{"title":"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。","authors":"Hriday Shah, Hitinder S Gurm","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>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.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 9","pages":"1059-65"},"PeriodicalIF":0.0000,"publicationDate":"2010-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"M-118, a novel, low-molecular-weight heparin for the potential treatment of cardiovascular disorders.\",\"authors\":\"Hriday Shah, Hitinder S Gurm\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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.</p>\",\"PeriodicalId\":10978,\"journal\":{\"name\":\"Current opinion in investigational drugs\",\"volume\":\"11 9\",\"pages\":\"1059-65\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2010-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current opinion in investigational drugs\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current opinion in investigational drugs","FirstCategoryId":"1085","ListUrlMain":"","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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.