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durlobactam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-lactamase inhibitors | 5731 | 1467829-71-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -2.545 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.764 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.200 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.718 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 74.560 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 66.100 | % | High | 1 |
| herg | hERG pIC50 | 4.065 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.047 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.592 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 76.270 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PRKDC,SYK,TEK | 20 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,EPHB4,ERBB2,GRK2,MAP2K6,MAP3K14,MAPK7,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 15 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.254 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 3.724 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 84.030 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.308 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 69.710 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.629 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 94.840 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 72.410 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 845.279 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| ATC | J01CG30 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE BETA-LACTAM ANTIBACTERIALS, PENICILLINS Beta-lactamase inhibitors |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D065093 | beta-Lactamase Inhibitors |
| FDA MoA | N0000000202 | beta Lactamase Inhibitors |
| FDA EPC | N0000175930 | beta Lactamase Inhibitor |
| CHEBI has role | CHEBI:35625 | EC 3.5.2.6 (β-lactamase) inhibitor |
| CHEBI has role | CHEBI:36047 | antibacterial drug |
Related Drugs by ATC class:
J01CG Beta-lactamase inhibitors 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| CHEBI:229539 | CHEBI |
| CHEMBL4298137 | ChEMBL_ID |
| C000626193 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12693 | IUPHAR_LIGAND_ID |
| DB16704 | DRUGBANK_ID |
| 4042481 | VANDF |
| 4042482 | VANDF |
| C5420986 | UMLSCUI |
| CHEMBL4297378 | ChEMBL_ID |
| 10824 | INN_ID |
| 1467157-21-6 | SECONDARY_CAS_RN |
| 89851852 | PUBCHEM_CID |
| 368020 | MMSL |
| 41619 | MMSL |
| d10064 | MMSL |
| 019452 | NDDF |
| 019453 | NDDF |
| D11591 | KEGG_DRUG |
| PSA33KO9WA | UNII |
| 2639089 | RXNORM |
| C000714947 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
None