Tenecteplase in current clinical practice

Česká verzia

Authors: S. Janoušek
Authors place of work: Interní kardiologická klinika, FN Brno‑Bohunice
Published in the journal: Kardiol Rev Int Med 2010, 12(1): 46-53

Summary

Tenecteplase is the third generation thrombolytic agent produced by genetic engineering by mutation of the classical Plasminogen Activator (tPA) and with the main aim to increase resistence against natural Plasminogen Activator Inhibitor (PAI‑ l) and prolongation of its biological halftime. Tenecteplase is fibrin‑specific and, as its substantial advantage, its halftime allows IV administration by single bolus. Recently, it has become the trombolytic agent of the first choice in the developed countries for the treatment of acute myocardial infarction (AMI) with ST‑segment elevation (STEMI) and its properties predestine it to be an ideal drug for pre‑hospital treatment. At present, a large international multicentric study STREAM is under way to evaluate its benefits in the early stage of AIM over direct coronary angioplasty. It has been used with favourable results in other acute clinical indications, such as a pulmonary embolism and arterial and venous closure. However, no randomized trials have been conducted so far in these indications. The possibility of its application in acute ischemic stroke is being verified, the small randomized studies performed so far have provided favourable results.

Keys words:
tenecteplase – acute myocardial infarction – pre‑hospital treatment – acute pulmonary embolism –

acute vessel closure – acute ischemic stroke

Zdroje

1. Tillett WS, Garner RL. The fibrinolytic activity of hemolytic streptococci. J Exp Med 1933; 58: 485– 502.

2. Collen D, Bounameaux H, De Cock F et al. Analysis of coagulation and fibrinolysis during intravenous infusion of recombinant human tissue‑type plasminogen activator in patients with acute myocardial infarction. Circulation 1986; 73: 511– 517.

3. Ueshima S, Matsuo O. Development of new fibrinolytic agents. Curr Pharm Des 2006; 12: 849– 857.

4. Janoušek S. Trombolytická (fibrinolytická) léčba akutního infarktu myokardu. Kardioforum 2006; 4: 66– 80.

5. Tsikouris JP, Tsikouris AP. A review of available fibrin‑specific thrombolytic agents used in acute myocardial infarction. Pharmacotherapy 2001; 21: 207– 217.

6. Modi NB, Eppler S, Breed J et al. Pharmacokinetics of a slower clearing tissue plasminogen activator variant, TNK‑ tPA, in patients with acute myocardial infarction. Thromb Haemost 1998; 79: 134– 139.

7. Serebruany V, Malinin A, Callahan K et al. Effect of tenecteplase versus alteplase on platelets during the first 3 hours of treatment for acute myocardial infarction: The Assessment of the Safety and Efficacy of a New Thrombolytic Agent (ASSENT‑ 2) platelet substudy. Am Heart J 2003; 145: 636– 642.

8. Collen D, Stassen JM, Yasuda T et al. Comparative thrombolytic properties of tissue‑type plasminogen activator and of a plasminogen activator – I‑ resistant glycosylation variant, in a combined arterial and venous

thrombosis model in the dog. Thromb Haemost 1994; 72: 98– 104.

9. Keyt BA, Paoni NF, Refino CJ et al. A faster‑ acting and more potent form of tissue plasminogen activator. Proc Natl Acad Sci USA 1994; 91: 3670– 3674.

10. Benedict CR, Refino CJ, Keyt BA et al. New variant of human tissue plasminogen activator (TPA) with enhanced efficacy and lower incidence of bleeding. compared with recombinant human TPA. Circulation 1995; 92: 3032– 3040.

11. Cannnon CP, McCabe CH, Gibson CM et al. TNK‑ tissue plasminogen activator in acute myocardial infarction. Results of of the Thrombolysis in Myocardial Infarction (TIMI) 10A dose‑ranging trial. Circulation 1997; 95: 351– 356.

12. Cannnon CP, Gibson CM, McCabe CH et al. TNK‑ tissue plasminogen activator compared with front‑ loaded alteplase in acute myocardial infarction. Results of TIMI 10B trial. Circulation 1998; 98: 2805– 2814.

13. van de Werf F, Cannon CP, Luyten A et al. Safety assessment of single‑bolus administration of TNK tissue‑ plasminogen activator in acute myocardial infarction: the ASSENT‑ I trial. The ASSENT‑ I Investigators. Am Heart J 1999; 137: 786– 791.

14. Giugliano RP, McCabe CH, Antman EM et al. Lower‑dose heparin with fibrinolysis is associated with lower rates of intracranial hemorrhage. Am Heart J 2001; 141: 742– 750.

15. Van de Werf F, Adgey J, Ardissino D et al. Single‑bolus tenecteplase compared with front‑ loaded alteplase in acute myocardial infarction: the ASSENT‑ 2 double‑blind randomised trial. Assessment of the Safety and Efficacy of a New Thrombolytic Investigators. Lancet 1999; 354: 716– 722.

16. Van de Werf F, Barron HV, Armstrong PW et al. Incidence and predictors of bleeding events after fibrinolytic therapy with fibrin‑specific agents: a comparison of TNK‑ tPA and rt‑ PA. Eur Heart J 2001; 22: 2253– 2261.

17. Sinnaeve PA, Alexander JB, Belmans AC et al. One‑year follow up of the ASSENT‑ 2 trial: A double‑blind, randomized comparison of single‑bolus tenecteplas and front‑ loaded alteplase in 16,949 patients with ST elevation acute myocardial infarction. Am Heart J 2003; 146: 27– 32.

18. Assessment of the safety and efficacy of a new thrombolytic regimen (ASSENT )‑ 3 investigators. Efficacy and safety of tenecteplase in combination with enoxaparin, abciximab or unfractionated heparin: the ASSENT‑ 3 randomised trial in acute myocardial infarction. Lancet 2001; 358: 605– 613.

19. Kaul P, Armstrong PW, Cowper PA et al. Economic analysis of the assessment of the safety and efficacy of a new thrombolytic regimen (ASSENT‑ 3) study: costs of reperfusion strategies in acute myocardial infarction. Am Heart J 2005; 149: 637– 644.

20. Antman EM, Louwerenburg HW, Baars HF et al. ENTIRE‑ TIMI 23 investigators. Enoxaparin as adjunctive antithrombin therapy for ST‑elevation myocardial infarction: results of the ENTIRE‑ thrombolysis in myocardial infarction (TIMI) 23 Trial. Circulation 2002; 105: 1642– 1649.

21. Giugliano RP, Roe MT, Harrington RA et al. Combination reperfusion therapy with eptifibatide and reduced‑dose tenecteplase for ST‑elevation myocardial infarction: results of the integrilin and tenecteplase in acute myocardial infarction (INTEGRITI) Phase II Angiographic Trial. J Am Coll Cardiol 2003; 41: 1251– 1260.

22. Wallentin L, Goldstein P, Armstrong PW et al. Efficacy and safety of tenecteplase in combination with the low‑ molecular‑weight heparin enoxaparin or unfractionated heparin in the prehospital setting: the Assessment of the safety and efficacy of a new thrombolytic regimen (ASSENT)‑ 3 PLUS randomized trial in acute myocardial infarction. Circulation 2003; 108: 135– 142.

23. Armstrong PW, Chang WC, Wallentin L et al. Efficacy and safety of unfractionated heparin versus enoxaparin: a pooled analysis of ASSENT‑ 3 and‑ 3 plus data. CMAJ 2006; 174: 1421– 1426.

24. Le May MR, Wells GA, Labinaz M et al. Combined angioplasty and pharmacological intervention versus thrombolysis alone in acute myocardial infarction (CAPITAL AMI study). J Am Coll Cardiol 2005; 46: 417– 424.

25. Assessment of the safety and efficacy of a new treatment strategy with percutaneous coronary intervention (ASSENT‑ 4 PCI) investigators. Primary versus tenecteplase‑ facilitated percutaneous coronary intervention in patients with ST‑ segment elevation acute myocardial infarction (ASSENT‑ 4 PCI): randomised trial. Lancet 2006: 367: 569– 578.

26. Mcdonald MA, Fu Y, Zeymer U et al. Adverse outcomes in fibrinolytic‑based facilitated percutaneous coronary intervention: insights from the ASSENT‑ 4 PCI electrocardiographic substudy. Eur Heart J 2008; 29: 871– 879.

27. Armstrong PW. WEST Steering Committee. A comparison of pharmacologic therapy with/ without timely coronary intervention vs primary percutaneous intervention early after ST‑elevation myocardial infarction: the WEST (Which Early ST‑elevation myocardial infarction therapy) study. Eur Heart J 2006; 27: 1530– 1538.

28. Bonnefoy E, Lapostolle F, Leizorovicz A et al. Primary angioplasty versus prehospital fibrinolysis in acute myocardial infarction: a randomised study. Lancet 2002; 360: 825– 829.

29. Fernández‑ Avilés F, Alonso JJ, Peña G et al. Primary angioplasty vs early routine post‑fibrinolysis angioplasty for acute myocardial infarction with ST‑segment elevation: the GRACIA‑ 2 non‑inferiority, randomized, controlled trial. Eur Heart J 2007; 28: 949– 960.

30. Gibson CM, Karha J, Giugliano RP et al. Association of the timing of ST‑segment resolution with TIMI myocardial perfusion grade in acute myocardioal infarction. Am Heart J 2004; 147: 847– 852.

31. Sabatine MS, Cannon CP, Gibson CM et al. Investigators. Addition of clopidogrel to aspirin and fibrinolytic therapy for myocardial infarction with ST‑segment elevation. N Engl J Med 2005; 352: 1179– 1189.

32. Sabatine MS, Cannon CP, Gibson CM et al. Effect of clopidogrel pretreatment before percutaneous coronary intervention in patients with ST‑elevation myocardial infarction treated with fibrinolytics: the PCI‑ CLARITY study. JAMA 2005; 294: 1224– 1232.

33. STREAM‑ Strategic Reperfusion (With Tenecteplase and Antithrombotic Treatment) Early After Myocardial Infarction. Drug Lib [online]. [http:/ / clinicaltrials. gov/ ct2/ show/ study/ NCT00623623?‑ show_locs=Y#locn].

34. Janoušek S, Groch L, Urbánek P et al. Léčba AIM kombinací přednemocničně podané tenekteplázy a akutní PCI. Kardiol Rev 2008; 10: 58– 61.

35. Goodman SG, Menon V, Cannon CP et al. Acute ST‑segment elevation myocardial infarction: American College of Chest physicians evidence‑based clinical practice guidelines (8th edition). Chest 2008; 133 (Suppl 6): 708S– 755S.

36. Kalla K, Christ G, Karnik R et al. Implementation of guidelines improves the standard of care: the Viennese registry on reperfusion strategies in ST‑elevation myocardial infarction (Vienna STEMI registry). Circulation 2006; 113: 2398– 2405.

37. Ting HH, Rihal CS, Gersh BJ et al. Regional systems of care to optimize timeliness of reperfusion therapy for ST‑elevation myocardial infarction: the Mayo Clinic STEMI protocol. Circulation 2007; 116: 729– 736.

38. Danchin N, Coste P, Ferrières J et al. Comparison of thrombolysis followed by broad use of percutaneous coronary intervention with primary percutaneous coronary intervention with primary percutaneous coronary intervention for ST‑segment‑ elevation acute myocardial infarction: data from the french registry on acute ST‑elevation myocardial infarction (FAST‑MI). Circulation 2008; 118: 268– 276.

39. Kamenský G, Hricák V, Studenčan M et al. Odborné usmernenie Ministerstva zdravotníctva SR pre reperfúznu liečbu akútneho infarktu myokardu s eleváciou ST segmentu. Cardiol 2007; 16: K/ C141– K/ C145.

40. Van De Werf F, Bax J, Betriu A et al. The Task Force on the management of ST‑segment elevation acute myocardial infarction of the European Society of Cardiology. Management of acute myocardial infarction in patients presenting with persistent ST‑segment elevation. Eur Heart J 2008; 29: 2909– 2945.

41. Stein PD, Henry JW. Prevalence of acute pulmonary embolism among patients in a general hospital and at autopsy. Chest 1995; 108: 978– 981.

42. Tebbe U, Graf A, Kamke W et al. Hemodynamic effects of double bolus reteplase versus alteplase infusion in massive pulmonary embolism. Am Heart J 1999; 138: 39– 44.

43. Kline JA, Hernandez‑ Nino J, Jones AE. Tenecteplase to treat pulmonary embolism in the emergency department. J Thromb Thrombolysis 2007; 23: 101– 105.

44. Livaditis IG, Paraschos M. Dimopoulos K. Massive pulmonary embolism with ST elevation in leads V1– V3 and successful hrombolysis with tenecteplase. Heart 2004; 90: e41.

45. Abdulla W, Netter U. Case report. Successful use of tenecteplase in massive pulmonary embolism with cardiopulmonary resuscitation immediately following tracheostomy. Acta Anaesthesiol Belg 2005; 56: 179– 182.

46. Allocca G, Dall‘Aglio V, Nicolosi GL. Tenecteplase for massive pulmonary embolism in a 92‑year‑ old man. Ital Heart J Suppl 2005; 6: 390– 393.

47. Melzer C, Richter C, Rogalla P et al. Tenecteplase for the treatment of massive and submassive pulmonary

embolism. J Thromb Thrombolysis 2004; 18: 47– 50.

48. Caldicott D, Parasivam S, Harding J et al. Tenecteplase for massive pulmonary embolus. Resuscitation 2002; 550: 211– 213.

49. Isma‘eel H, Taher A, Alam S et al. Massive pulmonary embolism in a Lebanese patient doubly heterozygous for MTHFR and factor V Leiden presenting with syncope and treated with tenecteplase. J Thromb Thrombolysis 2006; 21: 179– 184.

50. Hovland A, Bjørnstad H, Hallstensen RF et al. Massive pulmonary embolism with cardiac arrest treated with continuous thrombolysis and concomitant hypothermia. Emerg Med J 2008; 25: 310– 311.

51. Kline JA, Hernandez‑ Nino J, Jones AE. Tenecteplase to treat pulmonary embolism in the emergency department. J Thromb Thrombolysis 2007; 23: 101– 105.

52. Goldhaber SZ. Pulmonary embolism thrombolysis: Do we need another agent? Am Heart J 1999; 138: 1– 2.

53. Spöhr F, Arntz H, Bluhmki E et al. International multicentre trial protocol to assess the efficacy and safety of tenecteplase during cardiopulmonary resuscitation in patients with out‑ of‑ hospital cardiac arrest: the Thrombolysis in Cardiac Arrest (TROICA) Study.

Eur J Clin Invest 2007; 35: 315– 323.

54. Semba CP, Sugimoto K, Razavi MK. Society of Cardiovascular and Interventional Radiology (SCVIR). Alteplase and tenecteplase: applications in the peripheral circulation. Tech Vasc Interv Radiol 2001; 4: 99– 106.

55. Melzer C, Richter C, Kröncke T et al. Fibrinolysis of acute peripheral arterial occlusion with tenecteplase – a new weight‑ optimized treatment regimen. J Thromb Thrombolysis 2004; 18: 43– 46.

56. Hull JE, Hull MK, Urso JA et al. Tenecteplase in acute lower‑ leg ischemia: efficacy, dose, and adverse events. J Vasc Interv Radiol 2006; 17: 629– 636.

57. Burkart DJ, Borsa JJ, Anthony JP et al. Thrombolysis of acute peripheral arterial and venous occlusions with tenecteplase and eptifibatide: a pilot study. J Vasc Interv Radiol 2003; 14: 729– 733.

58. Burkart DJ, Borsa JJ, Anthony JP et al. Thrombolysis of occluded peripheral arteries and veins with tenecteplase: a pilot study. J Vasc Interv Radiol 2002; 13: 1099– 1102.

59. Allie DE, Hebert CJ, Lirtzman MD et al. Novel simultaneous combination chemical thrombolysis/ rheolytic thrombectomy therapy for acute critical limb ischemia: the power‑ pulse spray technique. Catheter Cardiovasc Interv 2004; 63: 512– 522.

60. Arko FR, Davis CM 3rd, Murphy EH et al. Aggressive percutaneous mechanical thrombectomy of deep venous thrombosis: early clinical results. Arch Surg 2007; 142: 513– 518.

61. Parikh S, Motarjeme A, McNamara T et al. Ultrasound‑accelerated thrombolysis for the treatment of deep vein thrombosis: initial clinical experience. J Vasc Interv Radiol 2008; 19: 521– 528.

62. Hacke W, Donnan G, Fieschi C et al. Association of outcome with early stroke treatment: pooled analysis of ATLANTIC, ECASS, and NINDS rt‑ PA stroke trials. Lancet 2004; 363: 768– 774.

63. Saver JL. Number needed to treat estimates incorporating effects over the entire range of clinical outcomes. Arch Neurol 2004; 61: 1066– 1070.

64. Davydov L, Cheng JW. Tenecteplase: a review. Clin Ther 2001; 23: 982– 997.

65. Thomas GR, Thibodeaux H, Errett CJ et al. A long‑half‑life and fibrin‑specific form of tissue plasminogen activator in rabbit models of embolic stroke and peripheral bleeding. Stroke 1994; 25: 2072– 2078.

66. Chapman DF, Lyden P, Lapchak PA et al. Comparison of TNK with wild‑type tissue plasminogen activator in a rabbit embolic stroke model. Stroke 2001; 32: 748– 752.

67. Lapchak PA, Araujo DM, Zivin JA. Comparison of tenecteplase with alteplase on clinical rating score following small clot emoblic strokes in rabbits. Exp Neurol 2004; 185: 154– 159.

68. Haley EC Jr, Lyden PD, Johnston KC et al. TNK in Stroke Investigators. A pilot dose‑escalation safety study of tenecteplase in acute ischemic stroke. Stroke 2005; 36: 607– 612.

69. Clinical Trial. Study of tenecteplase in acute ischemic stroke (TNK‑ S2B). [http:/ / clinicaltrials. gov/ ct2/ show/ NCT00252239].

70. Stroke trials registry: TNKilas trial [online]. [http:/ / www.strokecenter.org/ trials/ TrialDetail. aspx?tid=598].

71. Parsons MW, Miteff F, Bateman GA et al. Acute ischemic stroke: imaging‑ guided tenecteplase treatment in an extended time window. Neurology 2009; 72: 915– 921.

72. Zhang L, Zhang ZG, Zhang C et al. Intravenous administration of a GPIIb/ IIIa receptor antagonist extends the therapeutic window of intra‑ arterial tenecteplase‑ tissue plasminogen activator in a rat stroke model. Stroke 2004; 35: 2890– 2895.

73. Meretoja A, Tatlisumak T. Thrombolytic therapy in acute ischemic stroke – basic concepts. Curr Vasc Pharmacol 2006; 4: 31– 44.

74. Smadja D, Olindo S, Saint‑ Vil M et al. Sequential combination of two intravenous thrombolytics (recombinant tissue plasminogen activator/ tenecteplase) in a patient with stroke and cardioembolic basilar artery occlusion. J Stroke Cerebrovasc Dis 2009; 18: 68– 71.

75. Meretoja A, Tatlisumak T. Novel thrombolytic drugs: will they make a difference in the treatment of ischaemic stroke? CNS Drugs 2008; 22: 619– 629.

76. Schumacher HC, Gupta R, Higashida RT et al. Advances in revascularization for acute ischemic stroke treatment. Expert Rev Neurother 2005; 5: 189– 201.

77. Xavier AR, Siddiqui AM, Kirmani JF et al. Clinical potential of intra‑ arterial thrombolytic therapy in patients with acute ischaemic stroke. CNS Drugs 2003; 17: 213– 224.

78. Qureshi AI, Pande RU, Kim SH et al. Third generation thrombolytics for the treatment of ischemic stroke. Curr Opin Investig Drugs 2002; 3: 1729– 1732.

79. Lopez‑ Atalaya JP, Roussel BD, Levrat D et al. Toward safer thrombolytic agents in stroke: molecular requirements for NMDA receptor‑ mediated neurotoxicity. J Cereb Blood Flow Metab 2008; 28: 1212– 1221.

80. Molina CA, Saver JL. Extending reperfusion therapy for acute ischemic stroke: emerging pharmacological, mechanical, and imaging strategies. Stroke 2005; 36: 2311– 2320.

81. Goldemund D, Mikulík R, Reif M. Trombolytická terapie mozkového infarktu. Kardiol Rev 2008; 10: 168– 176.