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

Stem definitionDrug idCAS RN
antibiotics, produced by Streptomyces strains 1052 134-36-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • erythromycin estolate
  • erythromycin propionate
  • propiocine
  • propionyl erythromicin
  • propionylerythromycin
A macrolide antibiotic, produced by Streptomyces erythreus. It is the lauryl sulfate salt of the propionic ester of erythromycin. This erythromycin salt acts primarily as a bacteriostatic agent. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.
  • Molecular weight: 790.00
  • Formula: C40H71NO14
  • CLOGP: 3
  • LIPINSKI: 2
  • HAC: 15
  • HDO: 4
  • TPSA: 199.98
  • ALOGS: -3.63
  • ROTB: 10

  • Status: OFM

  • 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 2.499 High 0.87
caco2-efflux Caco-2 efflux ratio (BA/AB) 27.040 High 0.87
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 4.656 10^-6 cm/s High 0.87
dh-clint Dog hepatocyte intrinsic clearance 18.578 uL/min/10^6 cells High 0.87
dppb Dog plasma protein binding (% unbound) 22.070 % High 0.87
fcs-ppb Fetal calf serum protein binding (% unbound) 29.040 % High 0.87
herg hERG pIC50 4.394 pIC50 High 0.87
hh-clint Human hepatocyte intrinsic clearance 6.237 uL/min/10^6 cells High 0.87
hlm-clint Human liver microsomal intrinsic clearance 68.549 uL/min/mg protein High 0.87
hppb Human plasma protein binding (% unbound) 25.830 % High 0.87
kinase-safety-class ACVR2B,AXL,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K21,MAPK7,NTRK2,PDK1,PDK2,PRKDC,TEK 17
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 4.102 High 0.84
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 11.169 High 0.87
mh-clint Mouse hepatocyte intrinsic clearance 16.218 High 0.87
mppb Mouse plasma protein binding (% unbound) 25.970 High 0.87
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 19.055 High 0.87
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 High 0.84
pppb Pig plasma protein binding (% unbound) 30.630 % High 0.87
rat-kpuu-brain Rat brain Kpuu 0.014 % High 0.84
rh-clint Rat hepatocyte intrinsic clearance 15.136 uL/min/10^6 cells High 0.87
rh-fuinc Rat hepatocyte fraction unbound in incubation 67.070 % High 0.87
rppb Rat plasma protein binding (% unbound) 23.770 % High 0.87
solubility-dd Solubility at pH 7.4 in DMSO 450.817 uM High 0.87

Approvals:

None

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
International normalised ratio fluctuation 317.51 77.58 50 917 3043 90624437
Bloody discharge 302.54 77.58 46 921 2217 90625263
Lyme disease 273.44 77.58 46 921 4216 90623264
Iron deficiency 152.41 77.58 32 935 9580 90617900
Secretion discharge 125.90 77.58 30 937 15866 90611614
Platelet count increased 122.75 77.58 31 936 20828 90606652
Therapeutic product effect incomplete 112.53 77.58 50 917 193846 90433634
Staphylococcal infection 96.92 77.58 31 936 48408 90579072
Drug hypersensitivity 93.75 77.58 59 908 463550 90163930
Infection 85.63 77.58 51 916 362043 90265437
Drug intolerance 85.52 77.58 55 912 447536 90179944
Red blood cell sedimentation rate increased 80.73 77.58 31 936 82564 90544916

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
International normalised ratio fluctuation 322.24 124.88 51 892 4029 110584327
Bloody discharge 311.85 124.88 47 896 2686 110585670
Lyme disease 290.39 124.88 47 896 4269 110584087
Iron deficiency 144.11 124.88 33 910 18443 110569913
Secretion discharge 130.59 124.88 31 912 20213 110568143
Platelet count increased 127.47 124.88 32 911 26302 110562054

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
CHEBI has role CHEBI:23924 enzyme inhibitor
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 7.61 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Bile salt export pump Transporter IC50 5.39 CHEMBL
Bile salt export pump Transporter IC50 4.94 CHEMBL

External reference:

IDSource
D02525 KEGG_DRUG
3521-62-8 SECONDARY_CAS_RN
4017593 VANDF
4017594 VANDF
C0059564 UMLSCUI
CHEBI:48913 CHEBI
CHEMBL2220427 ChEMBL_ID
CHEMBL2218877 ChEMBL_ID
C011807 MESH_SUPPLEMENTAL_RECORD_UI
HB75CIT999 UNII
71277 PUBCHEM_CID
4053 RXNORM
3636 MMSL
4675 MMSL
4676 MMSL
4799 MMSL
72164 MMSL
d00046 MMSL
002755 NDDF
002756 NDDF
005412 NDDF
10270000 SNOMEDCT_US
30427009 SNOMEDCT_US
372694001 SNOMEDCT_US
734518007 SNOMEDCT_US
D004918 MESH_DESCRIPTOR_UI
C0014806 UMLSCUI
DB00199 DRUGBANK_ID
12560 PUBCHEM_CID
39 INN_ID
D004917 MESH_DESCRIPTOR_UI
CHEBI:42355 CHEBI

Pharmaceutical products:

None