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Tenecteplase

Pharmaceutical drug From Wikipedia, the free encyclopedia

Tenecteplase, sold under the brand name Tnkase among others, is an enzyme used as a thrombolytic drug.[1]

Quick Facts Clinical data, Trade names ...
Tenecteplase
Clinical data
Trade namesTnkase
AHFS/Drugs.comMonograph
MedlinePlusa625007
License data
Routes of
administration		Intravenous
Drug classTissue plasminogen activator
ATC code
Legal status
Legal status
Pharmacokinetic data
ExcretionLiver
Identifiers
  • Human tissue plasminogen activator
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC2561H3919N747O781S40
Molar mass58951.37 g·mol−1
 NY (what is this?)  (verify)
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Tenecteplase is a tissue plasminogen activator (tPA) produced by recombinant DNA technology using an established mammalian cell line (Chinese hamster ovary cells).[1] Tenecteplase is a 527 amino acid glycoprotein developed by introducing the following modifications to the complementary DNA 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.[1]

Tenecteplase was approved for medical use in the United States in June 2000.[1][3]

Medical uses

Tenecteplase is indicated to reduce the risk of death associated with acute ST elevation myocardial infarction and acute ischemic stroke.[1][4]

Pharmacokinetics

Distribution: approximates plasma volume

Metabolism: Primarily liver

Half-life elimination: Biphasic: Initial: 20–24 minutes; Terminal: 90–130 minutes

Excretion: Clearance: Plasma: 99–119 mL/minute

Gallery

  • Thumb
    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.
  • Thumb
    In human t-PA, the amino acids at position 296–299 are lysine, histidine, and two arginines.
  • Thumb
    In TNK-tPA, these amino acids have been replaced by four alanines. This mutation is responsible for increased resistance to PAI-1.

Research

Researchers at Newcastle University in Australia say they have had a significant breakthrough in treating stroke patients using the commonly used drug.[5] The findings were published in the New England Medical Journal. Though safety has been established through previous clinical trials, there is ongoing debate about whether this is an effective treatment for ischemic stroke, and significant ongoing discussion between emergency physicians, neurologists and pharmacists about whether this treatment should be used for that indication.

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.[6]

References

Further reading

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