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|Systematic (IUPAC) name|
|Human tissue plasminogen activator|
|Mol. mass||58951.2 g/mol|
|(what is this?)|
Tenecteplase is a tissue plasminogen activator (tPA) produced by recombinant DNA technology using an established mammalian cell line (Chinese hamster ovary cells). Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA (cDNA) for natural human tPA: a substitution of threonine 103 with asparagine, and a substitution of asparagine 117 with glutamine, both within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296–299 in the protease domain.
Tenecteplase is a recombinant fibrin-specific plasminogen activator that is derived from native t-PA by modifications at three sites of the protein structure. It binds to the fibrin component of the thrombus (blood clot) and selectively converts thrombus-bound plasminogen to plasmin, which degrades the fibrin matrix of the thrombus. Tenecteplase has a higher fibrin specificity and greater resistance to inactivation by its endogenous inhibitor (PAI-1) compared to native t-PA.
Researchers at Newcastle University in Australia say they have had a significant breakthrough in treating stroke patients using the commonly used drug. The findings were published in the New England Medical Journal. There is ongoing controversy about whether this is a harmful treatment, and significant ongoing discussion between Emergency Physicians and Neurologists about whether this treatment should be used at all.
Distribution: approximates plasma volume
Metabolism: Primarily hepatic
Half-life elimination: Biphasic: Initial: 20-24 minutes; Terminal: 90-130 minutes
Excretion: Clearance: Plasma: 99-119 mL/minute
- MedlinePlus DrugInfo uspdi-500145
- Gurbel P, Hayes K, Bliden K, Yoho J, Tantry U (2005). "The platelet-related effects of tenecteplase versus alteplase versus reteplase.". Blood Coagul Fibrinolysis 16 (1): 1–7. doi:10.1097/00001721-200501000-00001. PMID 15650539.
- Melzer C, Richter C, Rogalla P, Borges A, Theres H, Baumann G, Laule M (2004). "Tenecteplase for the treatment of massive and submassive pulmonary embolism.". J Thromb Thrombolysis 18 (1): 47–50. doi:10.1007/s11239-004-0174-z. PMID 15744554.
- Ohman E, Van de Werf F, Antman E, Califf R, de Lemos J, Gibson C, Oliverio R, Harrelson L, McCabe C, DiBattiste P, Braunwald E (2005). "Tenecteplase and tirofiban in ST-segment elevation acute myocardial infarction: results of a randomized trial.". Am Heart J 150 (1): 79–88. doi:10.1016/j.ahj.2005.01.007. PMID 16084152.
- De Luca G, Suryapranata H, Chiariello M (2005). "Tenecteplase followed by immediate angioplasty is more effective than tenecteplase alone for people with STEMI. Commentary.". Evid Based Cardiovasc Med 9 (4): 284–7. doi:10.1016/j.ebcm.2005.09.021. PMID 16380055.
- Assessment of the Safety and Efficacy of a New Treatment Strategy with Percutaneous Coronary Intervention (ASSENT-4 PCI) investigators (2006). "Primary versus tenecteplase-facilitated percutaneous coronary intervention in patients with ST-segment elevation acute myocardial infarction (ASSENT-4 PCI): randomised trial.". Lancet 367 (9510): 569–78. doi:10.1016/S0140-6736(06)68147-6. PMID 16488800.
- Bozeman W, Kleiner D, Ferguson K (2006). "Empiric tenecteplase is associated with increased return of spontaneous circulation and short term survival in cardiac arrest patients unresponsive to standard interventions.". Resuscitation 69 (3): 399–406. doi:10.1016/j.resuscitation.2005.09.027. PMID 16563599.
- Hull J, Hull M, Urso J, Park H (2006). "Tenecteplase in Acute Lower-leg Ischemia: Efficacy, Dose, and Adverse Events.". J Vasc Interv Radiol 17 (4): 629–36. doi:10.1097/01.RVI.0000202751.74625.79. PMID 16614145.