Third-generation thrombolytic drugs.
Several third-generation thrombolytic agents have been developed. They are either conjugates of plasminogen activators with monoclonal antibodies against fibrin, platelets, or thrombomodulin; mutants, variants, and hybrids of alteplase and prourokinase (amediplase); or new molecules of animal (vampire bat) or bacterial (Staphylococcus aureus) origin. These variations may lengthen the drug's half-life, increase resistance to plasma protease inhibitors, or cause more selective binding to fibrin. Compared with the second-generation agent (alteplase), third-generation thrombolytic agents such as monteplase, tenecteplase, reteplase, lanoteplase, pamiteplase, and staphylokinase result in a greater angiographic patency rate in patients with acute myocardial infarction, although, thus far, mortality rates have been similar for those few drugs that have been studied in large-scale trials. Bleeding risk, however, may be greater.
Center for Molecular and Vascular Biology, University of Leuven, Leuven, Belgium.
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D002986:Clinical Trials as Topic; D004341:Drug Evaluation; D005337:Fibrin / Q000187:drug effects / Q000378:metabolism; D005343:Fibrinolytic Agents / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006207:Half-Life; D006801:Humans; D017202:Myocardial Ischemia / Q000097:blood / Q000188:drug therapy*; D010960:Plasminogen Activators / Q000187:drug effects / Q000378:metabolism; D015912:Thrombolytic Therapy / Q000379:methods*; D018180:Thrombomodulin / Q000187:drug effects / Q000378:metabolism
D005343:Fibrinolytic Agents; D018180:Thrombomodulin; D005337:Fibrin; D010960:Plasminogen Activators