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cyclacillin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, 6-aminopenicillanic acid derivatives | 632 | 3485-14-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A cyclohexylamido analog of PENICILLANIC ACID.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 97.53 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 90 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.169 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.531 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.461 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.963 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 79.920 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 64.170 | % | High | 1 |
| herg | hERG pIC50 | 4.285 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.112 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.083 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 86.050 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK7,NTRK2,PDK1,PDK2,PRKDC,SYK,TEK,TGFBR1 | 20 | |||
| kinase-selectivity-class | GRK2 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 1.607 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 1.963 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 79.590 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 2.270 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 74.250 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.500 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 87.240 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 82.250 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 939.723 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 13, 1979 | FDA | WYETH AYERST |
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 |
|---|---|---|
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Infection of skin AND/OR subcutaneous tissue | indication | 19824006 | |
| Bronchitis | indication | 32398004 | DOID:6132 |
| Urinary tract infectious disease | indication | 68566005 | |
| Infective otitis media | indication | 312218008 | |
| Pharyngitis | indication | 405737000 | DOID:2275 |
| Sinusitis | off-label use | 36971009 | |
| Cholangitis | off-label use | 82403002 | DOID:9446 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Infectious mononucleosis | contraindication | 271558008 | DOID:8568 |
| Pseudomembranous enterocolitis | contraindication | 397683000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.79 | acidic |
| pKa2 | 8.58 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Bacterial penicillin-binding protein | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Penicillin-binding protein 1A | Enzyme | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| 4018054 | VUID |
| N0000146395 | NUI |
| D01334 | KEGG_DRUG |
| 2968 | RXNORM |
| CHEBI:31444 | CHEBI |
| CHEMBL1200356 | ChEMBL_ID |
| 4817 | IUPHAR_LIGAND_ID |
| 2764 | INN_ID |
| DB01000 | DRUGBANK_ID |
| 72ZJ154X86 | UNII |
| 002696 | NDDF |
| 387382002 | SNOMEDCT_US |
| 69331001 | SNOMEDCT_US |
| C0010523 | UMLSCUI |
| D003493 | MESH_DESCRIPTOR_UI |
| 19003 | PUBCHEM_CID |
| 4018054 | VANDF |
| 72ZJ154X86 | INXIGHT DRUGS |
Pharmaceutical products:
None