erythromycin acistrate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
1049 96128-89-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • erythromycin acistrate
  • oxacyclotetradecane, erythromycin deriv.
  • 2'-Acetylerythromycin stearate
  • erasis
prodrug of erythromycin; 2'-acetyl ester & stearate salt of erythromycin
  • Molecular weight: 775.97
  • Formula: C39H69NO14
  • CLOGP: 2.48
  • LIPINSKI: 2
  • HAC: 15
  • HDO: 4
  • TPSA: 199.98
  • ALOGS: -3.49
  • ROTB: 9

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BA (Bioavailability) 35 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.211 High 0.84
caco2-efflux Caco-2 efflux ratio (BA/AB) 40.087 High 0.84
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 1.766 10^-6 cm/s High 0.84
dh-clint Dog hepatocyte intrinsic clearance 15.740 uL/min/10^6 cells High 0.84
dppb Dog plasma protein binding (% unbound) 32.020 % High 0.84
fcs-ppb Fetal calf serum protein binding (% unbound) 35.520 % High 0.84
herg hERG pIC50 4.203 pIC50 High 0.84
hh-clint Human hepatocyte intrinsic clearance 3.614 uL/min/10^6 cells High 0.84
hlm-clint Human liver microsomal intrinsic clearance 38.371 uL/min/mg protein High 0.84
hppb Human plasma protein binding (% unbound) 38.140 % High 0.84
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 2.944 High 0.85
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 8.054 High 0.84
mh-clint Mouse hepatocyte intrinsic clearance 11.041 High 0.84
mppb Mouse plasma protein binding (% unbound) 34.830 High 0.84
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 10.740 High 0.84
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 0.85
pppb Pig plasma protein binding (% unbound) 39.340 % High 0.84
rat-kpuu-brain Rat brain Kpuu 0.015 % High 0.85
rh-clint Rat hepatocyte intrinsic clearance 8.054 uL/min/10^6 cells High 0.84
rh-fuinc Rat hepatocyte fraction unbound in incubation 71.010 % High 0.84
rppb Rat plasma protein binding (% unbound) 30.680 % High 0.84
solubility-dd Solubility at pH 7.4 in DMSO 623.735 uM High 0.84

Approvals:

None

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:

SourceCodeDescription
FDA CS M0028311 Macrolides
FDA PE N0000009982 Decreased Sebaceous Gland Activity
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005765 Gastrointestinal Agents
MeSH PA D011500 Protein Synthesis Inhibitors
FDA EPC N0000175877 Macrolide
FDA EPC N0000175935 Macrolide Antimicrobial
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:76969 bacterial metabolite
CHEBI has role CHEBI:78298 environmental contaminant

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 levelDissociation constantType (acidic/basic)
pKa1 7.62 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D02523 KEGG_DRUG
4017594 VANDF
C0116531 UMLSCUI
CHEMBL1908310 ChEMBL_ID
C056625 MESH_SUPPLEMENTAL_RECORD_UI
5728 INN_ID
6383U5A1KE UNII
5284554 PUBCHEM_CID
4053 RXNORM
4675 MMSL
4799 MMSL
72164 MMSL
d00046 MMSL
002755 NDDF
30427009 SNOMEDCT_US
372694001 SNOMEDCT_US
C0014806 UMLSCUI
CHEBI:135882 CHEBI
DB00199 DRUGBANK_ID
12560 PUBCHEM_CID
39 INN_ID
D004917 MESH_DESCRIPTOR_UI
CHEBI:42355 CHEBI

Pharmaceutical products:

None