Alteplase
/api/v1/drug/alteplaseMechanism of action
Sourced from openFDAMechanism-of-action classes: Plasminogen Activators; Tissue Plasminogen Activators.
Indications
Sourced from openFDA- Cathflo ® Activase ® (Alteplase) is indicated for the restoration of function to central venous access devices as assessed by the ability to withdraw blood.
Contraindications
Sourced from openFDA- Cathflo Activase should not be administered to patients with known hypersensitivity to Alteplase or any component of the formulation (see DESCRIPTION ).contraindicated
Dosage & administration
Sourced from openFDACathflo ® Activase ® (Alteplase) is for instillation into the dysfunctional catheter at a concentration of 1 mg/mL. • Patients weighing ≥30 kg: 2 mg in 2 mL • Patients weighing <30 kg: 110% of the internal lumen volume of the catheter, not to exceed 2 mg in 2 mL If catheter function is not restored at 120 minutes after 1 dose of Cathflo Activase, a second dose may be instilled (see Instructions for Administration ). There is no efficacy or safety information on dosing in excess of 2 mg per dose for this indication. Studies have not been performed with administration of total doses greater than 4 mg (two 2‑mg doses). Instructions for Administration Preparation of Solution Reconstitute Cathflo Activase to a final concentration of 1 mg/mL: Aseptically withdraw 2.2 mL of Sterile Water for Injection, USP (diluent is not provided). Do not use Bacteriostatic Water for Injection. Inject the 2.2 mL of Sterile Water for Injection, USP, into the Cathflo Activase vial, directing the diluent stream into the powder. Slight foaming is not unusual; let the vial stand undisturbed to allow large bubbles to dissipate. Mix by gently swirling until the contents are completely dissolved. Complete dissolution should occur within 3 minutes. DO NOT SHAKE. The reconstituted preparation results in a colorless to pale yellow transparent solution containing 1 mg/mL Cathflo Activase at a pH of approximately 7.3. Cathflo Activase contains no antibacterial preservatives and should be reconstituted immediately before use.
Warnings & precautions
Sourced from openFDANone.
Adverse reactions
Sourced from openFDAThe following adverse reactions are discussed in greater detail in Section PRECAUTIONS of the label: Bleeding Hypersensitivity In the clinical trials, the most serious adverse events reported after treatment were sepsis (see PRECAUTIONS, Infections ), gastrointestinal bleeding, and venous thrombosis. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Trials 1 and 2 The data described for Trials 1 and 2 reflect exposure to Cathflo Activase in 1122 patients, of whom 880 received a single dose and 242 received two sequential doses of Cathflo Activase. In the Cathflo Activase Trials 1 and 2, only limited, focused types of serious adverse events were recorded, including death, major hemorrhage, intracranial hemorrhage, pulmonary or arterial emboli, and other serious adverse events not thought to be attributed to underlying disease or concurrent illness. Major hemorrhage was defined as severe blood loss ( > 5 mL/kg), blood loss requiring transfusion, or blood loss causing hypotension. Non‑serious adverse events and serious events thought to be due to underlying disease or concurrent illness were not recorded. Patients were observed for serious adverse events until catheter function was deemed to be restored or for a maximum of 4 or 6 hours depending on study. For most patients the observation period was 30 minutes to 2 hours.
Use in specific populations
Sourced from openFDAPregnancy Alteplase has been shown to have an embryocidal effect due to an increased postimplantation loss rate in rabbits when administered intravenously during organogenesis at a dose (3 mg/kg) approximately 50 times human exposure (based on AUC) at the dose for restoration of function to occluded CVADs. No maternal or fetal toxicity was evident at a dose (1 mg/kg) approximately 16 times human exposure at the dose for restoration of function to occluded CVADs. There are no adequate and well‑controlled studies in pregnant women. Cathflo Activase should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Approval history
Sourced from openFDA- Nov 13, 1987BLABLA103172Genentech
FDA shortages
Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.
- Activase, Injection, 1 KIT in 1 CARTON (50242-085-27) * 100 mL in 1 VIAL, SINGLE-USE * 100 mL in 1 VIAL, SINGLE USE (NDC 50242-085-27)To be discontinuedSponsor: Genentech, IncUpdated
FAERS reports
- 1No Adverse Event2,48917%
- 2Off Label Use1,84613%
- 3Death1,1858.0%
- 4Gingival Bleeding1,0206.9%
- 5Cerebral Haemorrhage8035.4%
- 6Haemorrhage Intracranial7264.9%
- 7Drug Ineffective6264.2%
- 8Angioedema6204.2%
- 9Haemorrhage5703.9%
- 10Haemorrhagic Transformation Stroke4302.9%
- 11Product Storage Error3812.6%
- 12Nausea3632.5%
- 13Hypotension3432.3%
- 14Dyspnoea3392.3%
- 15Vomiting3352.3%
Literature
Recent PubMed references pinned to Alteplase as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.
- Epithelial SERPINB2 Overexpression Contributes to Impaired Fibrinolysis in Chronic Rhinosinusitis With Nasal Polyps via tPA Downregulation.Frontiers in bioscience (Landmark edition) · 2026 · Zhu Y, Zhou J, Zhang S, et al.PMID 42216541DOI 10.31083/FBL50406
- Exosomes Released by Cerebrolysin-Treated Cerebral Endothelial Cells Reverse Fibrin- or tPA-Impaired Endothelial Cell Permeability.Cells · 2026 · Teng H, Li C, Wang M, et al.PMID 42193943DOI 10.3390/cells15100934
- 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
- Neutrophil Extracellular Traps Are Associated With Early Neurological Deterioration in Patients With Acute Ischemic Stroke Receiving Intravenous Thrombolysis: A Prospective Cohort Study.Journal of the American Heart Association · 2026 · Pei L, Zhang W, Zhang D, et al.PMID 42179266DOI 10.1161/JAHA.125.045163
- Systemic-to-local nanorobot thrombolysis.Science advances · 2026 · Zhang D, Zhu O, Mou F, et al.PMID 42160438DOI 10.1126/sciadv.aed9464
- Comparative performance of stress hyperglycemia ratio, glycemic gap, and hemoglobin glycation index for predicting functional outcomes after intravenous thrombolysis in acute ischemic stroke.Clinical neurology and neurosurgery · 2026 · Shen H, Wang H, Cao Z, et al.PMID 42150220DOI 10.1016/j.clineuro.2026.109481
- Effect of ambient temperature changes on the treatment and prognosis in patients with acute stroke receiving intravenous thrombolysis.International journal of biometeorology · 2026 · Zhang T, Xue J, Chen X, et al.PMID 42149238DOI 10.1007/s00484-026-03232-2
Clinical trials
The 10 most recently updated of 507 ClinicalTrials.gov registrations naming Alteplase as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.
- Alteplase Through an Indwelling Pleural Catheter for the Management of Symptomatic Septated Malignant Pleural EffusionRecruiting · Early phase 1 · Interventional · 30 enrolled · M.D. Anderson Cancer CenterNCT06184321updated 2026-06-12
- CleaRRAflow: Isotonic Solution vs. TPA for IVH ClearanceNot yet recruiting · Phase 4 · Interventional · 80 enrolled · David DornbosNCT07643493updated 2026-06-11
- Endovascular Thrombectomy Alone Versus Intravenous Thrombolysis Plus Thrombectomy on Acute Basilar Artery OcclusionRecruiting · Phase 3 · Interventional · 338 enrolled · The First Affiliated Hospital of University of Science and Technology of ChinaNCT05827042updated 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 WellRecruiting · Phase 3 · Interventional · 1,325 enrolled · Boehringer IngelheimNCT07361302updated 2026-06-09
- Lacunar Stroke hyperAcute Clinical Utilization of Novel Approach Regimens: Rt-PA vs. DAPT Randomised Clinical TrialRecruiting · Phase 4 · Interventional · 500 enrolled · Nippon Medical SchoolNCT07111559updated 2026-06-05
- Tissue-Type Plasminogen Activator (t-PA) Release Predicts Major Adverse Cardiac Events (MACE) in Patients With Non-critical Coronary Artery DiseaseTerminated · Phase 1 · Interventional · 16 enrolled · Vanderbilt UniversityNCT00868855updated 2026-06-01
- rhTNK-tPA for Acute Ischemic Stroke Under Simplified Imaging in the Extended Time WindowNot yet recruiting · Phase 3 · Interventional · 750 enrolled · Sun Yat-Sen Memorial Hospital of Sun Yat-Sen UniversityNCT07606807updated 2026-05-26
- Targeting TFPI With Concizumab to Improve Haemostasis in Glanzmann Thrombasthenia Patients: an in Vitro StudyCompleted · Interventional · 20 enrolled · University Hospital, BordeauxNCT06234813updated 2026-05-26
- Intracoronary rhTNK-tPA Versus Tirofiban in Patients With STEMI and High Thrombus BurdenRecruiting · Phase 4 · Interventional · 300 enrolled · Henan Institute of Cardiovascular EpidemiologyNCT06769256updated 2026-05-22
- STRATEGY-PE: Real-World Treatment Strategies for Intermediate-High Risk Pulmonary EmbolismNot yet recruiting · Observational · 1,300 enrolled · Nanjing First Hospital, Nanjing Medical UniversityNCT07603700updated 2026-05-22
Frequently asked questions
- How does Alteplase work?
- Mechanism-of-action classes: Plasminogen Activators; Tissue Plasminogen Activators.
- What is Alteplase used for?
- According to FDA labeling, Alteplase carries indications including: Cathflo ® Activase ® (Alteplase) is indicated for the restoration of function to central venous access devices as assessed by the ability to withdraw blood.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
- What class of drug is Alteplase?
- Alteplase is classified as Enzymes, Other ophthalmologicals, Plasminogen Activators, Tissue Plasminogen Activators, Increased Thrombolysis.
- What are the brand names for Alteplase?
- Alteplase is marketed under brand names including Activase.
- What are the contraindications for Alteplase?
- Alteplase labeling lists contraindications including: Cathflo Activase should not be administered to patients with known hypersensitivity to Alteplase or any component of the formulation (see DESCRIPTION ).. Always consult the full prescribing information and a clinician.
alteplase is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.