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Cyklokapron (Tranexamic Acid)

Pfizer Inc. · FDA-approved approved Small molecule Quality 60/100

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 nameTranexamic Acid
SponsorPfizer Inc.
Drug classAntifibrinolytic agent
TargetPlasminogen lysine binding sites; fibrin
ModalitySmall molecule
Therapeutic areaRare Disease
PhaseFDA-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

Common side effects

Drug interactions

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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