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enoximone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1014 | 77671-31-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 96.65 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 55 % | |
| Vd (Volume of distribution) | 1.48 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 19.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.30 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.94 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.783 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 7.447 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 32.961 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.592 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 34.780 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 38.090 | % | High | 1 |
| herg | hERG pIC50 | 4.132 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.598 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 18.030 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 31.370 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IRAK1,ITK,JAK1,JAK2,KIT,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 | 58 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,GRK2,MAP2K3,MAP2K6,MAPK12,MAPK7,MARK4,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ULK1 | 23 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 9.036 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 50.350 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 36.050 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 9.183 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 35.680 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 17.022 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.130 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 22.830 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 74.989 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1988 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C01CE03 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Phosphodiesterase inhibitors |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D010726 | Phosphodiesterase Inhibitors |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D058987 | Phosphodiesterase 3 Inhibitors |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C01CE Phosphodiesterase inhibitors 3 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.41 | acidic |
| pKa2 | 13.0 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| cGMP-inhibited 3',5'-cyclic phosphodiesterase A | Enzyme | IC50 | 5.35 | WOMBAT-PK | |||||
| Phosphodiesterase 4 | Enzyme | IC50 | 5.54 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167073 | NUI |
| D04004 | KEGG_DRUG |
| C0116190 | UMLSCUI |
| CHEBI:135010 | CHEBI |
| CHEMBL249856 | ChEMBL_ID |
| DB04880 | DRUGBANK_ID |
| D017335 | MESH_DESCRIPTOR_UI |
| 53708 | PUBCHEM_CID |
| 9063 | IUPHAR_LIGAND_ID |
| 5582 | INN_ID |
| C7Z4ITI7L7 | UNII |
| 49626 | RXNORM |
| 003676 | NDDF |
| 320067009 | SNOMEDCT_US |
| 396042009 | SNOMEDCT_US |
Pharmaceutical products:
None