T enecteplase is an altered form of human tissue plasmin- ogen activator (tPA) indicated for the reduction of mor- tality associated with acute myocardial infarction (AMI). 1,2 It was designed to have increased fibrin specificity, an in- creased half-life, and to exhibit resistance to plasminogen activator inhibitor 1. 2 Tenecteplase is derived from a cell line of Chinese hamster ovary cells; the polypeptide por- tion weighs approximately 58 742 daltons, and the molec- ular formula is C 2558 H 3872 N 738 S 40 . 3 Tenecteplase is the sixth thrombolytic to gain approval for manufacturing and mar- keting by the Food and Drug Administration (FDA). Table 1 lists the thrombolytics approved for use and the FDA-ap- proved indications. 1,4-7 Methods for Selection and Assessment of Literature Computerized literature searches were conducted in MEDLINE (from 1966 to December 2000) and Current Contents (all sections). Search terms included tenecteplase, alteplase, reteplase, acute myocardial infarction, peripheral arterial disease, catheter occlusion, central venous catheter, and stroke. Various tertiary references were used for back- ground information, including pharmaceutical company– prepared monographs. The authors independently reviewed literature identified in the searches. Dose-ranging and piv- otal trials were included in the Clinical Trials section. Pharmacology/Toxicology Structurally, tenecteplase is a 527 amino acid glycopro- tein developed by altering the complementary DNA for The Annals of Pharmacotherapy ■ 2001 October, Volume 35 ■ 1233 Tenecteplase for Treatment of Acute Myocardial Infarction Nannette M Turcasso and Jean M Nappi www.theannals.com Formulary Forum OBJECTIVE: To describe the pharmacology, pharmacokinetics, efficacy, and safety of tenecteplase in reducing mortality associated with acute myocardial infarction (AMI). DATA SOURCES: Published articles were identified from MEDLINE (from 1966 to December 2000) and Current Contents (all sections) searches. STUDY SELECTION AND DATA EXTRACTION: Dose-ranging and pivotal studies were included for analysis in the clinical trials section. DATA SYNTHESIS: 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. KEY WORDS: acute myocardial infarction, tenecteplase. Ann Pharmacother 2001;35:1233-40. ACPE UNIVERSAL PROGRAM NUMBER: 407-000-01-027-H01 Author information provided at the end of the text. Tenecteplase (TNKase, Genentech). by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from by guest on October 11, 2013 aop.sagepub.com Downloaded from