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Reteplase, trade names include Retavase, is a
thrombolytic drug Thrombolysis, also called fibrinolytic therapy, is the breakdown ( lysis) of blood clots formed in blood vessels, using medication. It is used in ST elevation myocardial infarction, stroke, and in cases of severe venous thromboembolism (massiv ...
, used to treat
heart attacks A myocardial infarction (MI), commonly known as a heart attack, occurs when blood flow decreases or stops to the coronary artery of the heart, causing damage to the heart muscle. The most common symptom is chest pain or discomfort which may tra ...
by breaking up the clots that cause them. Reteplase is a recombinant non-glycosylated form of human tissue plasminogen activator, which has been modified to contain 357 of the 527
amino acid Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although hundreds of amino acids exist in nature, by far the most important are the alpha-amino acids, which comprise proteins. Only 22 alpha am ...
s of the original
protein Proteins are large biomolecules and macromolecules that comprise one or more long chains of amino acid residues. Proteins perform a vast array of functions within organisms, including catalysing metabolic reactions, DNA replication, respo ...
. It is produced in the
bacterium Bacteria (; singular: bacterium) are ubiquitous, mostly free-living organisms often consisting of one biological cell. They constitute a large domain of prokaryotic microorganisms. Typically a few micrometres in length, bacteria were among ...
Escherichia coli ''Escherichia coli'' (),Wells, J. C. (2000) Longman Pronunciation Dictionary. Harlow ngland Pearson Education Ltd. also known as ''E. coli'' (), is a Gram-negative, facultative anaerobic, rod-shaped, coliform bacterium of the genus ''Escher ...
. Reteplase was approved for use in 1996. Reteplase is similar to recombinant human tissue plasminogen activator ( alteplase), but the modifications give reteplase a longer
half-life Half-life (symbol ) is the time required for a quantity (of substance) to reduce to half of its initial value. The term is commonly used in nuclear physics to describe how quickly unstable atoms undergo radioactive decay or how long stable ato ...
of 13–16 minutes. Reteplase also binds
fibrin Fibrin (also called Factor Ia) is a fibrous, non-globular protein involved in the clotting of blood. It is formed by the action of the protease thrombin on fibrinogen, which causes it to polymerize. The polymerized fibrin, together with platele ...
with lower affinity than alteplase, improving its ability to penetrate into clots. As reteplase is able to penetrate inside the thrombi, an enhanced fibrinolytic activity will be achieved → rapid reperfusion → low incidence of bleeding.


References

Antithrombotic enzymes {{blood-drug-stub