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.
Llevadot
J
J
Cardiovascular Division, Brigham & Women's Hospital and Harvard Medical School, Boston, MA, USA.
Guigliano
R P
RP
D000208:Acute Disease; D000818:Animals; D002986:Clinical Trials as Topic; D017023:Coronary Angiography; D005343:Fibrinolytic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D009203:Myocardial Infarction / Q000000981:diagnostic imaging / Q000188:drug therapy*; D010959:Tissue Plasminogen Activator / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*
D005343:Fibrinolytic Agents; C081981:lanoteplase; D010959:Tissue Plasminogen Activator