Tenecteplase

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.

• TNKase ® is indicated to reduce the risk of death associated with acute ST elevation myocardial infarction (STEMI). TNKase is a tissue plasminogen activator, indicated to reduce the risk of death associated with acute ST elevation myocardial infarction (STEMI).ICD-10: I21.9

• TNKase is contraindicated in patients with [see Warnings and Precautions (5.1) ] : Active internal bleeding History of cerebrovascular accident Intracranial or intraspinal surgery or trauma within 2 months Intracranial neoplasm, arteriovenous malformation, or aneurysm Known bleeding diathesis Severe uncontrolled hypertension Active internal bleeding ( 4 ) History of cerebrovascular accident ( 4 ) Intracranial or intraspinal surgery or trauma within 2 months ( 4 ) Intracranial neoplasm, arteriovenous malformation, or aneurysm ( 4 ) Known bleeding diathesis ( 4 ) Severe uncontrolled hypertension ( 4 )contraindicated

Initiate treatment as soon as possible after the onset of STEMI symptoms. ( 2.1 ) TNKase is for intravenous administration only, administered as a single bolus over 5 seconds. Individualize dosage based on patient's weight. ( 2.1 ) 2.1 Recommended Dosage Initiate treatment as soon as possible after the onset of STEMI symptoms. TNKase is for intravenous (IV) administration only, administered as a single bolus over 5 seconds. Individualize dosage based on the patient's weight (see Table 1 ). Table 1: Recommended Dosage Patient Weight (kg) TNKase (mg) Volume TNKase From one vial of TNKase reconstituted with 10 mL Sterile Water for Injection. to be administered (mL) < 60 30 6 ≥ 60 to < 70 35 7 ≥ 70 to < 80 40 8 ≥ 80 to < 90 45 9 ≥ 90 50 10 2.2 Preparation Follow the below steps to prepare TNKase for administration: Remove the shield assembly from the supplied B-D ® 10 mL syringe with TwinPak™ Dual Cannula Device (see Figure 1 ) and aseptically withdraw 10 mL of Sterile Water for Injection, USP, from the supplied diluent vial using the red hub cannula syringe filling device. Only use the supplied Sterile Water for Injection, USP for reconstitution. Note: Do not discard the shield assembly. Aseptically reconstitute the vial with 10 mL Sterile Water for Injection, USP by directing the stream into the lyophilized powder to obtain a final concentration of 5 mg/mL. Slight foaming upon reconstitution is not unusual; any large bubbles will dissipate if the product is allowed to stand undisturbed for several minutes. Gently swirl until contents are completely dissolved. DO NOT SHAKE.

Bleeding: Increases the risk of bleeding. Avoid intramuscular injections. Monitor for bleeding. ( 5.1 ) Thromboembolism: The use of thrombolytics can increase the risk of thrombo-embolic events in patients with high likelihood of left heart thrombus. ( 5.2 ) Cholesterol Embolization: Has been reported in patients treated with thrombolytic agents. ( 5.3 ) Arrhythmias: It is recommended that anti-arrhythmic therapy for bradycardia and/or ventricular irritability be available when TNKase is administered. ( 5.4 ) Increased Risk of Heart Failure and Recurrent Ischemia when used with Planned Percutaneous Coronary Intervention (PCI) in STEMI: In patients with a large ST segment elevation myocardial infarction, physicians should choose either thrombolysis or PCI as the primary treatment strategy for reperfusion. Rescue PCI or subsequent elective PCI may be performed after administration of thrombolytic therapies if medically appropriate. ( 5.5 ) Hypersensitivity: Monitor patients treated with TNKase during and for several hours after infusion. If symptoms of hypersensitivity occur, initiate appropriate therapy (e.g., antihistamines, corticosteroids). ( 5.6 ) 5.1 Bleeding TNKase can cause bleeding, including intracranial hemorrhage and fatal bleeding. Concomitant use of other drugs that impair hemostasis increases the risk of bleeding. Should serious bleeding that is not controlled by local pressure occur, discontinue any concomitant heparin or antiplatelet agents immediately and treat appropriately.

The following adverse reactions are discussed in other sections of the label: Bleeding [see Contraindications (4) , Warnings and Precautions (5.1) ] Hypersensitivity [see Warnings and Precautions (5.6) ] The most common adverse reactions are bleeding and hypersensitivity. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Roche at 1-800-526-6367 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Immunogenicity Four of 625 (0.64%) patients tested for antibody formation to TNKase had a positive antibody titer at 30 days in studies with TNKase. The observed incidence of antibody positivity in an assay may be influenced by several factors including sample handling, concomitant medications, and underlying disease. For these reasons, comparison of the incidence of antibodies to TNKase with the incidence of antibodies to other products may be misleading.

8.1 Pregnancy Risk Summary There are risks to the mother and fetus from acute ST elevation myocardial infarction, which is a medical emergency in pregnancy and can be fatal if left untreated (see Clinical Considerations ). Published data consisting of a small number of case reports involving the use of related thrombolytic agents in pregnant women have not identified an increased risk of major birth defects. There are no data on the use of tenecteplase during pregnancy to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. TNKase does not elicit maternal and direct embryo toxicity in rabbits following a single IV administration. In developmental toxicity studies conducted in rabbits, the no observable effect level (NOEL) of a single IV administration of TNKase on maternal or developmental toxicity (5 mg/kg) was approximately 7 times human exposure (based on AUC) at the dose for STEMI. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Metabolism

Distribution In patients with STEMI, TNKase administered as a single IV bolus exhibits a biphasic disposition from the plasma. Volume of distribution at central compartment ranges from 4.22 to 5.43 L, approximating plasma volume.

• Jun 2, 2000BLABLA103909Genentech

1. 1Off Label Use41127%
2. 2No Adverse Event30620%
3. 3Cerebral Haemorrhage15310%
4. 4Angioedema1167.7%
5. 5Haemorrhage Intracranial1147.5%
6. 6Death785.2%
7. 7Haemorrhage775.1%
8. 8Drug Ineffective674.4%
9. 9Cerebrovascular Accident593.9%
10. 10Haemorrhagic Transformation Stroke553.6%
11. 11Subarachnoid Haemorrhage432.8%
12. 12Medication Error402.6%
13. 13Hypotension372.4%
14. 14Cardiogenic Shock342.3%
15. 15Cardiac Arrest332.2%

Recent PubMed references pinned to Tenecteplase as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Safety and efficacy of intravenous tenecteplase in patients with acute ischemic stroke in the extended time window: an updated meta-analysis.
  European journal of clinical pharmacology · 2026 · Rejili M, Khan Y, Rawat A, et al.
  PMID 42189257DOI 10.1007/s00228-026-04082-y
• Association of 24-Hour Computed Tomography Infarct Density on Functional Outcomes in Stroke: Secondary Analysis From the AcT Trial.
  Journal of the American Heart Association · 2026 · Pensato U, Zhang J, Barakhanov K, et al.
  PMID 42179273DOI 10.1161/JAHA.125.046038
• Intravenous Tenecteplase Prior to Endovascular Treatment for Ischemic Stroke at 4.5 to 24 Hours: The TNK-PLUS Randomized Clinical Trial.
  JAMA · 2026 · Xiong Y, Che F, Wang H, et al.
  PMID 42099212DOI 10.1001/jama.2026.4292
• Tenecteplase 4.5 to 24 h after non-LVO stroke with potentially salvageable brain tissue improved functional outcomes at 90 d.
  Annals of internal medicine · 2026 · Lo B, ACP Journal Club Editorial Team at McMaster University
  PMID 42081812DOI 10.7326/ANNALS-26-01142-JC
• Efficacy and Safety of Intravenous Thrombolysis with Tenecteplase in Patients with Wake-Up Branch Atheromatous Disease.
  Translational stroke research · 2026 · Zhu L, Zhang Y, Li J, et al.
  PMID 42062620DOI 10.1007/s12975-026-01443-8
• Clinical benefit of tenecteplase despite failed recanalization in late-window ischemic stroke: a post hoc analysis of the TRACE-3 trial.
  BMC medicine · 2026 · Lu Z, Wang Z, Jin A, et al.
  PMID 41992212DOI 10.1186/s12916-026-04877-x
• ''Sugar for the Heart'', a bitter pill for tenecteplase: the crystallisation trap of pre-hospital fibrinolysis.
  Scandinavian journal of trauma, resuscitation and emergency medicine · 2026 · Prevautel T, Adet A, Michoud G, et al.
  PMID 41987235DOI 10.1186/s13049-026-01594-5
• Outcomes After Minor Ischemic Stroke in Older Patients Treated With IV Thrombolysis vs Standard of Care in the TEMPO-2 Trial.
  Neurology · 2026 · Ganesh A, Vatanpour S, Yu AYX, et al.
  PMID 41980227DOI 10.1212/WNL.0000000000214925

The 10 most recently updated of 161 ClinicalTrials.gov registrations naming Tenecteplase as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Reperfusion Approach in Predicted In-hospital Delay for Primary PCI in STEMI
  Not yet recruiting · Phase 4 · Interventional · 240 enrolled · National Medical Research Center for Cardiology, Ministry of Health of Russian Federation
  NCT07641231updated 2026-06-11
• Robot-Assisted Hematoma Evacuation With Intrahematoma Tenecteplase for Post-Reperfusion PH2 Hemorrhagic Transformation
  Not yet recruiting · Phase 1 · Interventional · 20 enrolled · Beijing Tiantan Hospital
  NCT07641998updated 2026-06-11
• Endovascular Thrombectomy Alone Versus Intravenous Thrombolysis Plus Thrombectomy on Acute Basilar Artery Occlusion
  Recruiting · Phase 3 · Interventional · 338 enrolled · The First Affiliated Hospital of University of Science and Technology of China
  NCT05827042updated 2026-06-09
• A Study to Test if Tenecteplase Helps People to Recover From an Acute Stroke When Given More Than 4.5 Hours After the Person Was Last Seen Well
  Recruiting · Phase 3 · Interventional · 1,325 enrolled · Boehringer Ingelheim
  NCT07361302updated 2026-06-09
• Efficacy and Safety of Tenecteplase Intravenous Thrombolysis in Acute Posterior Circulation Ischemic Stroke Within 4.5-24 Hours After Onset
  Recruiting · Interventional · 406 enrolled · The First Affiliated Hospital of University of Science and Technology of China
  NCT07094763updated 2026-06-08
• Intra-Arterial Tenecteplase Following Endovascular Thrombectomy for Large Vessel Occlusion Stroke
  Enrolling by invitation · Phase 2 · Interventional · 40 enrolled · Wake Forest University Health Sciences
  NCT06781385updated 2026-06-02
• Efficacy and Safety of Tenecteplase Among acutE Ischemic Stroke Patients With Recent Ingestion of Direct Oral Anticoagulant
  Not yet recruiting · Phase 3 · Interventional · 660 enrolled · Hackensack Meridian Health
  NCT07621796updated 2026-06-02
• rhTNK-tPA for Acute Ischemic Stroke Under Simplified Imaging in the Extended Time Window
  Not yet recruiting · Phase 3 · Interventional · 750 enrolled · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University
  NCT07606807updated 2026-05-26
• Intravenous Thrombolysis With Tenecteplase Plus Thrombectomy Versus Thrombectomy Alone In Patients With A Large Ischemic Stroke: A Multicenter Randomized Controlled Trial (IVT-ALL-IN)
  Not yet recruiting · Phase 3 · Interventional · 486 enrolled · Assistance Publique - Hôpitaux de Paris
  NCT07603440updated 2026-05-22
• STRATEGY-PE: Real-World Treatment Strategies for Intermediate-High Risk Pulmonary Embolism
  Not yet recruiting · Observational · 1,300 enrolled · Nanjing First Hospital, Nanjing Medical University
  NCT07603700updated 2026-05-22

Frequently asked questions

How does Tenecteplase work?

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.

What is Tenecteplase used for?

According to FDA labeling, Tenecteplase carries indications including: TNKase ® is indicated to reduce the risk of death associated with acute ST elevation myocardial infarction (STEMI). TNKase is a tissue plasminogen activator, indicated to reduce the risk of death associated with acute ST elevation myocardial infarction (STEMI).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tenecteplase?

Tenecteplase is classified as Enzymes, Tissue Plasminogen Activators, Increased Thrombolysis.

What are the brand names for Tenecteplase?

Tenecteplase is marketed under brand names including Tnkase.

What are the contraindications for Tenecteplase?

Tenecteplase labeling lists contraindications including: TNKase is contraindicated in patients with [see Warnings and Precautions (5.1) ] : Active internal bleeding History of cerebrovascular accident Intracranial or intraspinal surgery or trauma within 2 months Intracranial neoplasm, arteriovenous malformation, or aneurysm Known bleeding diathesis Severe uncontrolled hypertension Active internal bleeding ( 4 ) History of cerebrovascular accident ( 4 ) Intracranial or intraspinal surgery or trauma within 2 months ( 4 ) Intracranial neoplasm, arteriovenous malformation, or aneurysm ( 4 ) Known bleeding diathesis ( 4 ) Severe uncontrolled hypertension ( 4 ). Always consult the full prescribing information and a clinician.