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racecadotril 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| endopeptidase inhibitors | 60 | 81110-73-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A potent inhibitor of membrane metalloendopeptidase (ENKEPHALINASE). Thiorphan potentiates morphine-induced ANALGESIA and attenuates naloxone-precipitated withdrawal symptoms.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 11.12 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKDC,STK33,TEK,TTK | 36 | |||
| kinase-selectivity-class | AXL,EIF2AK3,GRK2,PDK4 | 4 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1993 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Rash maculo-papular | 133.57 | 40.22 | 49 | 2654 | 40884 | 90584860 |
| Drug reaction with eosinophilia and systemic symptoms | 124.19 | 40.22 | 47 | 2656 | 42711 | 90583033 |
| Acute kidney injury | 113.61 | 40.22 | 86 | 2617 | 320301 | 90305443 |
| Hepatic cytolysis | 104.49 | 40.22 | 38 | 2665 | 30878 | 90594866 |
| Cholestasis | 98.55 | 40.22 | 38 | 2665 | 36261 | 90589483 |
| Agranulocytosis | 78.75 | 40.22 | 32 | 2671 | 34970 | 90590774 |
| Aplasia | 62.58 | 40.22 | 16 | 2687 | 3975 | 90621769 |
| Pancytopenia | 60.30 | 40.22 | 40 | 2663 | 120223 | 90505521 |
| Acute generalised exanthematous pustulosis | 58.29 | 40.22 | 20 | 2683 | 13683 | 90612061 |
| Hepatocellular injury | 56.75 | 40.22 | 24 | 2679 | 28934 | 90596810 |
| Febrile bone marrow aplasia | 56.63 | 40.22 | 18 | 2685 | 9720 | 90616024 |
| Eosinophilia | 53.77 | 40.22 | 23 | 2680 | 28510 | 90597234 |
| Thrombocytopenia | 50.52 | 40.22 | 45 | 2658 | 208680 | 90417064 |
| Pancreatitis acute | 47.99 | 40.22 | 22 | 2681 | 32093 | 90593651 |
| Housebound | 47.97 | 40.22 | 8 | 2695 | 238 | 90625506 |
| Hypokalaemia | 45.80 | 40.22 | 35 | 2668 | 131081 | 90494663 |
| Granulomatous liver disease | 42.90 | 40.22 | 9 | 2694 | 940 | 90624804 |
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 |
|---|---|---|---|---|---|---|
| Toxic epidermal necrolysis | 196.35 | 30.72 | 71 | 2646 | 26679 | 42591939 |
| Alveolar lung disease | 104.02 | 30.72 | 19 | 2698 | 443 | 42618175 |
| Pulmonary interstitial emphysema syndrome | 100.27 | 30.72 | 19 | 2698 | 544 | 42618074 |
| Hepatocellular injury | 99.50 | 30.72 | 42 | 2675 | 23636 | 42594982 |
| Diffuse alveolar damage | 76.16 | 30.72 | 20 | 2697 | 2572 | 42616046 |
| Eosinophilic pneumonia | 59.53 | 30.72 | 19 | 2698 | 4855 | 42613763 |
| Acute kidney injury | 58.18 | 30.72 | 92 | 2625 | 367245 | 42251373 |
| Hyperammonaemia | 58.01 | 30.72 | 21 | 2696 | 7845 | 42610773 |
| Eosinophilia | 57.47 | 30.72 | 32 | 2685 | 32867 | 42585751 |
| Generalised oedema | 50.70 | 30.72 | 23 | 2694 | 15313 | 42603305 |
| Angioedema | 49.89 | 30.72 | 32 | 2685 | 42445 | 42576173 |
| Rash maculo-papular | 48.42 | 30.72 | 30 | 2687 | 37473 | 42581145 |
| Hepatic cytolysis | 43.85 | 30.72 | 25 | 2692 | 26819 | 42591799 |
| Enterobacter sepsis | 40.69 | 30.72 | 10 | 2707 | 985 | 42617633 |
| Hepatic encephalopathy | 40.09 | 30.72 | 20 | 2697 | 16422 | 42602196 |
| Cholestasis | 39.17 | 30.72 | 25 | 2692 | 32854 | 42585764 |
| Glomerular filtration rate decreased | 37.26 | 30.72 | 19 | 2698 | 16332 | 42602286 |
| Confusional state | 35.06 | 30.72 | 48 | 2669 | 167549 | 42451069 |
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 |
|---|---|---|---|---|---|---|
| Toxic epidermal necrolysis | 199.79 | 31.44 | 83 | 5506 | 56644 | 110527066 |
| Rash maculo-papular | 162.95 | 31.44 | 78 | 5511 | 74144 | 110509566 |
| Acute kidney injury | 155.68 | 31.44 | 175 | 5414 | 635255 | 109948455 |
| Hepatocellular injury | 151.41 | 31.44 | 66 | 5523 | 50576 | 110533134 |
| Hepatic cytolysis | 142.95 | 31.44 | 65 | 5524 | 54988 | 110528722 |
| Cholestasis | 127.14 | 31.44 | 63 | 5526 | 64455 | 110519255 |
| Drug reaction with eosinophilia and systemic symptoms | 118.33 | 31.44 | 65 | 5524 | 82030 | 110501680 |
| Alveolar lung disease | 112.62 | 31.44 | 21 | 5568 | 698 | 110583012 |
| Eosinophilia | 109.49 | 31.44 | 55 | 5534 | 57881 | 110525829 |
| Pulmonary interstitial emphysema syndrome | 104.24 | 31.44 | 19 | 5570 | 556 | 110583154 |
| Pancytopenia | 80.80 | 31.44 | 74 | 5515 | 209539 | 110374171 |
| Agranulocytosis | 78.36 | 31.44 | 45 | 5544 | 61715 | 110521995 |
| Angioedema | 72.84 | 31.44 | 51 | 5538 | 98449 | 110485261 |
| Diffuse alveolar damage | 71.90 | 31.44 | 20 | 5569 | 4027 | 110579683 |
| Acute generalised exanthematous pustulosis | 60.70 | 31.44 | 27 | 5562 | 21637 | 110562073 |
| Thrombocytopenia | 60.50 | 31.44 | 81 | 5508 | 348804 | 110234906 |
| Febrile bone marrow aplasia | 59.53 | 31.44 | 25 | 5564 | 17440 | 110566270 |
| Eosinophilic pneumonia | 56.48 | 31.44 | 19 | 5570 | 7208 | 110576502 |
| Hyperammonaemia | 51.34 | 31.44 | 21 | 5568 | 13711 | 110569999 |
| Confusional state | 47.63 | 31.44 | 85 | 5504 | 468595 | 110115115 |
| Generalised oedema | 46.09 | 31.44 | 25 | 5564 | 30679 | 110553031 |
| Housebound | 44.60 | 31.44 | 9 | 5580 | 454 | 110583256 |
| Hypokalaemia | 40.54 | 31.44 | 48 | 5541 | 182400 | 110401310 |
| Enterobacter sepsis | 39.91 | 31.44 | 10 | 5579 | 1346 | 110582364 |
| Aplasia | 39.86 | 31.44 | 15 | 5574 | 7858 | 110575852 |
| Hepatic encephalopathy | 39.63 | 31.44 | 22 | 5567 | 28234 | 110555476 |
| Drug ineffective | 39.36 | 31.44 | 14 | 5575 | 1520526 | 109063184 |
| Diarrhoea | 38.15 | 31.44 | 135 | 5454 | 1139370 | 109444340 |
| Pancreatitis acute | 37.22 | 31.44 | 28 | 5561 | 60246 | 110523464 |
| Mixed liver injury | 36.89 | 31.44 | 16 | 5573 | 12063 | 110571647 |
| Neutropenia | 36.82 | 31.44 | 67 | 5522 | 374553 | 110209157 |
| Gamma-glutamyltransferase increased | 34.60 | 31.44 | 27 | 5562 | 61282 | 110522428 |
| General physical condition abnormal | 33.20 | 31.44 | 13 | 5576 | 7577 | 110576133 |
| Distal intestinal obstruction syndrome | 32.38 | 31.44 | 8 | 5581 | 1017 | 110582693 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A07XA04 | ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS OTHER ANTIDIARRHEALS Other antidiarrheals |
| MeSH PA | D000930 | Antidiarrheals |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D011480 | Protease Inhibitors |
Related Drugs by ATC class:
A07XA Other antidiarrheals 1 drug
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute diarrhea | indication | 409966000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Neprilysin | Enzyme | INHIBITOR | IC50 | 9 | CHEMBL | KEGG DRUG | |||
| Endothelin-converting enzyme 1 | Enzyme | IC50 | 8.10 | CHEMBL | |||||
| Angiotensin-converting enzyme | Enzyme | IC50 | 6.50 | CHEMBL | |||||
| Puromycin-sensitive aminopeptidase | Enzyme | IC50 | 4.24 | CHEMBL | |||||
| Angiotensin-converting enzyme | Enzyme | IC50 | 6.38 | CHEMBL | |||||
| Neprilysin | Enzyme | IC50 | 8.32 | CHEMBL | |||||
| Neprilysin | Enzyme | IC50 | 8.40 | CHEMBL | |||||
| Neprilysin | Enzyme | IC50 | 8.21 | CHEMBL | |||||
| Thermolysin | Enzyme | IC50 | 5.02 | CHEMBL | |||||
| Beta-lactamase NDM-1 | Enzyme | IC50 | 5.75 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4025231 | VUID |
| N0000179029 | NUI |
| D08464 | KEGG_DRUG |
| 112573-73-6 | SECONDARY_CAS_RN |
| 16738 | RXNORM |
| C0050461 | UMLSCUI |
| CHEBI:750459 | CHEBI |
| TIO | PDB_CHEM_ID |
| CHEMBL2103772 | ChEMBL_ID |
| CHEMBL1516410 | ChEMBL_ID |
| DB11696 | DRUGBANK_ID |
| C049331 | MESH_SUPPLEMENTAL_RECORD_UI |
| 107751 | PUBCHEM_CID |
| 11654 | IUPHAR_LIGAND_ID |
| 7378 | INN_ID |
| 76K53XP4TO | UNII |
| DB08626 | DRUGBANK_ID |
| C0039945 | UMLSCUI |
| CHEMBL10247 | ChEMBL_ID |
| 6896 | INN_ID |
| 76721-89-6 | SECONDARY_CAS_RN |
| 3132 | PUBCHEM_CID |
| 5278 | IUPHAR_LIGAND_ID |
| 4025231 | VANDF |
| D015244 | MESH_DESCRIPTOR_UI |
| B79L7B5X3Z | UNII |
| 006079 | NDDF |
| 699272003 | SNOMEDCT_US |
| 714679008 | SNOMEDCT_US |
| 785287002 | SNOMEDCT_US |
| CHEBI:9568 | CHEBI |
| 76K53XP4TO | INXIGHT DRUGS |
Pharmaceutical products:
None