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Cyklokapron (Tranexamic Acid)
Tranexamic acid occupies lysine receptor binding sites on plasmin, preventing fibrin dissolution.
Tranexamic acid is an antifibrinolytic agent indicated for short-term use (2-8 days) in hemophilia patients undergoing tooth extraction to reduce hemorrhage and replacement therapy needs. The drug works by occupying plasmin's lysine binding sites on fibrin, preventing fibrin dissolution and stabilizing clot structure. Key risks include contraindication in subarachnoid hemorrhage due to cerebral complications and increased thromboembolic risk with concomitant prothrombotic agents. Dose adjustment is required in renal impairment as the drug is primarily eliminated unchanged in urine.
At a glance
| Generic name | Tranexamic Acid |
|---|---|
| Sponsor | Pfizer Inc. |
| Drug class | Antifibrinolytic agent |
| Target | Plasminogen lysine binding sites; fibrin |
| Modality | Small molecule |
| Therapeutic area | Rare Disease |
| Phase | FDA-approved |
Mechanism of action
Tranexamic acid is a synthetic lysine amino acid derivative that diminishes the dissolution of hemostatic fibrin by plasmin. The drug works by occupying the lysine receptor binding sites of plasmin for fibrin, preventing plasmin from binding to fibrin monomers and thus preserving and stabilizing fibrin's matrix structure. The antifibrinolytic effects are mediated through reversible interactions at multiple binding sites within plasminogen. Native human plasminogen contains 4 to 5 lysine binding sites with low affinity for tranexamic acid (Kd = 750 μmol/L) and 1 with high affinity (Kd = 1.1 μmol/L). The high affinity lysine site is involved in plasminogen's binding to fibrin. Saturation of the high affinity binding site with tranexamic acid displaces plasminogen from the fibrin surface. Although plasmin may still be formed through conformational changes in plasminogen, binding to and dissolution of the fibrin matrix is inhibited.
Approved indications
- Reduce or prevent hemorrhage in hemophilia patients during tooth extraction
- Reduce or prevent hemorrhage in hemophilia patients following tooth extraction
- Reduce need for replacement therapy in hemophilia patients during tooth extraction
- Reduce need for replacement therapy in hemophilia patients following tooth extraction
Common side effects
- Nausea
- Vomiting
- Dizziness
- Urticaria or dermatitis
Drug interactions
- Prothrombotic medical products
Key clinical trials
- Comparative Evaluation of Topical Metformin and Topical Tranexamic Acid in Melasma (NA)
- Tranexamic Acid for The Treatment of Gastrointestinal Bleeding (NA)
- Hemoglobin Drop and Need for Blood Transfusion in Primary Knee Arthroplasty With or Without Drain Insertion (NA)
- Extended Oral Tranexamic Acid After Primary Total Knee Arthroplasty (NA)
- Prevention of Postpartum Hemorrhage With Tranexamic Acid (PHASE2)
- Effects of Red and Infrared Photobiomodulation in Rhinoplasty at a Single Centre (NA)
- Bleeding Reduction in Acute and Chronic Kidney Patients Having Surgery (BRACKETS) Pilot Trial (PHASE3)
- The Effects of Intraoperative Tranexamic Acid on Perioperative Bleeding In Craniotomies (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Cyklokapron CI brief — competitive landscape report
- Cyklokapron updates RSS · CI watch RSS
- Pfizer Inc. portfolio CI