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cefsulodin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, cefalosporanic acid derivatives | 558 | 62587-73-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A pyridinium-substituted semisynthetic, broad-spectrum antibacterial used especially for Pseudomonas infections in debilitated patients.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 50 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 187.77 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.29 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.96 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.64 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 | -2.402 | High | 0.88 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.288 | High | 0.88 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.284 | 10^-6 cm/s | High | 0.88 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.746 | uL/min/10^6 cells | High | 0.88 |
| dppb | Dog plasma protein binding (% unbound) | 82.590 | % | High | 0.88 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 73.180 | % | High | 0.88 |
| herg | hERG pIC50 | 4.356 | pIC50 | High | 0.88 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.552 | uL/min/10^6 cells | High | 0.88 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.648 | uL/min/mg protein | High | 0.88 |
| hppb | Human plasma protein binding (% unbound) | 73.860 | % | High | 0.88 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GRK3,GSK3B,ITK,JAK2,KIT,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TTK,ZAP70 | 47 | |||
| kinase-selectivity-class | AXL,CDK9,EIF2AK3,GRK2,MAP2K6,MAPK7,STK33,TEK | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.395 | High | 0.88 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.844 | High | 0.88 | |
| mppb | Mouse plasma protein binding (% unbound) | 79.020 | High | 0.88 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.973 | High | 0.88 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 64.320 | % | High | 0.88 |
| rh-clint | Rat hepatocyte intrinsic clearance | 2.056 | uL/min/10^6 cells | High | 0.88 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.620 | % | High | 0.88 |
| rppb | Rat plasma protein binding (% unbound) | 57.710 | % | High | 0.88 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 922.571 | uM | High | 0.88 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1981 | 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 | J01DD03 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Third-generation cephalosporins |
| CHEBI has role | CHEBI:33282 | antibacterial agent |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
Related Drugs by ATC class:
J01DD Third-generation cephalosporins 17 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 | 0.17 | acidic |
| pKa2 | 2.83 | acidic |
| pKa3 | 12.0 | acidic |
| pKa4 | 12.33 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-adrenergic receptor kinase 1 | Kinase | EC50 | 7.15 | CHEMBL | |||||
| Tyrosine-protein phosphatase non-receptor type 11 | Enzyme | IC50 | 4.77 | CHEMBL | |||||
| Lethal(3)malignant brain tumor-like protein 1 | Nuclear other | IC50 | 7.01 | CHEMBL | |||||
| Protein-tyrosine phosphatase 1C | Enzyme | IC50 | 4.68 | CHEMBL | |||||
| Penicillin-binding protein 1A | Enzyme | IC50 | 6.52 | WOMBAT-PK | |||||
| Penicillin-binding protein 1B | Enzyme | IC50 | 5.33 | WOMBAT-PK | |||||
| tRNA 2'-phosphotransferase | Enzyme | IC50 | 5.77 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000166876 | NUI |
| D02005 | KEGG_DRUG |
| 2190 | RXNORM |
| C0007558 | UMLSCUI |
| CHEBI:3507 | CHEBI |
| CHEMBL3351077 | ChEMBL_ID |
| D002441 | MESH_DESCRIPTOR_UI |
| DB13499 | DRUGBANK_ID |
| 10783 | IUPHAR_LIGAND_ID |
| 4390 | INN_ID |
| 52152-93-9 | SECONDARY_CAS_RN |
| OV42LHE42B | UNII |
| 656575 | PUBCHEM_CID |
| 003801 | NDDF |
| 003802 | NDDF |
| 387537000 | SNOMEDCT_US |
| 96053001 | SNOMEDCT_US |
| 3LU | PDB_CHEM_ID |
| CHEMBL1590946 | ChEMBL_ID |
Pharmaceutical products:
None