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Reteplase: A Market-tested Thrombolytic Agent for Your Portfolio

Views: 32     Author: Unibest Digital     Publish Time: 2024-12-17      Origin: Unibest Digital

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Introduction to Thrombolytic Drugs

Thrombolytic drugs play a crucial role in treating various venous and arterial thromboembolic conditions, particularly acute myocardial infarction. These agents, primarily plasmin activators, convert plasminogen to plasmin, which dissolves insoluble fibrin clots through its fibrinolytic action.


Thrombolytic agents are classified based on their fibrin specificity:
  1. - Non-fibrin-specific agents: streptokinase and urokinase

  2. - Fibrin-specific agents: tissue plasminogen activator (tPA)

  3. - Next-generation agents: reteplase, tenecteplase, monteplase, lanoteplase, pamiteplase, desmoteplase (Bat-PA), and chimeric thrombolytics


Reteplase: A Game-Changer in Thrombolytic Therapy

Approved in Europe and the United States in 1996, Reteplase represents a significant advancement in thrombolytic therapy.

Structure and Composition

Reteplase is a genetically engineered, purified form of human tissue plasminogen activator. Known as a "third-generation" thrombolytic agent, it is specifically designed to retain and delete certain portions of human tPA for enhanced efficacy:
  • - Molecular weight: 39 kDa

  • - Composition: 355 amino acids (starting with serine, ending with proline)

  • - Structure: Single-chain deletion mutant of tPA with nine disulfide bonds

  • - Retained domains: Kringle-2 and serine protease (activity-related)

  • - Deleted domains: Kringle-1, finger, and epidermal growth factor (EGF)

Tissue plasminogen activator and reteplase schematic figure

Tissue plasminogen activator and reteplase schematic figure. src: Mohammadi, E., Seyedhosseini-Ghaheh, H., Mahnam, K., Jahanian-Najafabadi, A. & Mir Mohammad Sadeghi, H. Reteplase: Structure, Function, and Production. Adv Biomed Res 8, 19 (2019).


Mechanism of Action

Reteplase's thrombolytic action involves:
  1. - Binding to fibrin-rich clots via the Kringle-2 domain

  2. - Cleaving the Arg/Val bond in plasminogen to form plasmin (via the protease domain)

  3. - Degrading the fibrin matrix of the thrombus through plasmin action

mechanism of Thrombolytic action of plasminogen activators

Thrombolytic action of plasminogen activators. src: Mohammadi, E., Seyedhosseini-Ghaheh, H., Mahnam, K., Jahanian-Najafabadi, A. & Mir Mohammad Sadeghi, H. Reteplase: Structure, Function, and Production. Adv Biomed Res 8, 19 (2019).


Key advantages over tPA include:

  • - Extended plasma half-life

  • - Reduced fibrin specificity

  • - Enhanced ability to penetrate blood clots


Clinical Applications and Benefits

Reteplase is primarily used for:
  • - Acute myocardial infarction

  • - Cerebral infarction

  • - Pulmonary embolism

  • - Deep vein thrombosis

Key benefits include:
  • - Significant reduction in post-infarction transient ischemia burden

  • - Lower early and late mortality rates

  • - Improved patient recovery


Our Offering: A Market-tested Thrombolytic Solution

We are proud to represent and offer Reteplase as a small-volume lyophilized powder injection. Launched in 2007, it was the first & only third-generation thrombolytic drug available in China. Safety, efficacy, and cost can be greatly guaranteed.

reteplase product