OBJECTIVE To describe the pharmacology, pharmacokinetics, efficacy, and safety of tenecteplase in reducing mortality associated with acute myocardial infarction (AMI). METHODS Published articles were identified from MEDLINE (from 1966 to December 2000) and Current Contents (all sections) searches. METHODS Dose-ranging and pivotal studies were included for analysis in the clinical trials section. RESULTS Tenecteplase is a third-generation thrombolytic indicated for the reduction of mortality associated with AMI. Tenecteplase has a longer half-life that allows for single-dose, intravenous bolus administration. Data from clinical trials support that tenecteplase is similar to alteplase in reducing 30-day mortality rates in patients who have had an AMI. In the ASSENT-2 (Assessment of the Safety and Efficacy of a New Thrombolytic) trial, patients treated with tenecteplase required fewer blood transfusions and experienced fewer episodes of noncerebral bleeding compared with those treated with alteplase. CONCLUSIONS Tenecteplase is an effective thrombolytic agent for the treatment of AMI. It can be given as a single weight-based dose; however, it appears to offer no significant advantage over other agents in terms of its efficacy or rate of intracranial hemorrhage.