Product Details:

CasNo： 191588-94-0

Molecular Formula： C₂₅₆₁H₃₉₁₉N₇₄₇O₇₈₁S₄₀

Appearance： Commonly white to off-white powder

Throughput： 10KG/Month

Purity： 99%

Tenecteplase (CAS No: 191588-94-0) - Detailed Introduction

The Chinese generic name of Tenecteplase is Tinaiplase, with a CAS number of 191588-94-0. It is a genetically engineered thrombolytic drug widely used in the treatment of acute thrombotic diseases due to its high fibrin specificity and prolonged action. Below is a detailed overview:

1. Basic Physicochemical & Manufacturing Information

2. Core Pharmacological Properties

Mechanism of Action

As a plasminogen activator, it specifically binds to fibrin in thrombi, converting thrombus-bound plasminogen into plasmin. This subsequently degrades the fibrin matrix, achieving thrombolysis and restoring blood flow. Compared with natural tissue-type plasminogen activator, it exhibits stronger resistance to plasminogen activator inhibitor-1 (PAI-1) and a longer duration of action.

Pharmacokinetics

• Distribution: Approximates plasma volume
• Metabolism: Primarily metabolized in the liver
• Half-life: Approximately 20-24 minutes; single intravenous injection suffices for therapeutic effect without the need for continuous infusion, ensuring convenient administration.

3. Clinical Applications

Core Indications

• Treatment of acute ST-segment elevation myocardial infarction (STEMI), reducing mortality risk in patients
• Thrombolytic therapy for acute ischemic stroke (administered within 3 hours of symptom onset)
• Management of pulmonary embolism and other thrombus-related diseases

Administration & Dosage

• Route: Intravenous injection only
• Dosage: Adult dosage adjusted by body weight; conventional single-dose administration. Reconstituted drug concentration is 5mg/mL. Avoid shaking during reconstitution to prevent efficacy impairment.Example: For acute myocardial infarction patients, a single dose of 30-50mg may be administered within 6 hours of symptom onset, based on body weight.

4. Safety & Contraindications

Adverse Reactions

• Most common risk: Bleeding (severe events such as intracranial hemorrhage and cerebral hemorrhage are rare but life-threatening)
• Other reactions: Allergic responses (rash, pruritus, laryngeal edema) and arrhythmias.

Contraindications

Contraindicated in patients with:

• History of central nervous system (CNS) damage (e.g., intracranial tumors, aneurysms)
• Recent intracranial/spinal surgery or head trauma
• Active bleeding or bleeding diathesis
• Uncontrolled severe hypertension

5. Market & Approval Status

• Approved by the U.S. FDA in June 2000 and the European EMA in February 2001. Early commercialization was driven by companies such as Genentech and Boehringer Ingelheim.
• Classified as a high-alert medication, requiring strict compliance with pharmaceutical quality standards for production and sales. Clinical use must be performed and monitored by professional healthcare personnel.