Tenecteplase

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Tenecteplase
Names
Trade namesTNKase, Metalyse, others
  • Human tissue plasminogen activator
Clinical data
Drug classTissue plasminogen activator (tPA)[1]
Main usesST elevation myocardial infarction (STEMI), pulmonary embolism[1]
Side effectsBleeding[2]
Typical dose30 to 50 mg[1]
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetics
ExcretionLiver
Chemical and physical data
FormulaC2561H3919N747O781S40
Molar mass58951.37 g·mol−1
 ☒NcheckY (what is this?)  (verify)

Tenecteplase (TNK), sold under the trade names TNKase among others, is a medication used to treat ST elevation myocardial infarction or pulmonary embolism with low blood pressure.[1][3] It may also be used for stroke.[3] It is given by injection into a vein.[1]

Common side effects include bleeding such as nosebleeds, gastrointestinal bleeding, bruising, or blood in the urine.[1][2] It should not be used by those with anaphylaxis to gentamicin.[2] It is a tissue plasminogen activator (tPA) produced by recombinant DNA technology.[1] It works by dissolving blood clots.[2]

Tenecteplase was approved for medical use in the United States in 2000 and Europe in 2001.[1][2] In the United Kingdom it costs the NHS about £600 per dose as of 2021.[4] This amount in the United States costs about 6,500 USD.[5]

Medical uses

It is most commonly used for ST elevation myocardial infarction.[1] It may also be used for pulmonary embolism with low blood pressure and to treat stroke.[3][1]

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 people without contraindication to intravenous thrombolytics.[6]

Dosage

For STEMI the typical dose is 30 to 50 mg.[1] It is given over 5 to 10 seconds.[1][2]

The amount of 10,000 units is equal to 50 mg.[7]

Mechanism of action

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.

Pharmacokinetics

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

Manufacture

It 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.

References

  1. 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 "Tenecteplase Monograph for Professionals". Drugs.com. Retrieved 19 September 2021.
  2. 2.0 2.1 2.2 2.3 2.4 2.5 "Metalyse". Retrieved 19 September 2021.
  3. 3.0 3.1 3.2 Burgos, Adrian M.; Saver, Jeffrey L. (August 2019). "Evidence that Tenecteplase Is Noninferior to Alteplase for Acute Ischemic Stroke: Meta-Analysis of 5 Randomized Trials". Stroke. 50 (8): 2156–2162. doi:10.1161/STROKEAHA.119.025080.
  4. BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 231. ISBN 978-0-85711-369-6.CS1 maint: date format (link)
  5. "TNKase Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 19 September 2021.
  6. "Guidelines for the Early Management of Patients With Acute Ischemic Stroke: 2019 Update to the 2018 Guidelines for the Early Management of Acute Ischemic Stroke: A Guideline for Healthcare Professionals From the American Heart Association/American Stroke Association". www.ahajournals.org. doi:10.1161/str.0000000000000211. Retrieved 2021-05-13.
  7. "Metalyse 10,000 units - Summary of Product Characteristics (SmPC) - (emc)". www.medicines.org.uk. Retrieved 19 September 2021.

External links

Identifiers: