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

Stem definitionDrug idCAS RN
beta-lactamase inhibitors 4946 1192500-31-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • NXL-104
  • avibactam
  • NXL104
  • AVE1330A
  • avibactam sodium
a non-beta-lactam beta-lactamase inhibitor that inactivates some beta-lactamases and protects ceftazidime from degradation by certain beta-lactamases
  • Molecular weight: 265.24
  • Formula: C7H11N3O6S
  • CLOGP: -4.18
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 130.24
  • ALOGS: -1.25
  • ROTB: 3
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.24 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.76 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.93 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.70 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 10 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -2.898 Moderate 0.68
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.933 Moderate 0.68
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 0.202 10^-6 cm/s Moderate 0.68
dh-clint Dog hepatocyte intrinsic clearance 2.754 uL/min/10^6 cells Moderate 0.68
dppb Dog plasma protein binding (% unbound) 77.010 % Moderate 0.68
fcs-ppb Fetal calf serum protein binding (% unbound) 69.710 % Moderate 0.68
herg hERG pIC50 4.007 pIC50 Moderate 0.68
hh-clint Human hepatocyte intrinsic clearance 1.050 uL/min/10^6 cells Moderate 0.68
hlm-clint Human liver microsomal intrinsic clearance 4.315 uL/min/mg protein Moderate 0.68
hppb Human plasma protein binding (% unbound) 75.810 % Moderate 0.68
kinase-safety-class ACVR2B,AXL,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PRKDC,TEK 19
kinase-selectivity-class AXL,BRAF,CDK9,EPHB4,GRK2,MAP2K6,MAP3K14,MAPK7,PRKDC,STK33,SYK,TEK,ZAP70 13
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.238 Moderate 0.68
mh-clint Mouse hepatocyte intrinsic clearance 1.600 Moderate 0.68
mppb Mouse plasma protein binding (% unbound) 82.050 Moderate 0.68
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.356 Moderate 0.68
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 74.560 % Moderate 0.68
rh-clint Rat hepatocyte intrinsic clearance 1.652 uL/min/10^6 cells Moderate 0.68
rh-fuinc Rat hepatocyte fraction unbound in incubation 95.970 % Moderate 0.68
rppb Rat plasma protein binding (% unbound) 75.590 % Moderate 0.68
solubility-dd Solubility at pH 7.4 in DMSO 926.830 uM Moderate 0.68

Approvals:

DateAgencyCompanyOrphan
Feb. 25, 2015 FDA CEREXA INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug resistance 59.13 56.17 18 484 56356 110532441

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
FDA MoA N0000000202 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 EPC N0000175930 beta Lactamase Inhibitor
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:35625 EC 3.5.2.6 (β-lactamase) inhibitor
CHEBI has role CHEBI:36047 antibacterial drug

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

DiseaseRelationSNOMED_IDDOID
Pyelonephritis indication 45816000 DOID:11400
Infectious disease of abdomen indication 128070006
Bacterial urinary infection indication 312124009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.64 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.5GM BASE;2GM/VIAL AVYCAZ ABBVIE N206494 Feb. 25, 2015 RX POWDER INTRAVENOUS 7112592 Jan. 7, 2026 A METHOD OF TREATING BACTERIAL INFECTIONS IN COMPLICATED INTRA-ABDOMINAL INFECTION AND COMPLICATED URINARY TRACT INFECTION, INCLUDING PYELONEPHRITIS, PATIENTS COMPRISING ADMINISTERING A BACTERICIDALLY EFFECTIVE AMOUNT OF AVIBACTAM SODIUM
EQ 0.5GM BASE;2GM/VIAL AVYCAZ ABBVIE N206494 Feb. 25, 2015 RX POWDER INTRAVENOUS 7112592 Jan. 7, 2026 A METHOD OF TREATING BACTERIAL INFECTIONS IN HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP) PATIENTS COMPRISING ADMINISTERING A BACTERICIDALLY EFFECTIVE AMOUNT OF AVIBACTAM SODIUM
EQ 0.5GM BASE;2GM/VIAL AVYCAZ ABBVIE N206494 Feb. 25, 2015 RX POWDER INTRAVENOUS 7112592 Jan. 7, 2026 METHOD OF TREATING BACTERIAL INFECTIONS
EQ 0.5GM BASE;2GM/VIAL AVYCAZ ABBVIE N206494 Feb. 25, 2015 RX POWDER INTRAVENOUS 7112592 Jan. 7, 2026 TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTIONS, COMPLICATED URINARY TRACT INFECTIONS, AND HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA IN ADULT AND PEDIATRIC PATIENTS (AT LEAST 31 WEEKS GESTATIONAL AGE)
EQ 0.5GM BASE/VIAL;1.5GM/VIAL EMBLAVEO ABBVIE N217906 Feb. 7, 2025 RX POWDER INTRAVENOUS 7112592 Jan. 7, 2026 TREATMENT OF COMPLICATED INTRA-ABDOMINAL BACTERIAL INFECTIONS IN ADULT PATIENTS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.5GM BASE;2GM/VIAL AVYCAZ ABBVIE N206494 Feb. 25, 2015 RX POWDER INTRAVENOUS Jan. 26, 2027 NEW PATIENT POPULATION
EQ 0.5GM BASE/VIAL;1.5GM/VIAL EMBLAVEO ABBVIE N217906 Feb. 7, 2025 RX POWDER INTRAVENOUS Feb. 7, 2028 NEW PRODUCT
EQ 0.5GM BASE/VIAL;1.5GM/VIAL EMBLAVEO ABBVIE N217906 Feb. 7, 2025 RX POWDER INTRAVENOUS Feb. 7, 2033 GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Beta-lactamase Enzyme INHIBITOR Kd 8.16 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Beta-lactamase Enzyme INHIBITOR Kd 6.18 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Beta-lactamase Enzyme INHIBITOR Kd 8.70 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Penicillin-binding protein 2 Enzyme IC50 6.23 CHEMBL
Beta-lactamase TEM Enzyme IC50 8.72 CHEMBL
Beta-lactamase Enzyme Ki 5.77 CHEMBL
Beta-lactamase Enzyme Ki 7.96 CHEMBL
Beta-lactamase OXA-1 Enzyme IC50 6.89 CHEMBL
Carbepenem-hydrolyzing beta-lactamase KPC Enzyme IC50 6.73 CHEMBL

External reference:

IDSource
7352665165 UNII
D10340 KEGG_DRUG
4034342 VUID
N0000191549 NUI
396731-20-7 SECONDARY_CAS_RN
1192491-61-4 SECONDARY_CAS_RN
4034342 VANDF
C3489748 UMLSCUI
FYG PDB_CHEM_ID
CHEMBL1689063 ChEMBL_ID
9835049 PUBCHEM_CID
DB09060 DRUGBANK_ID
CHEMBL2107817 ChEMBL_ID
8972 INN_ID
C543519 MESH_SUPPLEMENTAL_RECORD_UI
10761 IUPHAR_LIGAND_ID
C492231 MESH_SUPPLEMENTAL_RECORD_UI
1603833 RXNORM
30974 MMSL
d08357 MMSL
015925 NDDF
015926 NDDF
1193767002 SNOMEDCT_US
715180004 SNOMEDCT_US
CHEBI:85982 CHEBI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
EMBLAVEO HUMAN PRESCRIPTION DRUG LABEL 2 0074-3878 POWDER, FOR SOLUTION 42.30 mg INTRAVENOUS NDA 28 sections
AVYCAZ HUMAN PRESCRIPTION DRUG LABEL 2 0456-2700 POWDER, FOR SOLUTION 0.50 g INTRAVENOUS NDA 30 sections