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Expert Opin Investig Drugs ; 9(11): 2689-94, 2000 Nov.
Article in English | MEDLINE | ID: mdl-11060830

ABSTRACT

New bolus fibrinolytic agents derived from the recombinant human tissue plasminogen activator (t-PA) have emerged as a new means of dissolution of the occlusive thrombosis associated with acute myocardial infarction. Lanoteplase is a fibrinolytic drug derived from t-PA by deleting its fibronectin finger-like and epidermal growth factor domains and mutating Asn(117) to Gln(117). Lanoteplase has a reduced plasma clearance and a prolonged half-life such that it can be administered as a single bolus. In the InTIME I trial, patency (TIMI grade 2 or 3 flow) with the 120 KU/kg dose was higher compared with front-loaded t-PA. The InTIME II trial demonstrated that lanoteplase was as effective as alteplase with regard to mortality. However, the rate of intracranial haemorrhage was significantly higher in lanoteplase-treated patients and further development of this compound has been halted.


Subject(s)
Fibrinolytic Agents/therapeutic use , Myocardial Infarction/drug therapy , Tissue Plasminogen Activator/therapeutic use , Acute Disease , Animals , Clinical Trials as Topic , Coronary Angiography , Fibrinolytic Agents/adverse effects , Fibrinolytic Agents/pharmacokinetics , Fibrinolytic Agents/pharmacology , Humans , Myocardial Infarction/diagnostic imaging , Tissue Plasminogen Activator/adverse effects , Tissue Plasminogen Activator/pharmacokinetics , Tissue Plasminogen Activator/pharmacology
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