durlobactam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
beta-lactamase inhibitors 5731 1467829-71-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • durlobactam
  • durlobactam sodium
  • xacduro
  • EXT2514
Durlobactam is a diazabicyclooctane non-beta-lactam, beta-lactamase inhibitor, that protects sulbactam from degradation by certain serine-beta-lactamases. Durlobactam alone does not have antibacterial activity against Acinetobacter baumannii-calcoaceticus complex (ABC) isolates but in combination with sulbactam it has been approved for the treatment of hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia (HABP/VABP), caused by susceptible isolates of Acinetobacter baumannii-calcoaceticus complex.
  • Molecular weight: 277.25
  • Formula: C8H11N3O6S
  • CLOGP:
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 130.24
  • ALOGS:
  • ROTB: 3

  • Status: OFP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 23, 2023 FDA ENTASIS THERAP

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
MeSH PA D000900 Anti-Bacterial Agents
MeSH PA D000890 Anti-Infective Agents
MeSH PA D065093 beta-Lactamase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
FDA MoA N0000000202 beta Lactamase Inhibitors
FDA EPC N0000175930 beta Lactamase Inhibitor

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

DiseaseRelationSNOMED_IDDOID
Ventilator-associated bacterial pneumonia caused by acinetobacter baumannii-calcoaceticus complex indication 429271009
Infection caused by carbapenem-resistant acinetobacter baumannii-calcoaceticus complex indication 445780006
Hospital-acquired bacterial pneumonia caused by acinetobacter baumannii-calcoaceticus complex indication 1010634002




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL XACDURO (COPACKAGED) ENTASIS THERAP N216974 May 23, 2023 RX POWDER INTRAVENOUS 9623014 April 2, 2033 TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL XACDURO (COPACKAGED) ENTASIS THERAP N216974 May 23, 2023 RX POWDER INTRAVENOUS 10376499 Nov. 17, 2035 TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL XACDURO (COPACKAGED) ENTASIS THERAP N216974 May 23, 2023 RX POWDER INTRAVENOUS 9968593 Nov. 17, 2035 TREATMENT OF HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL XACDURO (COPACKAGED) ENTASIS THERAP N216974 May 23, 2023 RX POWDER INTRAVENOUS May 23, 2028 NEW CHEMICAL ENTITY
EQ 500MG BASE/VIAL; EQ 500MG BASE/VIAL;EQ 1GM BASE/VIAL XACDURO (COPACKAGED) ENTASIS THERAP N216974 May 23, 2023 RX POWDER INTRAVENOUS May 23, 2033 GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Betalactamase OXA24 Enzyme INHIBITOR IC50 6.72 SCIENTIFIC LITERATURE DRUG LABEL
Beta-lactamase Enzyme INHIBITOR IC50 7.86 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
CHEMBL4298137 ChEMBL_ID
C000626193 MESH_SUPPLEMENTAL_RECORD_UI
12693 IUPHAR_LIGAND_ID
DB16704 DRUGBANK_ID
019452 NDDF
019453 NDDF
C5420986 UMLSCUI
CHEMBL4297378 ChEMBL_ID
10824 INN_ID
1467157-21-6 SECONDARY_CAS_RN
89851852 PUBCHEM_CID
2639089 RXNORM
D11591 KEGG_DRUG
PSA33KO9WA UNII
41619 MMSL
d10064 MMSL

Pharmaceutical products:

None