Tenecteplase
 | This article includes a list of general references, but it lacks sufficient corresponding inline citations. (September 2012) |
| Clinical data | |
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| Trade names | TNKase |
| AHFS/Drugs.com | Monograph |
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| Pharmacokinetic data | |
| Excretion | Liver |
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| Chemical and physical data | |
| Formula | C2561H3919N747O781S40 |
| Molar mass | 58951.37 g·mol−1 |
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Tenecteplase, sold under the trade names TNKase, Metalyse and Elaxim, is an
Tenecteplase is a
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.
The abbreviation TNK is common for referring to tenecteplase, but abbreviating drug names is not best practice in medicine, and in fact "TNK" is one of the examples given on the Institute for Safe Medication Practices do-not-use list.
Research
Researchers at Newcastle University in Australia say they have had a significant breakthrough in treating stroke patients using the commonly used drug.
The American Heart Association/American Stroke Association 2019 update to the 2018 guidelines for the Early Management of Acute Ischemic Stroke supports considering tenecteplase over alteplase in patients without contraindication to intravenous thrombolytics.[2]
Pharmacokinetics
Distribution: approximates
Metabolism: Primarily hepatic
Half-life elimination: Biphasic: Initial: 20–24 minutes; Terminal: 90–130 minutes
Excretion: Clearance: Plasma: 99-119 mL/minute
Gallery
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Here is TNK-tPA. It is very similar to t-PA, but the glycosylation occurring in Kringle 1 is manipulated. The mutation T103N means that glycosylation occurs at that point. The mutation N117Q means that the high mannose sugar residue is absent at that point -
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In TNK-tPA, these amino acids have been replaced by fourPAI-1.
References
Further reading
- Gurbel PA, Hayes K, Bliden KP, Yoho J, Tantry US (January 2005). "The platelet-related effects of tenecteplase versus alteplase versus reteplase". Blood Coagulation & Fibrinolysis. 16 (1): 1–7. S2CID 44664652.
- Melzer C, Richter C, Rogalla P, Borges AC, Theres H, Baumann G, Laule M (August 2004). "Tenecteplase for the treatment of massive and submassive pulmonary embolism". Journal of Thrombosis and Thrombolysis. 18 (1): 47–50. S2CID 10947258.
- Ohman EM, Van de Werf F, Antman EM, Califf RM, de Lemos JA, Gibson CM, et al. (July 2005). "Tenecteplase and tirofiban in ST-segment elevation acute myocardial infarction: results of a randomized trial". American Heart Journal. 150 (1): 79–88. PMID 16084152.
- De Luca G, Suryapranata H, Chiariello M (December 2005). "Tenecteplase followed by immediate angioplasty is more effective than tenecteplase alone for people with STEMI. Commentary". Evidence-Based Cardiovascular Medicine. 9 (4): 284–287. PMID 16380055.
- "Primary versus tenecteplase-facilitated percutaneous coronary intervention in patients with ST-segment elevation acute myocardial infarction (ASSENT-4 PCI): randomised trial". Lancet. 367 (9510): 569–578. February 2006. S2CID 23972378.
- Bozeman WP, Kleiner DM, Ferguson KL (June 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. PMID 16563599.
- Hull JE, Hull MK, Urso JA, Park HA (April 2006). "Tenecteplase in acute lower-leg ischemia: efficacy, dose, and adverse events". Journal of Vascular and Interventional Radiology. 17 (4): 629–636. PMID 16614145.
- Peacock M (22 March 2012). "Stroke patients make 'Lazarus-like' recovery". The World Today.
- Parsons M, Spratt N, Bivard A, Campbell B, Chung K, Miteff F, et al. (March 2012). "A randomized trial of tenecteplase versus alteplase for acute ischemic stroke". The New England Journal of Medicine. 366 (12): 1099–1107. PMID 22435369.