You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
NameTranexamic Acid
Accession NumberDB00302  (APRD01270, EXPT00508)
TypeSmall Molecule
DescriptionAntifibrinolytic hemostatic used in severe hemorrhage. [PubChem]
Acide tranexamique
Acido tranexamico
Acidum tranexamicum
Tranexmic acid
Tranhexamic acid
trans-4-(Aminomethyl)cyclohexanecarboxylic acid
trans-4-aminomethylcyclohexane-1-carboxylic acid
trans-Tranexamic acid
External IDs Not Available
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CyklokapronInjection, solution100 mg/mLIntravenousPharmacia & Upjohn Inc1986-12-30Not applicableUs
Cyklokapron 100 mg/mlSolution100 mgIntravenousPfizer1995-12-31Not applicableCanada
Cyklokapron 500 mgTablet500 mgOralPfizer1995-12-31Not applicableCanada
Erfa-tranexamicSolution100 mgIntravenousErfa Canada 2012 IncNot applicableNot applicableCanada
Gd-tranexamic AcidTablet500 mgOralGenmed A Division Of Pfizer Canada Inc2014-03-07Not applicableCanada
Gd-tranexamic AcidSolution100 mgIntravenousGenmed A Division Of Pfizer Canada IncNot applicableNot applicableCanada
LystedaTablet650 mg/1OralFerring Pharmaceuticals2010-05-17Not applicableUs
LystedaTablet650 mg/1OralFerring Pharmaceuticals2010-05-172016-10-13Us
LystedaTablet650.0 mgOralFerring PharmaceuticalsNot applicableNot applicableCanada
Tranexamic AcidTablet650 mg/1OralAmring Pharmaceuticals, Inc.2016-03-01Not applicableUs
Tranexamic AcidTablet650 mg/1OralPrasco, Laboratories2010-05-17Not applicableUs
Tranexamic AcidTablet650 mg/1OralPrasco, Laboratories2010-05-17Not applicableUs
Tranexamic Acid InjectionSolution100 mgIntravenousMethapharm, Inc.Not applicableNot applicableCanada
Tranexamic Acid InjectionSolution100 mgIntravenousOmega Laboratories Ltd2013-03-27Not applicableCanada
Tranexamic Acid Injection BPSolution100 mgIntravenousSandoz Canada Incorporated2002-10-29Not applicableCanada
Tranexamic Acid Injection BPSolution100 mgIntravenousSterimax Inc2012-11-15Not applicableCanada
Tranexamic Acid Injection BPSolution100 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
Tranexamic Acid TabletsTablet500 mgOralSterimax Inc2013-02-13Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tranexamic AcidInjection, solution100 mg/mLIntravenousX Gen Pharmaceuticals, Inc.2012-05-18Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousMylan Institutional2011-11-29Not applicableUs
Tranexamic AcidTablet, film coated650 mg/1OralActavis Pharma Company2013-01-03Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousX Gen Pharmaceuticals, Inc.2012-05-18Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousMylan Institutional2011-11-29Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousVirtus Pharmaceuticals2017-02-13Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAcella Pharmaceuticals, LLC2014-02-11Not applicableUs
Tranexamic AcidTablet, film coated650 mg/1OralAmerincan Health Packaging2015-03-31Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAuro Medics Pharma Llc2016-01-14Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousNexus Pharmaceuticals Inc2012-03-15Not applicableUs
Tranexamic AcidTablet650 1/1OralGolden State Medical Supply2014-08-20Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAmerican Regent2011-11-15Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAmneal Biosciences2017-02-28Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAkorn2015-03-09Not applicableUs
Tranexamic AcidTablet650 1/1OralApotex Corporation2014-01-27Not applicableUs
Tranexamic AcidInjection, solution1 g/10mLIntravenousHeritage2012-02-20Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAthenex Pharmaceutical Division, Llc.2017-03-27Not applicableUs
Tranexamic AcidInjection, solution1 g/10mLIntravenousHeritage2014-08-13Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousFresenius Kabi2012-04-20Not applicableUs
Tranexamic AcidInjection, solution100 mg/mLIntravenousAkorn2016-06-09Not applicableUs
Tranexamic Acid Tranexamic AcidInjection, solution100 mg/mLIntravenousGland Pharma Limited2017-02-22Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Pure Whitenol SerumCream.05 mg/50mLTopicalSkin M.D. Korea2015-02-01Not applicableUs
International Brands
Cyclo-FNot Available
EspercilNot Available
FemstrualNot Available
RikavarinNot Available
TransaminNot Available
TranscamNot Available
TraxylNot Available
Brand mixturesNot Available
CAS number1197-18-8
WeightAverage: 157.2102
Monoisotopic: 157.110278729
Chemical FormulaC8H15NO2
(1r,4r)-4-(aminomethyl)cyclohexane-1-carboxylic acid
NC[[email protected]]1CC[C@@H](CC1)C(O)=O
IndicationFor use in patients with hemophilia for short term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction. It can also be used for excessive bleeding in menstruation, surgery, or trauma cases.
Structured Indications
PharmacodynamicsTranexamic acid is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin. Tranexamic acid is a competitive inhibitor of plasminogen activation, and at much higher concentrations, a noncompetitive inhibitor of plasmin, i.e., actions similar to aminocaproic acid. Tranexamic acid is about 10 times more potent in vitro than aminocaproic acid. Tranexamic acid binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. Tranexamic acid in a concentration of 1 mg per mL does not aggregate platelets in vitro. In patients with hereditary angioedema, inhibition of the formation and activity of plasmin by tranexamic acid may prevent attacks of angioedema by decreasing plasmin-induced activation of the first complement protein (C1).
Mechanism of actionTranexamic acid competitively inhibits activation of plasminogen (via binding to the kringle domain), thereby reducing conversion of plasminogen to plasmin (fibrinolysin), an enzyme that degrades fibrin clots, fibrinogen, and other plasma proteins, including the procoagulant factors V and VIII. Tranexamic acid also directly inhibits plasmin activity, but higher doses are required than are needed to reduce plasmin formation.
TargetKindPharmacological actionActionsOrganismUniProt ID
HumanP00747 details
Related Articles
AbsorptionAbsorption of tranexamic acid after oral administration in humans represents approximately 30 to 50% of the ingested dose and bioavailability is not affected by food intake.
Volume of distribution
  • 9 to 12 L
Protein bindingThe plasma protein binding of tranexamic acid is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen (does not bind serum albumin).

Only a small fraction of the drug is metabolized (less than 5%).

Route of eliminationUrinary excretion is the main route of elimination via glomerular filtration.
Half lifeBiological half-life in the joint fluid is about 3 hours.
  • 110 – 116 mL/min
ToxicityOral LD50 in mice is >10 gm/kg. Symptoms of overdosage may be nausea, vomiting, orthostatic symptoms and/or hypotension.
Affected organisms
  • Humans and other mammals
PathwayCategorySMPDB ID
Tranexamic Acid Action PathwayDrug actionSMP00287
Pharmacogenomic Effects/ADRs Not Available
Drug Interactions
DrugInteractionDrug group
ChlorotrianiseneChlorotrianisene may increase the thrombogenic activities of Tranexamic Acid.Withdrawn
Conjugated Equine EstrogensConjugated Equine Estrogens may increase the thrombogenic activities of Tranexamic Acid.Approved
DesogestrelDesogestrel may increase the thrombogenic activities of Tranexamic Acid.Approved
DienestrolDienestrol may increase the thrombogenic activities of Tranexamic Acid.Approved
DienogestDienogest may increase the thrombogenic activities of Tranexamic Acid.Approved
DiethylstilbestrolDiethylstilbestrol may increase the thrombogenic activities of Tranexamic Acid.Approved
DrospirenoneDrospirenone may increase the thrombogenic activities of Tranexamic Acid.Approved
EstradiolEstradiol may increase the thrombogenic activities of Tranexamic Acid.Approved, Investigational, Vet Approved
EstramustineEstramustine may increase the thrombogenic activities of Tranexamic Acid.Approved
Estrogens, esterifiedEstrogens, esterified may increase the thrombogenic activities of Tranexamic Acid.Approved
Estrone sulfateEstrone sulfate may increase the thrombogenic activities of Tranexamic Acid.Approved
Ethinyl EstradiolEthinyl Estradiol may increase the thrombogenic activities of Tranexamic Acid.Approved
Ethynodiol diacetateEthynodiol diacetate may increase the thrombogenic activities of Tranexamic Acid.Approved
EtonogestrelEtonogestrel may increase the thrombogenic activities of Tranexamic Acid.Approved, Investigational
Fibrinogen Concentrate (Human)The risk or severity of adverse effects can be increased when Tranexamic Acid is combined with Fibrinogen Concentrate (Human).Approved
GestodeneGestodene may increase the thrombogenic activities of Tranexamic Acid.Approved
HexestrolHexestrol may increase the thrombogenic activities of Tranexamic Acid.Withdrawn
LevonorgestrelLevonorgestrel may increase the thrombogenic activities of Tranexamic Acid.Approved, Investigational
LynestrenolLynestrenol may increase the thrombogenic activities of Tranexamic Acid.Investigational
Medroxyprogesterone acetateMedroxyprogesterone acetate may increase the thrombogenic activities of Tranexamic Acid.Approved, Investigational
MestranolMestranol may increase the thrombogenic activities of Tranexamic Acid.Approved
MethallenestrilMethallenestril may increase the thrombogenic activities of Tranexamic Acid.Experimental
NorelgestrominNorelgestromin may increase the thrombogenic activities of Tranexamic Acid.Approved
NorgestimateNorgestimate may increase the thrombogenic activities of Tranexamic Acid.Approved
NorgestrelNorgestrel may increase the thrombogenic activities of Tranexamic Acid.Approved
Synthetic Conjugated Estrogens, ASynthetic Conjugated Estrogens, A may increase the thrombogenic activities of Tranexamic Acid.Approved
TretinoinTretinoin may increase the thrombogenic activities of Tranexamic Acid.Approved, Investigational, Nutraceutical
Food InteractionsNot Available
Synthesis Reference

Noa Zerangue, Bernd Jandeleit, Yunxiao Li, “Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use.” U.S. Patent US20070027210, issued February 01, 2007.

General ReferencesNot Available
External Links
ATC CodesB02AA02
AHFS Codes
  • 20:28.16
PDB Entries
FDA labelNot Available
MSDSDownload (63.5 KB)
Clinical Trials
Clinical Trials
0Not Yet RecruitingPreventionBlood Loss,Surgical / Hysterectomy1
0RecruitingNot AvailableKnee Prosthesis1
1CompletedTreatmentHealthy Volunteers1
1Not Yet RecruitingTreatmentHeavy Menstrual Bleeding1
1RecruitingTreatmentFibroids / Hemorrhage/Blood Loss During Myomectomies1
1Unknown StatusPreventionDegenerative Arthritis1
1Unknown StatusTreatmentAcute Blood Loss Anemia / Osteoarthritis, Hip1
1, 2CompletedPreventionAdolescent Idiopathic Scoliosis (AIS)1
1, 2CompletedPreventionHemorrhage1
1, 2CompletedPreventionPostpartum Haemorrage Sever Bleeding After Delivery1
1, 2Not Yet RecruitingPreventionPostpartum Hemorrhage1
1, 2RecruitingTreatmentMenorrhagia1
1, 2Unknown StatusPreventionHemorrhage of Cesarean Section and/or Perineal Wound1
2Active Not RecruitingPreventionPostpartum Hemorrhage1
2Active Not RecruitingPreventionSynovitis of osteoarthritis1
2Active Not RecruitingTreatmentTraumatic Brain Injury (TBI)1
2CompletedPreventionBloodloss / Surgical Procedures, Operative1
2CompletedPreventionPostpartum Hemorrhage1
2CompletedSupportive CareBleeding1
2CompletedTreatmentAcute Blood Loss Anemia / Osteoarthritis,Knee1
2CompletedTreatmentEpistaxis / Hereditary Haemorrhagic Telangiectasia (HHT)1
2Enrolling by InvitationTreatmentCurvature of Spine1
2Not Yet RecruitingTreatmentBrain Injury / Hemorrhage / Wounds and Injuries1
2Not Yet RecruitingTreatmentTotal Knee Arthroplasty (TKA)1
2RecruitingTreatmentCancers / General Surgery / Tumour1
2RecruitingTreatmentHemorrhage / Shock / Wounds and Injuries1
2RecruitingTreatmentIntracerebral Haemorrhage / Stroke1
2RecruitingTreatmentIntracerebral Hemorrhage / Stroke1
2RecruitingTreatmentIntraoperative Bleeding1
2SuspendedTreatmentNon-idiopathic Scoliosis1
2TerminatedTreatmentCritical Illness / Hypotension / Sepsis / Shock1
2TerminatedTreatmentPost Operative Blood Loss1
2TerminatedTreatmentShock, Septic1
2Unknown StatusPreventionBronchoscopy Biopsy1
2, 3CompletedTreatmentBlood Loss,Surgical / Complications; Arthroplasty / Intraoperative Complications / Shoulder Joint Disease1
2, 3CompletedTreatmentIntraoperative Bleeding / Synovitis of osteoarthritis1
2, 3Not Yet RecruitingTreatmentSpinal Deformities / Spinal Injuries1
2, 3RecruitingPreventionBladder Cancers1
2, 3RecruitingTreatmentAdult Spinal Deformity1
2, 3RecruitingTreatmentChronic Subdural Hematomas1
2, 3RecruitingTreatmentIntracerebral Hemorrhage1
2, 3RecruitingTreatmentSubarachnoid Hemorrhage1
2, 3Unknown StatusTreatmentColon Cancer / Gastric Cancers / Hepatocellular Cancer / Pancreatic Cancers1
3Active Not RecruitingPreventionBlood Loss, Postoperative / Blood Loss,Surgical / Synovitis of osteoarthritis1
3Active Not RecruitingTreatmentAcetabular Fractures1
3Active Not RecruitingTreatmentBlood Loss After a Total Hip Replacement1
3Active Not RecruitingTreatmentPost Partum Haemorrhage1
3Active Not RecruitingTreatmentPostpartum Haemorrhage1
3CompletedDiagnosticBlood Loss1
3CompletedPreventionCoronary Artery Disease1
3CompletedPreventionKnee Arthropathy1
3CompletedPreventionObstetrical Hemorrhage1
3CompletedPreventionPlacenta Previa1
3CompletedTreatmentBlood Loss2
3CompletedTreatmentBlood Loss / Hip Fractures1
3CompletedTreatmentBrain Injury1
3CompletedTreatmentCancers / General Surgery / Tumour1
3CompletedTreatmentHeavy Menstrual Bleeding / Menorrhagia3
3CompletedTreatmentHereditary Angioedema1
3CompletedTreatmentHereditary Haemorrhagic Telangiectasia (HHT) / Osler-Rendu Disease1
3CompletedTreatmentHip Fractures1
3CompletedTreatmentNeoplasms, Head and Neck1
3CompletedTreatmentSpine Surgery1
3CompletedTreatmentSurgery, Cardiac1
3Enrolling by InvitationTreatmentOther Fusion of Spine, Lumbar Region / Scoliosis1
3Not Yet RecruitingBasic ScienceBleeding / Transfusion Related Complications1
3Not Yet RecruitingPreventionPlacenta Accreta1
3Not Yet RecruitingPreventionUterine Hemorrhage1
3Not Yet RecruitingTreatmentAnemias / Hip Fracture Pathologic / Hip Fractures Pathologic1
3Not Yet RecruitingTreatmentBrain Injuries,Traumatic1
3Not Yet RecruitingTreatmentIntra-Operative Injury - Other / Post Operative Hemorrhage / Tranexamic Acid1
3Not Yet RecruitingTreatmentIntracerebral Haemorrhage / Stroke Hemorrhagic1
3Not Yet RecruitingTreatmentType 1 Von Willebrand Disease1
3RecruitingOtherNeoplasms, Hematologic1
3RecruitingPreventionAnemias / Hip Fractures1
3RecruitingPreventionAtherosclerotic Disease / Postoperative Bleeding1
3RecruitingPreventionGeneral Surgery / Peri-operative Hemorrhage or Hematoma / Retrognathism1
3RecruitingPreventionImmediate Postpartum Hemorrhage1
3RecruitingPreventionPost Operative Hemorrhage1
3RecruitingPreventionPostpartum Haemorrhage1
3RecruitingTreatmentAbdominal Aortic Aneurysms (AAA) / Blood Transfusion Requirements1
3RecruitingTreatmentAcute Coagulopathy / Wounds and Injuries1
3RecruitingTreatmentGastrointestinal Bleedings1
3RecruitingTreatmentTotal Blood Loss1
3RecruitingTreatmentTraumatic Brain Injury (TBI)1
3RecruitingTreatmentTraumatic Hemorrhage1
3SuspendedTreatmentPostpartum Hemorrhage1
3TerminatedTreatmentBlood Loss / Bone Tumour1
3Unknown StatusTreatmentAcute Upper Gastrointestinal Hemorrhage1
3Unknown StatusTreatmentAstrocytomas / Gliomas / Meningiomas / Neoplasms / Tumor, Brain1
3Unknown StatusTreatmentCraniosynostoses1
3Unknown StatusTreatmentFemoral Neck Fractures1
3Unknown StatusTreatmentHemoptisis1
3Unknown StatusTreatmentNeoplasms, Head and Neck1
4Active Not RecruitingTreatmentHeavy Menstrual Bleeding1
4Active Not RecruitingTreatmentSynovitis of osteoarthritis1
4CompletedNot AvailableMenorrhagia1
4CompletedNot AvailableRevision Total Hip Arthroplasty (RTHA)1
4CompletedOtherComplication of Extracorporeal Circulation / Pediatric Cardiac Surgery1
4CompletedPreventionAdenoidectomy / Tonsillectomy / Tranexamic Acid1
4CompletedPreventionBleeding / Prostatectomy1
4CompletedPreventionGynecologic Surgical Procedures / Hysterectomy / Tranexamic Acid1
4CompletedPreventionHemorrhage of Cesarean Section and/or Perineal Wound / Postpartum Hemorrhage1
4CompletedPreventionHemorrhage of Cesarean Section and/or Perineal Wound / Postpartum Hemorrhage / Uterine Atony1
4CompletedPreventionHip Fractures1
4CompletedPreventionIntraoperative Bleeding / Postoperative Edema1
4CompletedPreventionPostoperative Hemorrhages / Postoperative Pain1
4CompletedPreventionSurgical Blood Loss / Total Knee Arthroplasty (TKA)1
4CompletedSupportive CareLumbar Spinal Stenosis / Thoracic Spinal Stenosis1
4CompletedTreatmentAntifibrinolytic Agents / Blood Transfusions / Hemorrhage / Spinal Fusions1
4CompletedTreatmentArthropathy of Hip / Arthropathy of Knee1
4CompletedTreatmentBlood Loss3
4CompletedTreatmentBlood Loss,Surgical / Hip Replacement Surgery / Tranexamic Acid Adverse Reaction1
4CompletedTreatmentBlood Loss / Postoperative Blood Loss / Thromboembolic Complications1
4CompletedTreatmentC.Surgical Procedure; Cardiac1
4CompletedTreatmentCancer, Ovarian1
4CompletedTreatmentCardiopulmonary Bypass / Hemorrhage1
4CompletedTreatmentCleft Palates / Hemorrhage1
4CompletedTreatmentCoronary Artery Occlusive Disease1
4CompletedTreatmentHip Arthroplasty1
4CompletedTreatmentPost Partum Hemorrhage1
4CompletedTreatmentUterine Hemorrhage1
4CompletedTreatmentSynovitis of osteoarthritis1
4Enrolling by InvitationTreatmentHip Fractures1
4Not Yet RecruitingPreventionBlood Loss Anemia / Blood Loss,Surgical1
4Not Yet RecruitingPreventionBlood Loss / Hip Fractures1
4Not Yet RecruitingPreventionHematoma / Seroma1
4Not Yet RecruitingPreventionInjuries and Wounds / Postoperative Hemorrhages1
4Not Yet RecruitingPreventionOsteoarthritis,Knee1
4Not Yet RecruitingPreventionPostpartum Hemorrhage, Cesarean Section1
4Not Yet RecruitingTreatmentAnemias / Arthritis / Total Hip Arthroplasty (THA) / Total Knee Arthroplasty (TKA)1
4Not Yet RecruitingTreatmentDeep Vein Thrombosis (DVT) / Myocardial Infarction (MI) / Prophylaxis of Pulmonary embolism / Safety / Stroke1
4Not Yet RecruitingTreatmentHip Fractures1
4Not Yet RecruitingTreatmentLiver Cirrhosis / Portal Hypertension / Upper Digestive Bleeding1
4RecruitingPreventionArthroplasty, Replacement, Hip / Blood Loss,Surgical / Tranexamic Acid1
4RecruitingPreventionHip Fractures / Surgical Blood Loss1
4RecruitingPreventionNeoplasms, Breast / Postoperative Hemorrhages / Seroma1
4RecruitingSupportive CareBleeding Reduction1
4RecruitingTreatmentAntifibrinolytic Agents / Emergency Department / Gastrointestinal Hemorrhage / Tranexamic Acid1
4RecruitingTreatmentBlood Loss,Surgical1
4RecruitingTreatmentBlood Loss / Hip Arthritis / Knee Arthritis1
4RecruitingTreatmentBurns / General Surgery / Tranexamic Acid / Wounds and Injuries1
4RecruitingTreatmentCalcium Nephrolithiasis / Staghorn Calculus1
4RecruitingTreatmentCesarean Section / Placenta Accreta / Postpartum Hemorrhage / Tranexamic Acid1
4RecruitingTreatmentComplications, Pregnancy / Hemorrhage1
4RecruitingTreatmentFemoral Neck Fractures1
4RecruitingTreatmentHip Arthropathy / Shoulder Arthropathy / Synovitis of osteoarthritis1
4RecruitingTreatmentPostpartum Hemorrhage1
4RecruitingTreatmentSubdural haematoma1
4TerminatedTreatmentBleeding / Cranial Vault Surgery for Craniosynostosis / Craniosynostosis1
4Unknown StatusDiagnosticBleeding1
4Unknown StatusPreventionPostoperative Blood Loss / Total Hip Arthroplasty (THA)1
4Unknown StatusSupportive CareBleeding1
4Unknown StatusTreatmentHemorrhage1
4Unknown StatusTreatmentNative Arteriovenous Fistula1
4Unknown StatusTreatmentOsteoarthritis,Knee1
4Unknown StatusTreatmentScoliosis1
4Unknown StatusTreatmentSynovitis of osteoarthritis1
4WithdrawnPreventionProximal Femur Surgery 1
4WithdrawnTreatmentBlood Loss / Hip Fractures1
4WithdrawnTreatmentHeart Defect, Congenital / Whole Blood Platelet Aggregation Following Tranexamic Acid Administration or Placebo Administration1
Not AvailableActive Not RecruitingTreatmentSynovitis of osteoarthritis1
Not AvailableCompletedPreventionAvascular Necrosis of Femoral Head / Degenerative Arthritis of Hip1
Not AvailableCompletedPreventionBlood Loss After Primary Total Joint Arthroplasty / Need for Blood Transfusion After Total Joint Arthroplasty1
Not AvailableCompletedPreventionBlood Platelet Disorders / Disorders, Blood Coagulation / Hematologic Diseases / Menorrhagia / Von Willebrand 's disease Type 11
Not AvailableCompletedPreventionCraniosynostosis Patients Undergoing Distraction Osteotomy1
Not AvailableCompletedPreventionOsteoarthritis Of Knee1
Not AvailableCompletedSupportive CareBleeding1
Not AvailableCompletedTreatmentAcetabulum Fractures / Pelvic Ring Injury1
Not AvailableCompletedTreatmentBlood Loss / Congenital Heart Disease (CHD)1
Not AvailableCompletedTreatmentCervical Myelopathy1
Not AvailableCompletedTreatmentChronic Hyperplastic Sinusitis / Chronic Rhinosinusitis With Polyposis1
Not AvailableCompletedTreatmentCoronary Artery Bypass Graft / Coronary Artery Disease1
Not AvailableCompletedTreatmentCoronary Artery Disease1
Not AvailableCompletedTreatmentHemophilia A1
Not AvailableCompletedTreatmentHemophilia / Platelet Coagulation Disorders / VonWillebrand's Disease1
Not AvailableCompletedTreatmentHemorrhage1
Not AvailableCompletedTreatmentHemorrhage / Valvular Heart Surgery1
Not AvailableCompletedTreatmentKnee Arthroplasty, Total1
Not AvailableCompletedTreatmentMenorrhagia1
Not AvailableCompletedTreatmentNeurosurgery / Orthopedic Surgery / Red Blood Cells Transfusion1
Not AvailableCompletedTreatmentOff Pump Coronary Artery Bypass Surgery1
Not AvailableCompletedTreatmentPost CABG Bleeding1
Not AvailableCompletedTreatmentPrimary Osteoarthritis of Knee Nos1
Not AvailableCompletedTreatmentSynovitis of osteoarthritis1
Not AvailableEnrolling by InvitationPreventionBlood Loss / Fractures / General Surgery / Traumas1
Not AvailableEnrolling by InvitationTreatmentDysplasia, Congenital Hip1
Not AvailableNot Yet RecruitingPreventionAnemias / Hip Fractures1
Not AvailableRecruitingNot AvailableHip Fractures1
Not AvailableRecruitingNot AvailableThrombosis, Venous1
Not AvailableRecruitingTreatmentAcute Hip Fractures1
Not AvailableRecruitingTreatmentAnatomic Total Shoulder Arthroplasty / Blood Loss / Reverse Total Shoulder Arthroplasty / Tranexamic Acid / Transfusions1
Not AvailableRecruitingTreatmentBlood Loss2
Not AvailableRecruitingTreatmentCancers / Major Surgery / Tranexamic Acid1
Not AvailableRecruitingTreatmentEpistaxis1
Not AvailableRecruitingTreatmentHemostasis1
Not AvailableRecruitingTreatmentMajor Surgery / Minor burns / Tranexamic Acid1
Not AvailableTerminatedTreatmentAnemias / Hip Fractures1
Not AvailableUnknown StatusPreventionAcute Aortic Dissection1
Not AvailableUnknown StatusPreventionClosed Fracture of Hip1
Not AvailableUnknown StatusPreventionNasolacrimal Tract Obstruction1
Not AvailableUnknown StatusTreatmentCardiopulmonary Bypass1
Not AvailableUnknown StatusTreatmentHemostasis / Hexacapron / Mortality / Rebleeding / Upper Gastrointestinal Bleeding1
Not AvailableUnknown StatusTreatmentHip Replacement Surgery / Postoperative Hemorrhages1
Not AvailableUnknown StatusTreatmentIdiopathic Scoliosis1
Not AvailableUnknown StatusTreatmentMenstrual Cycle and Uterine Bleeding Disorders1
Not AvailableWithdrawnNot AvailableCongenital Heart Disease (CHD)1
Not AvailableWithdrawnTreatmentArthroplasty, Replacement, Hip1
Not AvailableWithdrawnTreatmentChronic Rhinosinusitis1
Not AvailableWithdrawnTreatmentGastrointestinal Hemorrhage1
  • Pharmacia and upjohn co
  • Ferring pharmaceuticals as
Dosage forms
SolutionIntravenous100 mg
TabletOral500 mg
TabletOral650 mg/1
TabletOral650.0 mg
CreamTopical.05 mg/50mL
Injection, solutionIntravenous1 g/10mL
Injection, solutionIntravenous100 mg/mL
TabletOral650 1/1
Tablet, film coatedOral650 mg/1
Unit descriptionCostUnit
Cyklokapron 100 mg/ml ampul8.8USD ml
Tranexamic acid powder1.97USD g
Cyklokapron 500 mg Tablet1.3USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7947739 No2005-03-042025-03-04Us
US8022106 No2005-03-042025-03-04Us
US8273795 No2005-03-042025-03-04Us
US8487005 No2005-03-042025-03-04Us
US8791160 No2005-03-042025-03-04Us
US8809394 No2005-03-042025-03-04Us
US8957113 No2005-03-042025-03-04Us
US9060939 No2005-03-042025-03-04Us
Experimental Properties
melting point>300 °CPhysProp
water solubility1.67E+005 mg/LMERCK INDEX (1996)
logP0.3Not Available
Predicted Properties
Water Solubility18.2 mg/mLALOGPS
pKa (Strongest Acidic)4.56ChemAxon
pKa (Strongest Basic)10.22ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area63.32 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity41.9 m3·mol-1ChemAxon
Polarizability17.28 Å3ChemAxon
Number of Rings1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Human Intestinal Absorption+0.9538
Blood Brain Barrier+0.8672
Caco-2 permeable-0.8957
P-glycoprotein substrateNon-substrate0.7572
P-glycoprotein inhibitor INon-inhibitor0.9915
P-glycoprotein inhibitor IINon-inhibitor0.8475
Renal organic cation transporterNon-inhibitor0.7446
CYP450 2C9 substrateNon-substrate0.8862
CYP450 2D6 substrateNon-substrate0.7898
CYP450 3A4 substrateNon-substrate0.829
CYP450 1A2 substrateNon-inhibitor0.9504
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9577
CYP450 2C19 inhibitorNon-inhibitor0.9452
CYP450 3A4 inhibitorNon-inhibitor0.9313
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9698
Ames testNon AMES toxic0.8916
BiodegradationReady biodegradable0.6921
Rat acute toxicity1.0517 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8797
hERG inhibition (predictor II)Non-inhibitor0.9156
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Mass Spec (NIST)Not Available
SpectraNot Available
DescriptionThis compound belongs to the class of chemical entities known as amino acids. These are organic compounds that contain at least one carboxyl group and one amino group.
KingdomChemical entities
Super ClassOrganic compounds
ClassOrganic acids and derivatives
Sub ClassCarboxylic acids and derivatives
Direct ParentAmino acids
Alternative Parents
  • Amino acid
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Organic nitrogen compound
  • Organic oxygen compound
  • Organopnictogen compound
  • Organic oxide
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aliphatic homomonocyclic compound
Molecular FrameworkAliphatic homomonocyclic compounds
External Descriptors


Pharmacological action
General Function:
Serine-type peptidase activity
Specific Function:
Plasmin dissolves the fibrin of blood clots and acts as a proteolytic factor in a variety of other processes including embryonic development, tissue remodeling, tumor invasion, and inflammation. In ovulation, weakens the walls of the Graafian follicle. It activates the urokinase-type plasminogen activator, collagenases and several complement zymogens, such as C1 and C5. Cleavage of fibronectin ...
Gene Name:
Uniprot ID:
Molecular Weight:
90568.415 Da
  1. Dunn CJ, Goa KL: Tranexamic acid: a review of its use in surgery and other indications. Drugs. 1999 Jun;57(6):1005-32. [PubMed:10400410 ]
  2. Marti DN, Schaller J, Llinas M: Solution structure and dynamics of the plasminogen kringle 2-AMCHA complex: 3(1)-helix in homologous domains. Biochemistry. 1999 Nov 30;38(48):15741-55. [PubMed:10625440 ]
  3. Jansen AJ, Andreica S, Claeys M, D'Haese J, Camu F, Jochmans K: Use of tranexamic acid for an effective blood conservation strategy after total knee arthroplasty. Br J Anaesth. 1999 Oct;83(4):596-601. [PubMed:10673876 ]
  4. Bangert K, Thorsen S: Assay of functional plasminogen in rat plasma applicable to experimental studies of thrombolysis. Thromb Haemost. 2000 Aug;84(2):299-306. [PubMed:10959704 ]
  5. Hanson AJ, Quinn MT: Effect of fibrin sealant composition on human neutrophil chemotaxis. J Biomed Mater Res. 2002 Sep 5;61(3):474-81. [PubMed:12115473 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]


Pharmacological action
General Function:
Peptide:proton symporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
Gene Name:
Uniprot ID:
Molecular Weight:
81782.77 Da
  1. Dieck ST, Heuer H, Ehrchen J, Otto C, Bauer K: The peptide transporter PepT2 is expressed in rat brain and mediates the accumulation of the fluorescent dipeptide derivative beta-Ala-Lys-Nepsilon-AMCA in astrocytes. Glia. 1999 Jan;25(1):10-20. [PubMed:9888294 ]
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on April 25, 2017 04:16