Pharmacology and clinical trial results of lanoteplase in acute myocardial infarction

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.