M-118, a novel, low-molecular-weight heparin for the potential treatment of cardiovascular disorders.

Abstract

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.