tenecteplase

Tenecteplase
Systematic (IUPAC) name
	Human tissue plasminogen activator
Clinical data
Trade names	Tnkase
AHFS/Drugs.com	monograph
Legal status	℞ Prescription only;
Pharmacokinetic data
Excretion	Liver
Identifiers
CAS number	105857-23-6
ATC code	B01AD11
DrugBank	DB00031
UNII	WGD229O42W
KEGG	D02837
Chemical data
Formula	C2561H3919N747O781S40
Mol. mass	58951.2 g/mol
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/09/19 19:20:06」(JST)

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Tenecteplase (TNK) is an enzyme used as a thrombolytic drug.

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.

Research

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.

Pharmacokinetics

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

External links

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.
http://www.abc.net.au/news/2012-03-22/stroke-study-makes-treatment-breakthrough/3905512

UpToDate Contents

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1. ST上昇型心筋梗塞に対する線溶療法：治療開始 fibrinolytic therapy in acute st elevation myocardial infarction initiation of therapy
2. 入院前の血栓溶解療法の効果 performance of prehospital fibrinolysis
3. ST上昇型心筋梗塞における血栓溶解療法の特性および臨床試験 characteristics of fibrinolytic thrombolytic agents and clinical trials in acute st elevation myocardial infarction
4. ST上昇型心筋梗塞に対する血栓溶解後の経皮的冠動脈インターベンション percutaneous coronary intervention after fibrinolysis for acute st elevation myocardial infarction
5. 急性肺塞栓症および下肢深部静脈血栓症における線溶（血栓溶解）療法 fibrinolytic thrombolytic therapy in acute pulmonary embolism and lower extremity deep vein thrombosis

English Journal

In intermediate-risk acute PE, tenecteplase plus heparin reduced hemodynamic decompensation but increased stroke.

Akl EA, Guyatt GH.
Annals of internal medicine.Ann Intern Med.2014 Sep 16;161(6):JC8. doi: 10.7326/0003-4819-161-6-201409160-02008.
PMID 25222420

Time Is Penumbra: Imaging, Selection and Outcome. The Johann Jacob Wepfer Award 2014.

Davis S1, Donnan GA.
Cerebrovascular diseases (Basel, Switzerland).Cerebrovasc Dis.2014 Sep 16;38(1):59-72. [Epub ahead of print]
The foundation of modern therapy for ischaemic stroke involves reperfusion of the ischaemic penumbra and salvage of threatened but potentially viable brain tissue. Work on imaging of the penumbra and clinical trials using penumbral evaluation or selection have been a major focus of our collaborative
PMID 25227260

Intracoronary thrombolysis in patients with ST-segment elevation myocardial infarction presenting with massive intraluminal thrombus and failed aspiration.

Boscarelli D1, Vaquerizo B2, Miranda-Guardiola F3, Arzamendi D1, Tizon H3, Sierra G3, Delgado G1, Fantuzzi A3, Estrada D1, Garcia-Picart J1, Cinca J1, Serra A1.
European heart journal. Acute cardiovascular care.Eur Heart J Acute Cardiovasc Care.2014 Sep;3(3):229-36. doi: 10.1177/2048872614527008. Epub 2014 Mar 17.
AIM: Massive intracoronary thrombus is associated with adverse procedural results including failed aspiration and unfavourable reperfusion. In this scenario the best treatment remains unknown. We aim to evaluate the effect of low dose intracoronary thrombolysis in patients with ST-segment elevation
PMID 24637066

Japanese Journal

Quantitative analysis of Tenecteplase in rat plasma samples using LC-MS/MS as an alternative for ELISA

BUSCHER B. A. P.,GERRITSEN H.,VAN SCHOLL I.,CNUBBEN N. H. P.,BRULL L. P.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 852(1), 631-634, 2007-06-01
NAID 10025803191