue-type plasminogen activator. In plasma containing iron and carbon monoxide modified fibrinogen, which may be found in patients at risk of stroke, the coagulation kinetic differences observed with venom was still more vigorous than that seen with thrombin. These phenomena may provide insight into the clinical failure of ancrod, and may serve as an impetus to revisit the concept of fibrinogen depletion via fibrinogenolytic enzymes, not those with thrombin-like activity.
通过蛇毒酶催化消耗纤维蛋白原作为预防或治疗血栓性疾病的一种治疗策略已被应用了四十多年,其中安克洛酶是典型药物。然而,最终发现安克洛酶在大规模中风试验中并无临床效用,导致该药物最终停止用于任何适应症。据推测,具有凝血酶样活性的安克洛酶可能具有未被认识到的强大凝血动力学。使用血栓弹力图方法,对等效组织因子引发的凝血酶生成与红口蝮蛇毒(富含安克洛酶活性)对血浆凝血动力学的影响进行了比较。与凝血酶形成的凝块相比,该毒液导致血栓形成的速度几乎快两倍,并且组织型纤溶酶原激活剂引发的纤溶动力学没有差异。在可能存在于中风风险患者中的含有铁和一氧化碳修饰纤维蛋白原的血浆中,观察到的毒液引起的凝血动力学差异仍然比凝血酶引起的差异更显著。这些现象可能有助于解释安克洛酶的临床失败原因,并可能促使人们重新审视通过纤维蛋白溶解酶而非具有凝血酶样活性的酶来消耗纤维蛋白原的概念。