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aminocaproic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 163 | 60-32-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An antifibrinolytic agent that acts by inhibiting plasminogen activators which have fibrinolytic properties.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 16 | g | O |
| 16 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 333 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 65 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1524.67 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.39 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 2.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.92 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.90 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -3.679 | Moderate | 0.78 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 2.443 | Moderate | 0.78 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.578 | 10^-6 cm/s | Moderate | 0.78 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.596 | uL/min/10^6 cells | Moderate | 0.78 |
| dppb | Dog plasma protein binding (% unbound) | 91.870 | % | Moderate | 0.78 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 77.130 | % | Moderate | 0.78 |
| herg | hERG pIC50 | 4.766 | pIC50 | Moderate | 0.78 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.879 | uL/min/10^6 cells | Moderate | 0.78 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.285 | uL/min/mg protein | Moderate | 0.78 |
| hppb | Human plasma protein binding (% unbound) | 91.660 | % | Moderate | 0.78 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,ALK,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MTOR,NTRK1,NTRK2,PDK2,PDK4,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ZAP70 | 49 | |||
| kinase-selectivity-class | AXL,BRAF,CDK4,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,MAP2K6,MAP3K14,MAPK7,MAPK8,PLK1,PLK2,SIK2,STK33,SYK,TEK,TGFBR1,TTK,UHMK1 | 23 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.152 | Moderate | 0.78 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 1.683 | Moderate | 0.78 | |
| mppb | Mouse plasma protein binding (% unbound) | 96.200 | Moderate | 0.78 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.652 | Moderate | 0.78 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 94.640 | % | Moderate | 0.78 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.641 | uL/min/10^6 cells | Moderate | 0.78 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 85.990 | % | Moderate | 0.78 |
| rppb | Rat plasma protein binding (% unbound) | 97.050 | % | Moderate | 0.78 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 797.995 | uM | Moderate | 0.78 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 3, 1964 | FDA | CLOVER PHARMS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Haemorrhage | 165.61 | 28.68 | 61 | 1041 | 60502 | 42559731 |
| Haemarthrosis | 134.95 | 28.68 | 29 | 1073 | 3969 | 42616264 |
| Epistaxis | 69.51 | 28.68 | 34 | 1068 | 66792 | 42553441 |
| Mouth haemorrhage | 53.20 | 28.68 | 15 | 1087 | 6246 | 42613987 |
| Traumatic haemorrhage | 52.98 | 28.68 | 11 | 1091 | 1266 | 42618967 |
| Diabetes insipidus | 50.98 | 28.68 | 13 | 1089 | 3700 | 42616533 |
| Factor VIII inhibition | 40.17 | 28.68 | 7 | 1095 | 315 | 42619918 |
| Spontaneous haemorrhage | 30.22 | 28.68 | 6 | 1096 | 551 | 42619682 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Haemorrhage | 166.92 | 29.06 | 62 | 1611 | 106630 | 110480996 |
| Haemarthrosis | 138.40 | 29.06 | 30 | 1643 | 7299 | 110580327 |
| Epistaxis | 51.15 | 29.06 | 29 | 1644 | 130343 | 110457283 |
| Factor VIII inhibition | 50.59 | 29.06 | 8 | 1665 | 342 | 110587284 |
| Diabetes insipidus | 50.51 | 29.06 | 13 | 1660 | 6557 | 110581069 |
| Traumatic haemorrhage | 48.88 | 29.06 | 10 | 1663 | 1834 | 110585792 |
| Mouth haemorrhage | 33.10 | 29.06 | 11 | 1662 | 13477 | 110574149 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | B02AA01 | BLOOD AND BLOOD FORMING ORGANS ANTIHEMORRHAGICS ANTIFIBRINOLYTICS Amino acids |
| MeSH PA | D000933 | Antifibrinolytic Agents |
| MeSH PA | D003029 | Coagulants |
| MeSH PA | D006401 | Hematologic Agents |
| MeSH PA | D006490 | Hemostatics |
| FDA PE | N0000175632 | Decreased Fibrinolysis |
| FDA EPC | N0000175634 | Antifibrinolytic Agent |
| CHEBI has role | CHEBI:25212 | metabolite |
| CHEBI has role | CHEBI:48675 | antifibrinolytic drug |
| CHEBI has role | CHEBI:50248 | hematologic agent |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
Related Drugs by ATC class:
B02AA Amino acids 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Postsurgical Hemorrhage | indication | ||
| Hyperfibrinolysis Induced Hemorrhage | indication | ||
| Prevention of Peri-Operative Hemorrhage | off-label use | ||
| Hemorrhaging in Hemophilia | off-label use | ||
| Prevention of Hemorrhage with Cardiovascular Instability from Cardiopulmonary Bypass - CABG | off-label use | ||
| Blood in urine | contraindication | 34436003 | |
| Disseminated intravascular coagulation | contraindication | 67406007 | DOID:11247 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Thrombosis | contraindication | 439127006 | |
| Increased Creatine Phosphokinase | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.22 | acidic |
| pKa2 | 10.69 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Plasminogen | Enzyme | INHIBITOR | IC50 | 4.40 | CHEMBL | CHEMBL | |||
| Tissue-type plasminogen activator | Enzyme | INHIBITOR | DRUGBANK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017911 | VUID |
| N0000170207 | NUI |
| D00160 | KEGG_DRUG |
| 99 | RXNORM |
| C0000608 | UMLSCUI |
| CHEBI:16586 | CHEBI |
| ACA | PDB_CHEM_ID |
| CHEMBL1046 | ChEMBL_ID |
| 564 | PUBCHEM_CID |
| DB00513 | DRUGBANK_ID |
| D015119 | MESH_DESCRIPTOR_UI |
| 1189 | INN_ID |
| U6F3787206 | UNII |
| 4169 | MMSL |
| 4207 | MMSL |
| d00528 | MMSL |
| 6574 | IUPHAR_LIGAND_ID |
| 4017911 | VANDF |
| 002072 | NDDF |
| 360246003 | SNOMEDCT_US |
| 59882007 | SNOMEDCT_US |
| U6F3787206 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-1100 | SYRUP | 0.25 g | ORAL | NDA authorized generic | 19 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-1110 | TABLET | 1000 mg | ORAL | NDA authorized generic | 19 sections |
| AMINOCAPROIC ACID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0404-9812 | INJECTION, SOLUTION | 250 mg | INTRAVENOUS | ANDA | 12 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-4346 | INJECTION, SOLUTION | 250 mg | INTRAVENOUS | ANDA | 20 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-9120 | INJECTION, SOLUTION | 250 mg | INTRAVENOUS | ANDA | 19 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-9191 | INJECTION, SOLUTION | 250 mg | INTRAVENOUS | ANDA | 20 sections |
| Aminocaproic acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7165 | TABLET | 500 mg | ORAL | ANDA | 19 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13925-530 | TABLET | 500 mg | ORAL | ANDA | 19 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13925-531 | TABLET | 1000 mg | ORAL | ANDA | 19 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-447 | SYRUP | 0.25 g | ORAL | NDA authorized generic | 18 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-768 | TABLET | 500 mg | ORAL | NDA authorized generic | 18 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-769 | TABLET | 1000 mg | ORAL | NDA authorized generic | 18 sections |
| AMINOCAPROIC ACID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24658-798 | TABLET | 500 mg | ORAL | ANDA | 13 sections |
| AMINOCAPROIC ACID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24658-799 | TABLET | 1000 mg | ORAL | ANDA | 13 sections |
| AMINOCAPROIC ACID | HUMAN PRESCRIPTION DRUG LABEL | 1 | 31722-035 | SOLUTION | 0.25 g | ORAL | ANDA | 19 sections |
| Solmeet denti doctor | HUMAN OTC DRUG LABEL | 4 | 42352-2001 | PASTE, DENTIFRICE | 0.05 g | DENTAL | unapproved drug other | 8 sections |
| Solmeet | HUMAN OTC DRUG LABEL | 4 | 42352-3001 | PASTE, DENTIFRICE | 0.05 g | DENTAL | unapproved drug other | 8 sections |
| Solmeet | HUMAN OTC DRUG LABEL | 4 | 42352-7001 | PASTE, DENTIFRICE | 0.05 g | DENTAL | unapproved drug other | 8 sections |
| Solmeet denti doctor | HUMAN OTC DRUG LABEL | 4 | 42352-8001 | PASTE, DENTIFRICE | 0.05 g | DENTAL | unapproved drug other | 8 sections |
| AMICAR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49411-050 | TABLET | 500 mg | ORAL | NDA | 19 sections |
| AMICAR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49411-051 | TABLET | 1000 mg | ORAL | NDA | 19 sections |
| AMICAR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49411-052 | SOLUTION | 0.25 g | ORAL | NDA | 19 sections |
| Aminocaproic acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52817-815 | SOLUTION | 0.25 g | ORAL | ANDA | 19 sections |
| BAMBOO SALT Eunganggo Jook Yeom Toothpaste | HUMAN OTC DRUG LABEL | 7 | 53208-459 | PASTE | 0.05 g | DENTAL | OTC monograph not final | 4 sections |
| BAMBOO SALT Eunganggo Jook Yeom | HUMAN OTC DRUG LABEL | 7 | 53208-505 | PASTE | 0.05 g | DENTAL | OTC monograph not final | 8 sections |
| Aminocaproic acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54288-151 | SOLUTION | 0.25 g | ORAL | ANDA | 19 sections |
| Aminocaproic Acid | Human Prescription Drug Label | 1 | 59651-573 | SOLUTION | 0.25 g | ORAL | ANDA | 19 sections |
| Aminocaproic acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60219-1637 | TABLET | 500 mg | ORAL | ANDA | 19 sections |
| Aminocaproic Acid | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-739 | TABLET | 500 mg | ORAL | ANDA | 20 sections |
| AMICAR | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-3023 | TABLET | 500 mg | ORAL | NDA | 19 sections |