Details of the Drug

General Information of Drug (ID: DMFI8A7)

• Drug Name: Tranexamic Acid
• Synonyms: AMCA; AMCHA; AMH; Amikapron; Amstat; Anvitoff; Carxamin; Cyclocapron; Cyklokapron; Emorhalt; Exacyl; Frenolyse; Hexapromin; Hexatron; Mastop; Rikavarin; Spiramin; Tamcha; Tranex; Tranexamsaeure; Tranexan; Transamin; Transamlon; Trasamlon; Ugurol; Acide tranexamique; Acido tranexamico; Acidum tranexamicum; Tranexmic acid; Tranhexamic acid; Trans AMCHA; CL 65336; DV 79; DV79; KABI 2161; LT00159441; ALBB-006013; Acide tranexamique [INN-French]; Acido tranexamico [INN-Spanish]; Acidum tranexamicum [INN-Latin]; CL-65336; Cis-AMCHA; Cyklokapron (TN); DV-79; RP 18,429; Rikavarin (TN); Rikavarin-S; T-AMCHA; Tranexamic acid cis-form; Trans-Amcha; Trans-Tranexamic acid; Cis-4-(Aminomethyl)cyclohexanecarboxylic acid; Tranexamic acid (JP15/USAN/INN); Tranexamic acid [USAN:INN:BAN:JAN]; Trans-4-(Aminomethyl)cyclohexanecarboxylic acid; Trans-4-(Aminomethyl)cyclohexanecarboxylic acid ester; Trans-p-(Aminomethyl)cyclohexanecarboxylic; Trans-p-(Aminomethyl)cyclohexanecarboxylic acid; Cis-4-Aminomethylcyclohexane-1-carboxylic acid; Trans-1-Aminomethylcyclohexane-4-carboxylic acid; Trans-4-(Aminomethyl)cyclohexane-carboxylic acid; Trans-4-Aminomethylcyclohexane-1-carboxylic acid; Trans-1-(Aminomethyl)cyclohexane-4-carboxylic acid; Trans-4-(Aminomethyl)-1-cyclohexanecarboxylic acid; Trans-4-(Aminomethyl)cyclohexane-1-carboxylic acid; 4-(Aminomethyl)-Cyclohexanecarboxylic Acid; 4-(Aminomethyl)cyclohexanecarboxylic acid; 4-(aminomethyl)cyclohexane-1-carboxylic acid

Indication

Disease Entry	ICD 11	Status	REF
Excessive bleeding	GA30.02	Approved	[1]
Menorrhagia	GA20.50	Approved	[2]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Phase 2	[3]
Endometriosis	GA10	Investigative	[2]

• Therapeutic Class: Antifibrinolytic Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 157.21
  Logarithm of the Partition Coefficient (xlogp); -2
  Rotatable Bond Count (rotbonds); 2
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 3
• ADMET Property:
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
  Clearance: The drug present in the plasma can be removed from the body at the rate of 2.4 mL/min/kg [5]
  Half-life: The concentration or amount of drug in body reduced by one-half in 2.3 hours [5]
  Unbound Fraction: The unbound fraction of drug in plasma is 0.97% [5]
  Vd: Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 0.38 L/kg [5]
• Chemical Identifiers:
  Formula: C8H15NO2
  IUPAC Name: 4-(aminomethyl)cyclohexane-1-carboxylic acid
  Canonical SMILES: C1CC(CCC1CN)C(=O)O
  InChI: InChI=1S/C8H15NO2/c9-5-6-1-3-7(4-2-6)8(10)11/h6-7H,1-5,9H2,(H,10,11)
  InChIKey: GYDJEQRTZSCIOI-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 5526
  ChEBI ID: CHEBI:48669
  CAS Number: 701-54-2
  DrugBank ID: DB00302
  TTD ID: D05HXX
  ACDINA ID: D00696
• Repurposed Drugs (RPD): Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Plasminogen (PLG)	TTP86E2	PLMN_HUMAN	Inhibitor	[6]

Molecular Expression Atlas of This Drug

• The Studied Disease: Excessive bleeding
• ICD Disease Classification: GA30.02

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Plasminogen (PLG)	DTT	PLG	8.61E-01	-0.01	-0.09

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Tranexamic Acid (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Carfilzomib	DM48K0X	Major	Additive thrombogenic effects by the combination of Tranexamic acid and Carfilzomib.	Multiple myeloma [2A83]	[7]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Stearic acid	E00079	5281	Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Beta-D-lactose	E00099	6134	Diluent; Dry powder inhaler carrier; Lyophilization aid
Carmellose sodium	E00625	Not Available	Disintegrant
Crospovidone	E00626	Not Available	Disintegrant
Glyceryl dibehenate	E00537	22477175	Binding agent; Coating agent; Flavoring agent; Modified-release agent; Viscosity-controlling agent; lubricant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Triethyl citrate	E00128	6506	Plasticizing agent; Solvent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Tranexamic acid 650 mg tablet	650 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6573).
• [2] Tranexamic acid FDA Label
• [3] Tranexamic Acid (TXA) and Corona Virus 2019 (COVID19) in Inpatients (TCInpatient)
• [4] BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
• [5] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [6] Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8.
• [7] Cerner Multum, Inc. "Australian Product Information.".