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Tranexamic Acid

drug
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Also known as Acide tranexamiqueAcido tranexamicoAmchaCL 65336CL-65336CL65336Cyclo-fCyclocapronCyclokapronCyklo-f heavy period reliefCyklokapronEspercilExacylFemstrualHaematrixLB-1148LB1148LystedaMenstraliteNSC-291305

Summary

Tranexamic Acid (CHEMBL877) is an approved small-molecule antifibrinolytic drug (ATC B02AA02) targeting PLG; indicated across 64 conditions including hemophilia a and hip fracture.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: B02AA02
  • Targets: 1 (PLG)
  • Indications: 64 conditions
  • Clinical trials: 484
  • Chemistry: 157.21 Da · C8H15NO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL877
NameTranexamic Acid
TypeSmall molecule
Max phase4
FDA approvedno
PubChem CID5526
ChEBICHEBI:48669
ATCB02AA02
Molecular formulaC8H15NO2
Molecular weight157.21
InChIKeyGYDJEQRTZSCIOI-UHFFFAOYSA-N

SMILES: C1CC(CCC1CN)C(=O)O

IUPAC name: 4-(aminomethyl)cyclohexane-1-carboxylic acid

Pharmacological roles (ChEBI): antifibrinolytic drug, hematologic agent.

Also known as: Acide tranexamique, Acido tranexamico, Amcha, CL 65336, CL-65336, CL65336, Cyclo-f, Cyclocapron, Cyclokapron, Cyklo-f heavy period relief, Cyklokapron, Espercil

Patent coverage: 10,353 distinct patent families (27,519 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
PLGplasminogenBinding3.64.6%P00747

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Plasminogen, Tissue-type plasminogen activator.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 12 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
PLG5.96Kd1100nMCHEMBL_ACT_14739703
PLG5.96Kd1100nMCHEMBL_ACT_19054663
PLG5.66Kd2200nMCHEMBL_ACT_14739704
PLG5.51IC503100nMCHEMBL_ACT_12652159
PLG5.51IC503100nMCHEMBL_ACT_14739721
PLAT5.47IC503390nMCHEMBL_ACT_29168039

Target pathways

Aggregated over 1 target gene(s): PLG.

Top Reactome pathways

6 total, by targets touching each:

PathwayTargetsGenes
Platelet degranulation1PLG
Degradation of the extracellular matrix1PLG
Activation of Matrix Metalloproteinases1PLG
Signaling by PDGF1PLG
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)1PLG
Dissolution of Fibrin Clot1PLG

Dominant GO biological processes

GO termTargets
proteolysis1
blood coagulation1
negative regulation of cell population proliferation1
negative regulation of cell-substrate adhesion1
protein processing1
extracellular matrix disassembly1
tissue regeneration1
fibrinolysis1
positive regulation of blood vessel endothelial cell migration1
myoblast differentiation1
muscle cell cellular homeostasis1
tissue remodeling1
biological process involved in interaction with symbiont1
negative regulation of fibrinolysis1
positive regulation of fibrinolysis1

Indications & clinical

Indications

64 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
hemophilia A4MONDO:0010602MONDO:0010602
hip fracture3MONDO:0005327EFO:0003964
scoliosis3MONDO:0005392EFO:0004273
injury3MONDO:0021178EFO:0000546
uterine corpus leiomyoma3MONDO:0007886EFO:0000731
thrombocytopenia3MONDO:0002049HP:0001873
abdominal aortic aneurysm3MONDO:0005350EFO:0004214
lymphoid neoplasm3MONDO:0005157EFO:0001642
bone fracture3MONDO:0005315EFO:0003931
upper aerodigestive tract neoplasm3MONDO:0005398EFO:0004284
pelvic organ prolapse3MONDO:0000082EFO:0004710
placenta accreta3MONDO:0005916EFO:0007440
placenta praevia3MONDO:0005918EFO:0007442
arthropathy3MONDO:0006816EFO:1000999
femoral neck fracture3MONDO:0043589EFO:1001792
anemia3MONDO:0002280EFO:0004272
blood coagulation disease3MONDO:0001531EFO:0009314
nasal cavity polyp3MONDO:0006314EFO:1000391
astrocytoma (excluding glioblastoma)3MONDO:0019781EFO:0000272
brain injury3MONDO:0043510MONDO:0043510
hematopoietic and lymphoid system neoplasm3MONDO:0002334MONDO:0044881
coronary artery disorder3MONDO:0005010EFO:0001645
severe acute respiratory syndrome3MONDO:0005091MONDO:0100096
brain neoplasm3MONDO:0021211EFO:0003833
bone cancer3MONDO:0002129EFO:1000350
shoulder impingement syndrome3MONDO:0006968EFO:1001178
ileus3MONDO:0004567MONDO:0004567
female reproductive system neoplasm3MONDO:0021148MONDO:0021148
osteoarthritis3MONDO:0005178MONDO:0005178
meningioma3MONDO:0016642MONDO:0016642
hereditary hemorrhagic telangiectasia3MONDO:0019180MONDO:0019180
hereditary angioedema3MONDO:0019623MONDO:0019623
melanoma3MONDO:0005105EFO:0000756
burn3MONDO:0043519EFO:0009516
neoplasm3MONDO:0005070MONDO:0004992
paraganglioma3MONDO:0000448EFO:1000453
von Willebrand disease (hereditary or acquired)3MONDO:0024574Orphanet:903
subarachnoid hemorrhage2MONDO:0005099EFO:0000713
intracerebral hemorrhage2MONDO:0013792EFO:0005669
toxic shock syndrome2MONDO:0001881EFO:0006834
osteoarthritis, knee2MONDO:0005416EFO:0004616
intervertebral disk degenerative disorder2MONDO:0011385HP:0008419
spinal cord neoplasm1MONDO:0021234EFO:0003828
hypotensive disorder0MONDO:0005468EFO:0005251
skin neoplasm0MONDO:0002531EFO:0004198
cirrhosis of liver0MONDO:0005155EFO:0001422

18 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 484.

Phase distribution

PhaseTrials
PHASE4152
Not specified119
PHASE3105
PHASE255
PHASE2/PHASE319
PHASE1/PHASE213
EARLY_PHASE111
PHASE110

Top trials by phase / activity

NCTPhaseStatusTitle
NCT04312880PHASE4ENROLLING_BY_INVITATIONTranexamic Acid Infusion During Elective Spine Surgery
NCT05345613PHASE4RECRUITINGTranexamic Acid During Colonic Endoscopic Resection Procedures
NCT06025916PHASE4RECRUITINGPostpartum Hemorrhage Reduction With Oral Tranexamic Acid: a Clinical Trial
NCT06109155PHASE4RECRUITINGThe Effect of ACT and Tranexamic Acid on Bleeding in Cardiac Surgery
NCT06270407PHASE4RECRUITINGThe Effect of Local Application of Tranexamic Acid Versus Placebo on Postoperative Complications in Plastic Surgery
NCT06379724PHASE4RECRUITINGBurn Study- Tranexamic Acid Versus Thrombin in Split Thickness Skin Graft
NCT06384456PHASE4RECRUITINGTopical TRanexamic Acid vs. Placebo on Acute Postoperative Pain Following DRF Fixation
NCT06428682PHASE4RECRUITINGRole of TXA in Patients Undergoing Breast Free Flap Reconstruction
NCT06452342PHASE4NOT_YET_RECRUITINGTRanEXamic Acid to Decrease Heavy Menstrual Bleeding in Individuals Anticoagulated for Venous Thromboembolism Pilot Study
NCT06754371PHASE4RECRUITINGProphylactic Tranexamic Acid Reduces Postpartum Hemorrhage
NCT06777966PHASE4RECRUITINGNebulized Versus Intravenous Tranexamic Acid on Surgical Field Quality in Patients Undergoing Endoscopic Sinus Surgeries
NCT06820177PHASE4RECRUITINGTranexamic Acid for Second Trimester Dilation and Evacuation and Bleeding Outcomes
NCT06832878PHASE4NOT_YET_RECRUITINGPostoperative Oral Tranexamic Acid in Patients Undergoing Primary Total Joint Arthroplasty
NCT06881628PHASE4RECRUITINGTranxemic Acid and Vitamin K Injection to Control Upper Gastrointestinal Bleeding in Cirrhotic Patients
NCT07078942PHASE4NOT_YET_RECRUITINGProphylactic Intravenous Tranexamic Acid on Perioperative Blood Loss in Pregnant Women Undergoing Cesarean Section
NCT07089251PHASE4RECRUITINGThe Perioperative Outcome of Epinephrine Infusion and Tranexamic Acid in Knee Arthroplasty Surgery
NCT07098780PHASE4RECRUITINGRole of Tranexamic Acid in Reducing Hemorrhagic Events in Bariatric Surgery
NCT07460518PHASE4NOT_YET_RECRUITINGTranexamic Acid for Bleeding Reduction During TURP Surgery
NCT07501884PHASE4NOT_YET_RECRUITINGREDUCER Trial (TXA in Urethroplasty)
NCT07614087PHASE4NOT_YET_RECRUITINGPlasma Concentrations of Intraosseous Versus Intravenous Tranexamic Acid in Joint Arthroplasty
NCT00670345PHASE4COMPLETEDTranexamic Acid in Urologic Surgery
NCT00722436PHASE4TERMINATEDTranexamic Acid for Craniofacial Surgery
NCT00740116PHASE4COMPLETEDTranexamic Acid in Surgery of Advanced Ovarian Cancer
NCT00809393PHASE4COMPLETEDDose-ranging Study of Two Doses of Tranexamic Acid During Cardiac Surgery
NCT00827931PHASE4COMPLETEDStudy Of Tranexamic Acid For The Reduction Of Blood Loss In Patients Undergoing Major Abdominal Surgery
NCT00904709PHASE4COMPLETEDThe Assessment of Tranexamic Acid in Women With Menorrhagia Who Have Bleeding Disorders
NCT00958581PHASE4COMPLETEDTranexamic Acid (TXA) Versus Epsilon Aminocaproic Acid (EACA) Versus Placebo for Spine Surgery
NCT00985920PHASE4COMPLETEDTopical Tranexamic Acid for Total Knee Arthroplasty
NCT01067638PHASE4COMPLETEDThe Effect of Tranexamic Acid on Postoperative Blood Loss and Coagulation in Patients With Preoperative Anemia Undergoing Off-Pump Coronary Artery Bypass Graft; Double Blind Randomized Control Study
NCT01136590PHASE4COMPLETEDMulticenter, Randomized Placebo-controlled Clinical Trial to Evaluate the Effect of Perioperative Use of Tranexamic Acid on Transfusion Requirements and Surgical Bleeding in Major Spine Surgery
NCT01190150PHASE4COMPLETEDLysteda Pediatric Research Equity Act (PREA) Pharmacokinetic Study in Adolescent Females With Heavy Menstrual Bleeding
NCT01228136PHASE4COMPLETEDTranexamic Acid and Pediatric Adenotonsillectomy
NCT01295294PHASE4COMPLETEDManagement of Initial Bleeding/Spotting Associated With the Levonorgestrel-releasing Intrauterine System (MIRENA)
NCT01599468PHASE4COMPLETEDCan Tranexamic Acid Reduce Bleeding After Post Partum Hemorrhage in Cesarean Section Delivery
NCT01622946PHASE4COMPLETEDThe Effect of Topical Application of Tranexamic Acid in Total Hip Arthroplasty Through the Direct Anterior Approach
NCT01643135PHASE4COMPLETEDReduction Bleeding in Laminectomy With Double Doses of Tranexamic Acid
NCT01714336PHASE4COMPLETEDDoes Tranexamic Acid Reduce the Need for Blood Transfusions in Patients Undergoing Hip Fracture Surgery?
NCT01846507PHASE4COMPLETEDTranexamic Acid in Adolescents With Heavy Menstrual Bleeding
NCT01940419PHASE4COMPLETEDTesting of the Drug Tranexamic Acids as Prophylaxis of Bleeding in Benign Surgical Removal of the Uterus
NCT01940523PHASE4COMPLETEDRandomized Controlled Trial of Tranexamic Acid in Total Knee Arthroplasty: Intravenous vs. Topical

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

10 molecules share ≥1 primary target. Top 10 by shared-target count:

MoleculeSourceStatusShared targets
AMINOCAPROIC ACIDChEMBLPhase 4 (approved)PLG
BEROTRALSTATChEMBLPhase 4 (approved)PLG
MELAGATRANChEMBLPhase 4 (approved)PLG
PENTAMIDINEChEMBLPhase 4 (approved)PLG
TELAPREVIRChEMBLPhase 4 (approved)PLG
DABIGATRANChEMBLPhase 3PLG
GABEXATEChEMBLPhase 3PLG
MILVEXIANChEMBLPhase 3PLG
NAFAMOSTATChEMBLPhase 3PLG
EFEGATRANChEMBLPhase 2PLG

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot