Overview
Tenecteplase is a tissue plasminogen activator (tPA) developed from modifications of natural human tPA complementary DNA (cDNA). It is a 527 amino acid with a substitution of threonine 103 with asparagine and substitution of asparagine 117 with glutamine within the kringle 1 domain, and a tetra-alanine substitution at amino acids 296-299 in the protease domain.
Indication
用于溶栓治疗。
Associated Conditions
- Cardiovascular Mortality
Research Report
Tenecteplase: A Comprehensive Pharmacological and Clinical Review
1. Introduction to Tenecteplase
Tenecteplase is a third-generation thrombolytic agent, representing a significant advancement in the pharmacotherapy of acute thrombotic events. It is a genetically engineered variant of human tissue plasminogen activator (tPA), a naturally occurring serine protease integral to the endogenous fibrinolytic system.[1] The primary clinical utility of Tenecteplase lies in the emergency management of conditions where rapid dissolution of blood clots is critical, most notably in acute ST-segment elevation myocardial infarction (STEMI) and, following more recent investigations and regulatory approvals, in acute ischemic stroke (AIS).[1]
The development of Tenecteplase was driven by the objective to improve upon the characteristics of earlier generation tPAs, particularly alteplase. This was achieved through targeted modifications to the tPA protein structure, resulting in an agent with enhanced fibrin specificity, a greater resistance to inactivation by its principal physiological inhibitor, plasminogen activator inhibitor-1 (PAI-1), and a considerably longer plasma half-life.[2] These refined pharmacological properties confer a major practical advantage: the ability to administer Tenecteplase as a single, weight-adjusted intravenous (IV) bolus. This simplified administration contrasts with the more complex bolus and infusion regimens required for older agents like alteplase.[2]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/07/30 | Not Applicable | Not yet recruiting | |||
2025/07/18 | Not Applicable | Not yet recruiting | Second Affiliated Hospital, School of Medicine, Zhejiang University | ||
2025/07/02 | Not Applicable | Recruiting | Beijing Tiantan Hospital | ||
2025/05/01 | Phase 3 | Not yet recruiting | Beijing Tiantan Hospital | ||
2025/04/29 | Phase 2 | Recruiting | ProMedica Health System | ||
2025/01/30 | Phase 1 | Not yet recruiting | |||
2024/10/26 | Phase 3 | Not yet recruiting | |||
2024/08/26 | Phase 4 | Recruiting | |||
2024/08/16 | N/A | Recruiting | |||
2024/07/12 | Phase 4 | Recruiting |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 2/23/2001 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| METALYSE FOR INJECTION 10,000 u/vial | SIN12015P | INJECTION, POWDER, FOR SOLUTION | 10000 u/vial | 7/5/2002 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| METALYSE tenecteplase (rch) 50mg powder for injection vial plus prefilled syringe | 75013 | Medicine | A | 11/9/2000 | |
| METALYSE tenecteplase (rch) 40mg powder for injection vial plus prefilled syringe | 75012 | Medicine | A | 11/9/2000 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| TNKASE | Hoffmann-La Roche Limited | 02244826 | Powder For Solution - Intravenous | 50 MG / VIAL | 10/18/2001 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| METALYSE 8.000 UNIDADES (40 MG) POLVO Y DISOLVENTE PARA SOLUCION INYECTABLE | 00169005 | POLVO Y DISOLVENTE PARA SOLUCIÓN INYECTABLE | Uso Hospitalario | Commercialized | |
| METALYSE 10.000 UNIDADES (50 MG) POLVO Y DISOLVENTE PARA SOLUCION INYECTABLE | 00169006 | POLVO Y DISOLVENTE PARA SOLUCIÓN INYECTABLE | Uso Hospitalario | Commercialized | |
| METALYSE 5.000 UNIDADES (25 MG) POLVO PARA SOLUCION INYECTABLE | 1000169007 | POLVO PARA SOLUCIÓN INYECTABLE | Uso Hospitalario | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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