133652-38-7

Basic information

• Product Name: Reteplase
• Synonyms: Reteplase;Retavase
• CAS NO: 133652-38-7
• Molecular Weight: 0
• Mol File: 133652-38-7.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Reteplase(CAS DataBase Reference)
• NIST Chemistry Reference: Reteplase(133652-38-7)
• EPA Substance Registry System: Reteplase(133652-38-7)

Safety Data

• Hazardous Substances Data: 133652-38-7(Hazardous Substances Data)

Usage

Description

Reteplase, also known as Retavase, is a deletion mutant variant of tissue plasminogen activator (tPA) produced in recombinant E. coli. It is a third-generation thrombolytic agent with a mechanism of action similar to alteplase. Reteplase acts directly by catalyzing the cleavage of plasminogen and initiating thrombolysis, exhibiting high thrombolytic potency. The protein consists of the kringle-2 domain and protease domain of tPA but lacks the kringle-1 domain and the growth factor domain. The expression in E. coli results in a non-glycosylated protein, and the deletion of several domains allows for a longer half-life and slower clearance. Despite the deletions and refolding, the catalytic center remains intact, and the kringle-2 domain enables binding to lysine in fibrin, making it effective for rapid and complete lysis of coronary thrombi.

Uses

Used in Myocardial Infarction Therapy:
Reteplase is used as a plasminogen activator for the treatment of acute myocardial infarction. It is effective in the rapid and complete lysis of coronary thrombi, which is crucial for restoring blood flow to the affected area and minimizing damage to the heart muscle.
Used in Pharmaceutical Industry:
Reteplase is used as a third-generation thrombolytic agent for the development of new therapies and treatments for various conditions that involve blood clotting, such as stroke, deep vein thrombosis, and pulmonary embolism. Its high thrombolytic potency and fibrin selectivity make it a valuable asset in the pharmaceutical industry for the development of targeted and effective treatments.

Originator

Boehringer Mannheim (Germany)

Mechanism of action

Reteplase is a recombinant deletion mutant of tPA lacking the finger, epidermal growth factor, kringle 1 domain, and carbohydrate side chain. As a highly fibrin-specific thrombolytic agent, reteplase is missing the first 172 amino acids that are present in alteplase and has 355 amino acids with a molecular weight of 39 kDa. Because of the removal of the finger kringle 1 domain, reteplase binding to fibrin is reduced from that of alteplase, and reteplase has reduced fibrin selectivity. In addition, the structural modification reduces hepatic elimination, leading to a longer half-life (reteplase, 14–18 minutes; alteplase, 3–4 minutes).

Clinical Use

Administered as a double bolus of 10 U every 30 minutes, reteplase is approved for use in acute myocardial infarction.

Drug interactions

Potentially hazardous interactions with other drugs Antiplatelets, heparin, vitamin K antagonists: increased risk of bleeding.

Metabolism

Cleared primarily by liver and kidneys.