Tenecteplase

What it is and how it works

Mechanism of Action Tenecteplase is a modified form of human tissue plasminogen activator (tPA) that binds to fibrin and converts plasminogen to plasmin. In the presence of fibrin, in vitro studies demonstrate that tenecteplase-mediated conversion of plasminogen to plasmin is increased relative to its conversion in the absence of fibrin. This fibrin specificity decreases systemic activation of plasminogen and the resulting degradation of circulating fibrinogen as compared to a molecule lacking this property. The clinical significance of fibrin-specificity on safety (e.g., bleeding) or efficacy has not been established.

Indications

TNKase is a tissue plasminogen activator (tPA) indicated: for the treatment of acute ischemic stroke (AIS) in adults. to reduce the risk of death associated with acute ST elevation myocardial infarction (STEMI) in adults. Acute Ischemic Stroke TNKase is indicated for the treatment of acute ischemic stroke (AIS) in adults. Acute ST Elevation Myocardial Infarction TNKase is indicated to reduce the risk of death associated with acute ST elevation myocardial infarction (STEMI) in adults.

Dosage and administration (summary)

TNKase is for intravenous administration only, administered as a single bolus over 5 seconds. ( 2.1 , 2.2 ) AIS Initiate treatment as soon as possible and within 3 hours after the onset of stroke symptoms. Individualize dosage based on patient's weight; the maximum recommended dose is 25 mg (5 mL). Acute STEMI Initiate treatment as soon as possible after the onset of STEMI symptoms. Individualize dosage based on patient's weight; the maximum recommended dose is 50 mg (10 mL). Recommended Dosage for Acute Ischemic Stroke Initiate treatment as soon as possible and within 3 hours after the onset of stroke symptoms.

Contraindications

and STEMI Active internal bleeding Intracranial or intraspinal surgery or trauma within 2 months Known bleeding diathesis Current severe uncontrolled hypertension Presence of intracranial conditions that may increase the risk of bleeding (e.g., intracranial neoplasm, arteriovenous malformation, or aneurysm) AIS Active intracranial hemorrhage Acute STEMI History of intracranial hemorrhage History of ischemic stroke within 3 months AIS and Acute STEMI TNKase is contraindicated in any patients with…

Warnings and precautions

Bleeding: Increases the risk of bleeding. Avoid intramuscular injections. Monitor for bleeding. Hypersensitivity: Monitor patients treated with TNKase during and for several hours after administration. If symptoms of hypersensitivity occur, initiate appropriate therapy (e.g., antihistamines, corticosteroids, epinephrine). Thromboembolism: The use of thrombolytics can increase the risk of thrombo-embolic events in patients with high likelihood of left heart thrombus. Cholesterol Embolization: Has been reported in patients treated with thrombolytic agents.

Pregnancy

Pregnancy Risk Summary There are risks to the mother and fetus from acute ST elevation myocardial infarction and acute ischemic stroke, which are medical emergencies in pregnancy and can be fatal if left untreated (see Clinical Considerations ).

Storage and supply

Storage and Handling Store lyophilized TNKase at room temperature up to 30°C (86°F) or refrigerated at 2°C to 8°C (36°F to 46°F). Do not use beyond the expiration date stamped on the vial. For storage information for reconstituted TNKase, see Dosage and Administration .

Source: Tenecteplase (Tnkase) — US FDA prescribing information, 2025-12-15, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.