105857-23-6

Basic information

• Product Name: Alteplase
• Synonyms: Alteplase;Activase (tn);Alteplase (genetical recombination);Alteplase (genetical recombination) (jan);Alteplase (usp/inn);D02837;PlasMinogen activator (huMan tissue-type protein Moiety) (9CI)
• CAS NO: 105857-23-6
• Molecular Weight: 0
• Mol File: 105857-23-6.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Alteplase(CAS DataBase Reference)
• NIST Chemistry Reference: Alteplase(105857-23-6)
• EPA Substance Registry System: Alteplase(105857-23-6)

Safety Data

• Hazardous Substances Data: 105857-23-6(Hazardous Substances Data)

Usage

Description

Alteplase, also known as Activase, is a recombinant single-chain tissue plasminogen activator (t-PA) produced by recombinant DNA (rDNA) technology. It is a glycoprotein protease consisting of 527 amino acid residues, derived from a melanoma cell line. Alteplase is used for the intravenous management of acute myocardial infarction and is the only agent on the U.S. market indicated for the reduction of the incidence of congestive heart failure following a heart attack.

Uses

Used in Pharmaceutical Industry:
Alteplase is used as a tissue-type plasminogen activator for the management of thrombosis in acute myocardial infarct. It preferentially activates plasminogen bound to fibrin, confining its fibrinolytic action to thrombi with minimal systemic activation of plasminogen. This targeted action helps in the treatment of acute myocardial infarction.
Used in Medical Treatment:
Alteplase is used as a fibrinolytic agent for the intravenous management of acute myocardial infarction. It is indicated for the reduction of the incidence of congestive heart failure following a heart attack, providing a crucial treatment option for patients experiencing heart attacks.
Brand Names:
Activase (Genentech), Actilyse.

Application in Ischemic Stroke

In the therapy of Ischemic Stroke, Alteplase is initiated within 3 hours of symptom onset has been shown to reduce the ultimate disability due to ischemic stroke. A head CT scan must be obtained to rule out hemorrhage before beginning therapy. It is administrated 0.9 mg/kg IV (maximum 90 mg) over 1 hour in selected patients within 3 hours of onset.

Originator

Genentech (USA)

Mechanism of action

As a main endogenic promoter of fibrinolysis, t-PA binds with fibrin and, like urokinase, breaks Arg-560–Val-561 peptide bond in the fibrin-binded plasminogen molecule, thus turning it into an active plasmin molecule that breaks apart fibrin clots. Its action is localized in thrombotic regions, and thus the likelihood of systemic fibrinolysis originating during its use is much lower than that which can originate while using streptokinase and urokinase.

Clinical Use

Alteplase (tPA) is a serine protease with a low affinity for free plasminogen but a very high affinity for the plasminogen bound to fibrin in a thrombus (fibrin-specific agent). Both streptokinase and urokinase lack this specificity (i.e., are nonspecific) and act on free plasminogen, inducing a generalized thrombolytic state. Alteplase also has a greater specificity for older clots compared with newer clots relative to streptokinase and urokinase. Alteplase was originally isolated from cultures of human melanoma cells but is now produced commercially using recombinant DNA technology.

Side effects

Alteplase is unmodified human tPA, whereas reteplase is human tPA that has had several specific amino acid sequences removed. At low doses, alteplase is quite selective for degrading fibrin without concomitant lysis of other proteins, such as fibrinogen. At the higher doses currently used therapeutically, however, alteplase activates free plasminogen to some extent and, therefore, can cause hemorrhage. Many of the therapeutic indications for the other thrombolytic agents also are indications for alteplase (i.e., myocardial infarction, massive pulmonary embolism, and acute ischemic stroke).