cefpirome ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, cefalosporanic acid derivatives 553 84957-29-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cefpirome sulfate
  • cefpirome
  • cefrom
  • Molecular weight: 514.58
  • Formula: C22H22N6O5S2
  • CLOGP: -4.61
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 2
  • TPSA: 153.92
  • ALOGS: -4.90
  • ROTB: 7

Drug dosage:

DoseUnitRoute
4 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 111.05 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 0.24 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.90 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.90 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.70 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 100 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.928 Moderate 0.65
caco2-efflux Caco-2 efflux ratio (BA/AB) 2.128 Moderate 0.65
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.676 10^-6 cm/s Moderate 0.65
dh-clint Dog hepatocyte intrinsic clearance 1.905 uL/min/10^6 cells Moderate 0.65
dppb Dog plasma protein binding (% unbound) 66.720 % Moderate 0.65
fcs-ppb Fetal calf serum protein binding (% unbound) 57.710 % Moderate 0.65
herg hERG pIC50 4.461 pIC50 Moderate 0.65
hh-clint Human hepatocyte intrinsic clearance 1.982 uL/min/10^6 cells Moderate 0.65
hlm-clint Human liver microsomal intrinsic clearance 5.585 uL/min/mg protein Moderate 0.65
hppb Human plasma protein binding (% unbound) 58.160 % Moderate 0.65
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,ITK,JAK2,JAK3,MAP2K6,MAP3K1,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MELK,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 59
kinase-selectivity-class AXL,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK7,STK33,TEK,TTK 9
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.923 Moderate 0.65
mh-clint Mouse hepatocyte intrinsic clearance 15.812 Moderate 0.65
mppb Mouse plasma protein binding (% unbound) 56.980 Moderate 0.65
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 3.936 Moderate 0.65
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 68.180 % Moderate 0.65
rh-clint Rat hepatocyte intrinsic clearance 8.017 uL/min/10^6 cells Moderate 0.65
rh-fuinc Rat hepatocyte fraction unbound in incubation 85.140 % Moderate 0.65
rppb Rat plasma protein binding (% unbound) 46.780 % Moderate 0.65
solubility-dd Solubility at pH 7.4 in DMSO 709.578 uM Moderate 0.65

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1983 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:

SourceCodeDescription
ATC J01DE02 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
Fourth-generation cephalosporins
CHEBI has role CHEBI:33282 antibacterial agent
MeSH PA D000097902 beta Lactam Antibiotics
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents

Related Drugs by ATC class:

J01DE Fourth-generation cephalosporins 2 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

None




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.67 acidic
pKa2 13.31 acidic
pKa3 3.3 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
D01401 KEGG_DRUG
98753-19-6 SECONDARY_CAS_RN
151497 RXNORM
C0062986 UMLSCUI
CHEBI:3503 CHEBI
CHEMBL65794 ChEMBL_ID
CHEMBL2106076 ChEMBL_ID
D000097572 MESH_DESCRIPTOR_UI
DB13682 DRUGBANK_ID
12033 IUPHAR_LIGAND_ID
5414 INN_ID
S72Q2F09HY UNII
5479539 PUBCHEM_CID
387533001 SNOMEDCT_US
441741005 SNOMEDCT_US
96047001 SNOMEDCT_US
005103 NDDF
005104 NDDF

Pharmaceutical products:

None