doripenem 🐶 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 4149 148016-81-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • doribax
  • doripenem
  • doripenem hydrate
A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.
  • Molecular weight: 420.50
  • Formula: C15H24N4O6S2
  • CLOGP: -2.84
  • LIPINSKI: 0
  • HAC: 10
  • HDO: 5
  • TPSA: 162.06
  • ALOGS: -2.13
  • ROTB: 6
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.50 g P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.23 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.26 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.92 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.20 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 0 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -1.206 Moderate 0.75
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.567 Moderate 0.75
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.388 10^-6 cm/s Moderate 0.75
dh-clint Dog hepatocyte intrinsic clearance 1.954 uL/min/10^6 cells Moderate 0.75
dppb Dog plasma protein binding (% unbound) 86.670 % Moderate 0.75
fcs-ppb Fetal calf serum protein binding (% unbound) 62.400 % Moderate 0.75
herg hERG pIC50 4.542 pIC50 Moderate 0.75
hh-clint Human hepatocyte intrinsic clearance 1.690 uL/min/10^6 cells Moderate 0.75
hlm-clint Human liver microsomal intrinsic clearance 3.715 uL/min/mg protein Moderate 0.75
hppb Human plasma protein binding (% unbound) 76.640 % Moderate 0.75
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MAP2K6,MAP3K21,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 35
kinase-selectivity-class AXL,CDK16,CDK4,CDK9,CHUK,EIF2AK3,GRK2,MAP2K6,MAP3K14,PDK1,TEK 11
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.592 Moderate 0.75
mh-clint Mouse hepatocyte intrinsic clearance 6.808 Moderate 0.75
mppb Mouse plasma protein binding (% unbound) 78.010 Moderate 0.75
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 2 Moderate 0.75
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 71.670 % Moderate 0.75
rh-clint Rat hepatocyte intrinsic clearance 2.818 uL/min/10^6 cells Moderate 0.75
rh-fuinc Rat hepatocyte fraction unbound in incubation 90.340 % Moderate 0.75
rppb Rat plasma protein binding (% unbound) 69.660 % Moderate 0.75
solubility-dd Solubility at pH 7.4 in DMSO 881.049 uM Moderate 0.75

Approvals:

DateAgencyCompanyOrphan
Oct. 12, 2007 FDA SHIONOGI INC

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 J01DH04 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
Carbapenems
FDA CS M0024174 Carbapenems
FDA EPC N0000175496 Penem Antibacterial
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000900 Anti-Bacterial Agents
CHEBI has role CHEBI:33282 antibacterial agent
CHEBI has role CHEBI:35441 antiinfective agent

Related Drugs by ATC class:

J01DH Carbapenems 10 drugs
betamipronbiapenemcilastatinertapenemimipenemmeropenempanipenemrelebactamtebipenem pivoxilvaborbactam

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

DiseaseRelationSNOMED_IDDOID
Pyelonephritis indication 45816000 DOID:11400
Abdominal abscess indication 75100008
Cholecystitis indication 76581006 DOID:1949
Infectious disease of abdomen indication 128070006
Complicated appendicitis indication 418171008
Complicated Urinary Tract Infections indication
Impaired renal function disorder contraindication 197663003
Pseudomembranous enterocolitis contraindication 397683000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.79 acidic
pKa2 8.53 acidic
pKa3 11.22 acidic
pKa4 9.17 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
Bacterial penicillin-binding protein Enzyme INHIBITOR CHEMBL CHEMBL

External reference:

IDSource
D01836 KEGG_DRUG
4026738 VANDF
C0389169 UMLSCUI
O6P PDB_CHEM_ID
CHEMBL491571 ChEMBL_ID
CHEMBL4303454 ChEMBL_ID
D000077726 MESH_DESCRIPTOR_UI
DB06211 DRUGBANK_ID
12183 IUPHAR_LIGAND_ID
7975 INN_ID
BHV525JOBH UNII
73303 PUBCHEM_CID
119771 RXNORM
121413 MMSL
24610 MMSL
246877 MMSL
d07049 MMSL
012366 NDDF
428352004 SNOMEDCT_US
429369006 SNOMEDCT_US
CHEBI:135928 CHEBI

Pharmaceutical products:

None