J. Llevadot et Rp. Giugliano, Pharmacology and clinical trial results of lanoteplase in acute myocardialinfarction, EXPERT OP I, 9(11), 2000, pp. 2689-2694
New bolus fibrinolytic agents derived from the recombinant human tissue pla
sminogen activator (t-PA) have emerged as a new means of dissolution of the
occlusive thrombosis associated with acute myocardial infarction. Lanotepl
ase is a fibrinolytic drug derived from t-PA by deleting its fibronectin fi
nger-like and epidermal growth factor domains and mutating Asn-117 to Gln-1
17. Lanoteplase has a reduced plasma clearance and a prolonged half-life su
ch that it can be administered as a single bolus. In the InTIME I trial, pa
tency (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 w
as as effective as alteplase with regard to mortality. However, the rate of
intracranial haemorrhage was significantly higher in lanoteplase-treated p
atients and further development of this compound has been halted.