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

Stem definitionDrug idCAS RN
analogues of penicillanic acid antibiotics modified in the five-membered ring 2574 161715-24-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tebipenem pivoxil
  • orapenem
an oral carbapenem antibiotic, against penicillin-nonsusceptible Streptococcus pneumoniae
  • Molecular weight: 497.63
  • Formula: C22H31N3O6S2
  • CLOGP: 2.77
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 108.74
  • ALOGS: -3.47
  • ROTB: 9

Drug dosage:

DoseUnitRoute
0.56 g O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.864 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 7.656 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 4.457 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 52.240 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 14.120 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 16.470 % High 1
herg hERG pIC50 4.876 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 203.704 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 299.226 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 9.560 % High 1
kinase-safety-class ACVR2A,ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,IGF1R,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TTK,ZAP70 47
kinase-selectivity-class AXL,GRK2,PDK1 3
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 16.749 High 1
mh-clint Mouse hepatocyte intrinsic clearance 432.514 High 1
mppb Mouse plasma protein binding (% unbound) 15.370 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 27.925 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 25.130 % High 1
rh-clint Rat hepatocyte intrinsic clearance 397.192 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 68.680 % High 1
rppb Rat plasma protein binding (% unbound) 14.570 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 130.017 uM High 1

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
ATC J01DH06 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
Carbapenems
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35441 antiinfective agent
CHEBI has role CHEBI:231911 renoprotective agent

Related Drugs by ATC class:

J01DH Carbapenems 10 drugs
betamipronbiapenemcilastatindoripenemertapenemimipenemmeropenempanipenemrelebactamvaborbactam

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 9.8 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
Prolyl endopeptidase FAP Enzyme Ki 6.19 CHEMBL

External reference:

IDSource
D09598 KEGG_DRUG
C2699902 UMLSCUI
CHEBI:135799 CHEBI
1TE PDB_CHEM_ID
CHEMBL2107486 ChEMBL_ID
DB16840 DRUGBANK_ID
C120999 MESH_SUPPLEMENTAL_RECORD_UI
10864 IUPHAR_LIGAND_ID
7924 INN_ID
95AK1A52I8 UNII
9892071 PUBCHEM_CID
C1568612 UMLSCUI
CHEMBL576981 ChEMBL_ID
161715-21-5 SECONDARY_CAS_RN
9800194 PUBCHEM_CID
C500135 MESH_SUPPLEMENTAL_RECORD_UI
Q2TWQ1I31U UNII
CHEBI:749078 CHEBI

Pharmaceutical products:

None