M-118是一种新型的低分子量肝素,具有治疗心血管疾病的潜力。

Hriday Shah, Hitinder S Gurm
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引用次数: 0

摘要

安全抑制血栓形成是现代心血管医学的关键治疗策略,未分离肝素(UFH)和低分子肝素(LMWH)在临床中均得到广泛应用。然而,两者都有一些缺点,如UFH的不可预测的药代动力学和低分子肝素的不可逆性。由Momenta制药公司开发的M-118是一种新型的低分子水分子,它克服了UFH和现有低分子水分子的缺点,同时保持了它们的有益特性。在临床前研究和I期临床试验中,M-118显示出对凝血酶和Xa因子的有效活性,可以用鱼精蛋白逆转;M-118的生物利用度高,半衰期短。尽管需要III期临床试验来确定M-118在当代医学中的作用,但在接受冠状动脉介入治疗的患者中进行的II期临床试验中观察到有希望的结果。
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M-118, a novel, low-molecular-weight heparin for the potential treatment of cardiovascular disorders.

Safe inhibition of thrombosis is a key therapeutic strategy in modern cardiovascular medicine, and both unfractionated heparin (UFH) and low-molecular-weight heparin (LMWH) are commonly used in clinical practice. However, both have several drawbacks, such as the unpredictable pharmacokinetics of UFH and the non-reversibility of LMWH. M-118, being developed by Momenta Pharmaceuticals Inc, is a novel LMWH that has been engineered to overcome the drawbacks of UFH and currently available LMWHs, while maintaining their beneficial attributes. In preclinical studies and phase I clinical trials, M-118 demonstrated potent activity against thrombin and Factor Xa, which could be reversed with protamine; M-118 also demonstrated a high and predictable bioavailability, and a short half-life. Promising results were observed in a phase II clinical trial in patients undergoing coronary interventions, although phase III clinical trials are required to establish the role for M-118 in contemporary medicine.

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