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Alteplase and tenecteplase: applications in the peripheral circulation.
C P Semba1, K Sugimoto, M K Razavi
1Cardiovascular Clinical Research, Genentech Inc., MS 59, 1 DNA Way, South San Francisco, CA 94080-4990, USA.
Summary
Alteplase (t-PA) and tenecteplase (TNK) are thrombolytic drugs used for cardiovascular conditions. Guidelines for alteplase use in noncoronary applications are available, and TNK shows a promising safety profile for peripheral vascular uses.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Alteplase (t-PA), a recombinant tissue plasminogen activator, was the first genetically engineered thrombolytic approved by the FDA in 1987 for acute myocardial infarction (AMI).
- Alteplase is approved for acute ischemic stroke and pulmonary embolism, with anticipated approval for catheter clearance.
- Following urokinase withdrawal, alteplase is an alternative for peripheral vascular applications, with practice guidelines established for its noncoronary use.
Framework:
- Emerging clinical data suggest alteplase offers similar safety and efficacy to urokinase in peripheral vascular applications, but at a lower cost.
- Tenecteplase (TNK), a modified alteplase, demonstrates an enhanced safety profile in AMI, featuring a longer half-life, increased resistance to plasminogen activator inhibitor, and improved fibrin specificity.
Implementation:
- TNK is approved for AMI as a single-bolus injection.
- Initial clinical studies are evaluating TNK for acute arterial and venous diseases.
Implications:
- TNK's enhanced safety profile suggests its potential utility in peripheral vascular applications.
- This article provides guidelines for alteplase use and highlights TNK's features for interventionalists.