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|Systematic (IUPAC) name|
|Human tissue plasminogen activator|
|Legal status||℞ Prescription only|
|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.
Preliminary results show Tenecteplase helps stroke victims. The three-year study was trialled on 75 patients and showed significant improvement with drug use, but more tests will need to be run before the drug is widely used in stroke patients.
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
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- 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.