Reteplase
Encyclopedia
Reteplase is a thrombolytic drug
, used to treat heart attacks
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
s of the original protein
. It is produced in the bacterium Escherichia coli
.
Reteplase is similar to recombinant human tissue plasminogen activator (alteplase), but the modifications give reteplase a longer half-life
of 13–16 minutes. Reteplase also binds fibrin
with lower affinity than alteplase, improving its ability to penetrate into clots.
Reteplase was approved by the Food and Drug Administration
in 1996.
As reteplase is able to penetrate inside the thrombi, an enhanced fibrinolytic activity will be achieved → rapid reperfusion → low incidence of bleeding.
Thrombolytic drug
Thrombolytic drugs are used in medicine to dissolve blood clots in a procedure termed thrombolysis. They limit the damage caused by the blockage of the blood vessel.-Uses:...
, used to treat heart attacks
Myocardial infarction
Myocardial infarction or acute myocardial infarction , commonly known as a heart attack, results from the interruption of blood supply to a part of the heart, causing heart cells to die...
by breaking up the clots that cause them.
Reteplase is a recombinant non-glycosylated form of human tissue plasminogen activator
Tissue plasminogen activator
Tissue plasminogen activator is a protein involved in the breakdown of blood clots. It is a serine protease found on endothelial cells, the cells that line the blood vessels. As an enzyme, it catalyzes the conversion of plasminogen to plasmin, the major enzyme responsible for clot breakdown...
, which has been modified to contain 357 of the 527 amino acid
Amino acid
Amino acids are molecules containing an amine group, a carboxylic acid group and a side-chain that varies between different amino acids. The key elements of an amino acid are carbon, hydrogen, oxygen, and nitrogen...
s of the original protein
Protein
Proteins are biochemical compounds consisting of one or more polypeptides typically folded into a globular or fibrous form, facilitating a biological function. A polypeptide is a single linear polymer chain of amino acids bonded together by peptide bonds between the carboxyl and amino groups of...
. It is produced in the bacterium Escherichia coli
Escherichia coli
Escherichia coli is a Gram-negative, rod-shaped bacterium that is commonly found in the lower intestine of warm-blooded organisms . Most E. coli strains are harmless, but some serotypes can cause serious food poisoning in humans, and are occasionally responsible for product recalls...
.
Reteplase is similar to recombinant human tissue plasminogen activator (alteplase), but the modifications give reteplase a longer half-life
Half-life
Half-life, abbreviated t½, is the period of time it takes for the amount of a substance undergoing decay to decrease by half. The name was originally used to describe a characteristic of unstable atoms , but it may apply to any quantity which follows a set-rate decay.The original term, dating to...
of 13–16 minutes. Reteplase also binds fibrin
Fibrin
Fibrin is a fibrous, non-globular protein involved in the clotting of blood. It is a fibrillar protein that is polymerised to form a "mesh" that forms a hemostatic plug or clot over a wound site....
with lower affinity than alteplase, improving its ability to penetrate into clots.
Reteplase was approved by the Food and Drug Administration
Food and Drug Administration
The Food and Drug Administration is an agency of the United States Department of Health and Human Services, one of the United States federal executive departments...
in 1996.
As reteplase is able to penetrate inside the thrombi, an enhanced fibrinolytic activity will be achieved → rapid reperfusion → low incidence of bleeding.