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Alteplase

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Alteplase
Clinical data
Trade namesActivase, Actilyse
AHFS/Drugs.comMonograph
License data
ATC code
Legal status
Legal status
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC2569H3928N746O781S40
Molar mass59042.3 g/mol g·mol−1
  (verify)

Alteplase (trade names Activase, Actilyse) is a thrombolytic drug, used to treat acute myocardial infarctions (heart attacks) and other severe conditions caused by blood clotting by breaking up the blood clots that cause them.

It is a tissue plasminogen activator. It is approved by the US Food and Drug Administration for the treatment of myocardial infarction with ST-elevation (STEMI), acute ischemic stroke (AIS), acute massive pulmonary embolism, and occluded central venous access devices (CVAD).[1][2][3]

Medical uses

The primary uses of alteplase, as approved by the FDA, include acute ischemic stroke, acute myocardial infarction, and acute massive pulmonary embolism.[4]

In regards to acute myocardial infarction, a new randomized controlled trial published in January 2019 specifically looking at patients with acute STEMI, showed there was no reduction in microvascular obstruction when adjunctive low dose intracoronary alteplase was administered during the primary PCI. [5]

Mechanism of Action

Alteplase is a serine protease that assists fibrin in the conversion of plasminogen to plasmin. When in the systemic circulation, alteplase binds to fibrin in a thrombus and initiates fibrinolysis. [4]

References

  1. ^ "Thrombolytic Therapy: Background, Thrombolytic Agents, Thrombolytic Therapy for Acute Myocardial Infarction". 2017-05-02. {{cite journal}}: Cite journal requires |journal= (help)
  2. ^ Drugs.com: Monograph for Activase.
  3. ^ Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. 2017. Actilyse-Pulver und Lösungsmittel zur Herstellung einer Injektions- oder Infusionslösung. ISBN 3-85200-196-X.
  4. ^ a b Activase [package insert]. South San Francisco, CA: Genentech, Inc.; 2018.
  5. ^ McCartney, Peter (January 2019). "Effect of Low-Dose Intracoronary Alteplase During Primary Percutaneous Coronary Intervention on Microvascular Obstruction in Patients with Acute Myocardial Infarction". JAMA. 321: 56–68.