Last reviewed 2026-05-28 · How we verify

Cyklokapron (Tranexamic Acid)

Cyklokapron (generic name: Tranexamic Acid) is a Antifibrinolytic agent Small molecule drug developed by Pfizer Inc.. It is currently FDA-approved for 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.

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

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

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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

Frequently asked questions about Cyklokapron

Related

• Drug class: All Antifibrinolytic agent drugs
• Target: All drugs targeting Plasminogen lysine binding sites; fibrin
• Manufacturer: Pfizer Inc. — full pipeline
• Therapeutic area: All drugs in Rare Disease
• Indication: Drugs for Reduce or prevent hemorrhage in hemophilia patients during tooth extraction
• Indication: Drugs for Reduce or prevent hemorrhage in hemophilia patients following tooth extraction
• Indication: Drugs for Reduce need for replacement therapy in hemophilia patients during tooth extraction

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing