II. Indications

  1. ST Elevation Myocardial Infarction (STEMI)
    1. See Thrombolysis in ST Elevation Myocardial Infarction
  2. Acute Ischemic Cerebrovascular Accident (off label)
    1. See Thrombolysis in Cerebrovascular Accident
    2. Tenecteplase use for CVA (instead of t-PA) has become more common due to its single, rapid IV dosing

III. Mechanism

  1. Recombinant Tissue Plasminogen Activator (rt-PA)
    1. Serine protease that binds Fibrin and converts Fibrin-bound plasminogen to plasmin
      1. TNK has a higher Specificity for Fibrin than Alteplase (t-PA)
    2. Plasmin breaks down both Fibrin and Fibrinogen to Fibrin
      1. Fibrin Degradation Products result, which in turn also act to inhibit Fibrin formation

IV. Dosing

  1. ST Elevation Myocardial Infarction (STEMI)
    1. Give a single IV bolus dose over 5 seconds
    2. Once reconstituted, IV solution must be used within 8 hours
    3. Weight <60 kg: 30 mg IV
    4. Weight 60 to 69 kg: 35 mg IV
    5. Weight 70 to 79 kg: 40 mg IV
    6. Weight 80 to 89 kg: 45 mg IV
    7. Weight >=90 kg: 50 mg IV
  2. Cerebrovascular Accident (off-label)
    1. Give a single 0.25 mg/kg (up to 25 mg) IV over 5 to 10 seconds

V. Pharmacokinetics

  1. Half-Life: 20 minutes (contrast with 5 minutes for t-PA)

VI. Adverse Effects: CVA Protocol

  1. Intracerebral Hemorrhage (ICH)
    1. Early data suggested a possible higher risk of ICH compared with t-PA
    2. However, ICH data was based on higher doses (0.4 mg/kg) than current dosing (0.25 mg/kg)
    3. Later 2023 studies at lower dose (0.25 mg/kg) supported the use of TNK over t-PA (see efficacy below)
    4. Marcolini and Swaminathan (2023) Neurocritical Care Mailbag, EM:Rap, December, accessed 12/1/2023
    5. Kvistad (2022) Lancet Neurol 21(6):511-9 +PMID: 35525250 [PubMed]
    6. Qureshi (2023) J Stroke Cerebrovasc Dis 32(2):106898 +PMID: 36493706 [PubMed]

VII. Safety

  1. Unknown safety in pregnancy
  2. Unknown safety in Lactation

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Ontology: Tenecteplase (C0872913)

Definition (NCI) A 527 amino acid glycoprotein and the modified form of the naturally occuring human plasminogen activator (tPA) with tissue plasminogen activating activity. Tenecteplase (TNKase) is a serine protease created by introducing substitutions of threonine 103 with asparagine, asparagine 117 with glutamine within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain. TNKase converts fibrin-bound plasminogen to plasmin by cleaving the Arg/Val bond in plasminogen. Plasmin in turn degrades the fibrin matrix of the thrombus mass, thereby helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Concepts Pharmacologic Substance (T121) , Enzyme (T126) , Amino Acid, Peptide, or Protein (T116)
MSH C121182
SnomedCT 127967007, 387066007
English tenecteplase (medication), tenecteplase [Chemical/Ingredient], tenecteplase, Tenecteplase (product), Tenecteplase (substance), TNK-tPA, Tenecteplase, TENECTEPLASE
Spanish tenecteplasa (producto), tenecteplasa (sustancia), tenecteplasa