DT-Web

DB00302 - Tranexamic Acid


Identification
Name Tranexamic Acid
Accession Number DB00302 (APRD01270, EXPT00508)
Type small molecule
Description Antifibrinolytic hemostatic used in severe hemorrhage. [PubChem]
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 157.2102
Groups approved
Monoisotopic Weight 157.110278729
Pharmacology
Indication For 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.
Mechanism of action Tranexamic 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.
Absorption Absorption 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.
Protein binding The 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).
Biotransformation Only a small fraction of the drug is metabolized (less than 5%).
Route of elimination Urinary excretion is the main route of elimination via glomerular filtration.
Toxicity Oral 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
Interactions
Drug Interactions Not Available
Food Interactions Not Available

Targets


Plasminogen
Name Plasminogen
Gene Name PLG
Pharmacological action yes
Actions inhibitor
References
  • Dunn CJ, Goa KL: Tranexamic acid: a review of its use in surgery and other indications. Drugs. 1999 Jun;57(6):1005-32. - Pubmed
  • 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
  • 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
  • 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
  • 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
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.5383

Transporters


Oligopeptide transporter, kidney isoform
Name Oligopeptide transporter, kidney isoform
Gene Name SLC15A2
Actions Not Available
References
  • 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
DTHybrid score 0.3461

Predictions


Id Partner name Gene Name Score
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.2089
791 Urokinase plasminogen activator surface receptor PLAUR 0.1841
267 Plasminogen activator inhibitor 1 SERPINE1 0.169
595 Fibrinogen alpha chain FGA 0.1553
1193 Proteinase-activated receptor 1 F2R 0.0899
244 Angiotensin-converting enzyme ACE 0.0811
2876 Membrane-bound lytic murein transglycosylase B mltB 0.0726
3133 UDP-galactopyranose mutase glf 0.0725
5099 UDP-galactopyranose mutase glf 0.0725
1812 Kallikrein-1 KLK1 0.0676
2353 Apolipoprotein(a) LPA 0.0654
1792 Tissue-type plasminogen activator PLAT 0.062
633 Penicillin-binding proteins 1A/1B pbpA 0.0546
723 Cytosolic phospholipase A2 PLA2G4A 0.05
1349 Plasminogen activator inhibitor 2 SERPINB2 0.0448
118 Organic cation/carnitine transporter 2 SLC22A5 0.0438
6011 Chymotrypsinogen B CTRB1 0.0359
6020 Aldehyde oxidase AOX1 0.0358
1729 Solute carrier family 22 member 6 SLC22A6 0.0358
3834 Nidogen-1 NID1 0.027
3176 Trypsin-1 PRSS1 0.0248
3825 Tetranectin CLEC3B 0.0245
2111 Annexin A2 ANXA2 0.0245
3826 Keratin, type II cytoskeletal 8 KRT8 0.0245
3833 Plasma serine protease inhibitor SERPINA5 0.0235
3011 Suppressor of tumorigenicity protein 14 ST14 0.0225
1516 Calnexin CANX 0.0213
1 Peptidoglycan synthetase ftsI ftsI 0.0207
4155 Peptidoglycan synthetase ftsI ftsI 0.0207
1244 Low-density lipoprotein receptor-related protein 2 LRP2 0.0198
3831 Low-density lipoprotein receptor-related protein 1 LRP1 0.0197
471 Sodium- and chloride-dependent neutral and basic amino acid transporter B(0+) SLC6A14 0.0194
645 Penicillin-binding protein 1A mrcA 0.0192
5805 Penicillin-binding protein 1A ponA 0.0192
6185 Penicillin-binding protein 1A mrcA 0.0192
6799 Penicillin-binding protein 1A pbpA 0.0192
3830 Calreticulin CALR 0.0189
6142 Solute carrier family 22 member 8 SLC22A8 0.017
587 Serum albumin ALB 0.0158
543 Penicillin-binding protein 1B mrcB 0.0135
6186 Penicillin-binding protein 1B ponB 0.0135
6822 Penicillin-binding protein 1b pbp1b 0.0135
6844 Penicillin-binding protein 1b pbp1b 0.0135
1757 Myeloperoxidase MPO 0.0131
1385 Angiotensin-converting enzyme 2 ACE2 0.0128
115 Penicillin-binding protein 2 mrdA 0.0127
6069 Penicillin-binding protein 2 mrdA 0.0127
6118 Penicillin-binding protein 2 penA 0.0127
6187 Penicillin-binding protein 2 pbpA 0.0127
6686 Penicillin-binding protein 2 pbp2 0.0127
6939 Penicillin-binding protein 2 mrdA 0.0127
7163 Penicillin-binding protein 2 pbpA 0.0127
6067 Penicillin binding protein 2a mecA 0.0126
56 Delta-aminolevulinic acid dehydratase ALAD 0.0124
2356 Delta-aminolevulinic acid dehydratase hemB 0.0124
3613 Delta-aminolevulinic acid dehydratase hemB 0.0124
3674 Delta-aminolevulinic acid dehydratase hemB 0.0124
1074 Urokinase-type plasminogen activator PLAU 0.0124
1588 Multidrug resistance protein 1 ABCB1 0.011
3923 Cholinesterase BCHE 0.0109
230 ATP-binding cassette transporter sub-family C member 8 ABCC8 0.0109
1024 Solute carrier family 22 member 11 SLC22A11 0.0106
2544 Bacterial leucyl aminopeptidase Not Available 0.0106
3917 Methylenetetrahydrofolate reductase MTHFR 0.0089
6016 Cytochrome P450 2C19 CYP2C19 0.0087
4512 Cytochrome P450 3A4 CYP3A4 0.0082
3060 Leukotriene A-4 hydrolase LTA4H 0.008
4604 Liver carboxylesterase 1 CES1 0.0074
159 Penicillin-binding protein 2B penA 0.0067
6121 Penicillin-binding protein 2B penA 0.0067
4252 Penicillin-binding protein 5 dacA 0.0063
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0063
4757 Cytochrome P450 2C9 CYP2C9 0.0058
6143 Solute carrier family 22 member 7 SLC22A7 0.0058
738 Monocarboxylate transporter 1 SLC16A1 0.0056
332 Beta-lactamase blaZ 0.0055
2478 Beta-lactamase ampC 0.0055
2613 Beta-lactamase ampC 0.0055
2635 Beta-lactamase ampC 0.0055
2700 Beta-lactamase penP 0.0055
5445 Beta-lactamase blaB 0.0055
6019 Beta-lactamase SHV-7 0.0055
6701 Beta-lactamase cphA 0.0055
509 Thymidine kinase TK 0.0054
570 Thymidine kinase TK 0.0054
2559 Thymidine kinase TK 0.0054
3430 Thymidine kinase tdk 0.0054
3518 Thymidine kinase TK 0.0054
5301 Thymidine kinase tdk 0.0054
5771 Thymidine kinase ORF36 0.0054
7009 Thymidine kinase ORF36 0.0054
3760 Penicillin-binding protein 5 precursor dacA 0.005
709 ATP-sensitive inward rectifier potassium channel 1 KCNJ1 0.0048
3426 Glutamine synthetase glnA 0.0048
3987 Glutamine synthetase GLUL 0.0048
6184 D-alanyl-D-alanine carboxypeptidase dacC dacC 0.0047
338 DNA polymerase UL30 0.0047
379 DNA polymerase UL54 0.0047
697 DNA polymerase ORF28 0.0047
2482 DNA polymerase 43 0.0047
4104 DNA polymerase BALF5 0.0047
6140 Ileal sodium/bile acid cotransporter SLC10A2 0.0045
867 Penicillin-binding protein 3 pbpC 0.0045
6119 Penicillin-binding protein 3 pbp3 0.0045
7154 Penicillin-binding protein 3 pbp3 0.0045
7157 Penicillin-binding protein 3 LMHCC_2184 0.0045
7162 Penicillin-binding protein 3 pbpB 0.0045
7172 Penicillin-binding protein 3 pbp3 0.0045
20 Prostaglandin G/H synthase 1 PTGS1 0.0042
6139 Solute carrier organic anion transporter family member 1A2 SLCO1A2 0.0033
6160 Solute carrier organic anion transporter family member 3A1 SLCO3A1 0.0032
6154 Multidrug and toxin extrusion protein 1 SLC47A1 0.0032
6153 Solute carrier organic anion transporter family member 4A1 SLCO4A1 0.0032
6106 Cytochrome P450 2C18 CYP2C18 0.0026
833 Organic cation/carnitine transporter 1 SLC22A4 0.0026
4119 Cytochrome P450 2D6 CYP2D6 0.0026
2461 D-alanyl-D-alanine carboxypeptidase Not Available 0.0025
5756 D-alanyl-D-alanine carboxypeptidase dac 0.0025
3961 G protein-activated inward rectifier potassium channel 4 KCNJ5 0.0025
1490 Solute carrier organic anion transporter family member 1B1 SLCO1B1 0.0022
521 ATP-binding cassette transporter sub-family C member 9 ABCC9 0.0021
132 ATP-binding cassette sub-family A member 1 ABCA1 0.0019
2184 Cystic fibrosis transmembrane conductance regulator CFTR 0.0018
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0018
4924 Cytochrome P450 2C8 CYP2C8 0.0018
238 Peroxisome proliferator-activated receptor gamma PPARG 0.0017
2164 Multidrug resistance-associated protein 4 ABCC4 0.0016
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0016
781 ATP-sensitive inward rectifier potassium channel 11 KCNJ11 0.0016
6107 Cytochrome P450 3A7 CYP3A7 0.0013
4118 Cytochrome P450 3A5 CYP3A5 0.0012
1709 Canalicular multispecific organic anion transporter 2 ABCC3 0.0012
776 Bile salt export pump ABCB11 0.0012
862 Multidrug resistance-associated protein 1 ABCC1 0.0011
1735 Canalicular multispecific organic anion transporter 1 ABCC2 0.001
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.001
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