Tenecteplase

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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 YesY
ATC code B01AD11
DrugBank DB00031
UNII WGD229O42W YesY
KEGG D02837 YesY
Chemical data
Formula C2561H3919N747O781S40 
Mol. mass 58951.2 g/mol
 YesY (what is this?)  (verify)

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.

Preliminary results show Tenecteplase helps stroke victims. The three-year study was trialled on 75 patients and showed significant improvement with drug use, but more tests will need to be run before the drug is widely used in stroke patients.

Pharmacokinetics[edit]

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[edit]