vaborbactam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
beta-lactamase inhibitors 5253 1360457-46-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • RPX-7009
  • vaborbactam
  • RPX7009
  • RPX 7009
Vaborbactam is a non-suicidal beta-lactamase inhibitor that protects meropenem from degradation by certain serine beta-lactamases such as Klebsiella pneumoniae carbapenemase (KPC). Vaborbactam does not have any antibacterial activity. Vaborbactam does not decrease the activity of meropenem against meropenem-susceptible organisms.
  • Molecular weight: 297.13
  • Formula: C12H16BNO5S
  • CLOGP: 0.52
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 3
  • TPSA: 95.86
  • ALOGS: -3.28
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
3 g P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.29 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.94 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.67 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.34 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 29, 2017 FDA REMPEX PHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC J01DH52 ANTIINFECTIVES FOR SYSTEMIC USE
ANTIBACTERIALS FOR SYSTEMIC USE
OTHER BETA-LACTAM ANTIBACTERIALS
Carbapenems
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
Escherichia coli urinary tract infection indication 301011002
Urinary tract infection caused by Klebsiella indication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.76 acidic
pKa2 9.79 acidic
pKa3 13.85 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1GM/VIAL;1GM/VIAL VABOMERE REMPEX N209776 Aug. 29, 2017 RX POWDER INTRAVENOUS 10183034 Aug. 8, 2031 TREATMENT OF COMPLICATED URINARY TRACT INFECTION (CUTI) INCLUDING PYELONEPHRITIS CAUSED BY THE FOLLOWING SUSCEPTIBLE MICROORGANISMS: ESCHERICHIA COLI, KLEBSIELLA PNEUMONIA, AND ENTEROBACTER CLOACAE SPECIES COMPLEX
1GM/VIAL;1GM/VIAL VABOMERE REMPEX N209776 Aug. 29, 2017 RX POWDER INTRAVENOUS 10561675 Aug. 8, 2031 TREATMENT OF COMPLICATED URINARY TRACT INFECTION (CUTI) INCLUDING PYELONEPHRITIS CAUSED BY THE FOLLOWING SUSCEPTIBLE MICROORGANISMS: ESCHERICHIA COLI, KLEBSIELLA PNEUMONIA, AND ENTEROBACTER CLOACAE SPECIES COMPLEX
1GM/VIAL;1GM/VIAL VABOMERE REMPEX N209776 Aug. 29, 2017 RX POWDER INTRAVENOUS 11007206 Aug. 8, 2031 TREATMENT OF COMPLICATED URINARY TRACT INFECTIONS (CUTI) INCLUDING PYELONEPHRITIS CAUSED BY THE FOLLOWING SUSCEPTIBLE MICROORGANISMS: ESCHERICHIA COLI, KLEBSIELLA PNEUMONIA, ENTEROBACTER CLOACAE SPECIES COMPLEX WITH MEROPENEM & VABORBACTAM AS SPECIFIED
1GM/VIAL;1GM/VIAL VABOMERE REMPEX N209776 Aug. 29, 2017 RX POWDER INTRAVENOUS 9694025 Aug. 8, 2031 TREATMENT OF PATIENTS 18 YEARS OF AGE AND OLDER WITH COMPLICATED URINARY TRACT INFECTIONS CAUSED BY SUSCEPTIBLE MICROORGANISMS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1GM/VIAL;1GM/VIAL VABOMERE REMPEX N209776 Aug. 29, 2017 RX POWDER INTRAVENOUS Aug. 29, 2022 NEW CHEMICAL ENTITY
1GM/VIAL;1GM/VIAL VABOMERE REMPEX N209776 Aug. 29, 2017 RX POWDER INTRAVENOUS Aug. 29, 2027 GENERATING ANTIBIOTIC INCENTIVES NOW

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-lactamase Enzyme Ki 7.25 CHEMBL

External reference:

IDSource
1C75676F8V UNII
4036930 VANDF
C4519317 UMLSCUI
4D6 PDB_CHEM_ID
CHEMBL3317857 ChEMBL_ID
56649692 PUBCHEM_CID
DB12107 DRUGBANK_ID
D10998 KEGG_DRUG
C000626994 MESH_SUPPLEMENTAL_RECORD_UI
C000599945 MESH_SUPPLEMENTAL_RECORD_UI
10871 IUPHAR_LIGAND_ID
10182 INN_ID
1945213 RXNORM
33058 MMSL
d08644 MMSL
017323 NDDF
737669009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VABOMERE HUMAN PRESCRIPTION DRUG LABEL 2 70842-120 INJECTION, POWDER, FOR SOLUTION 1 g INTRAVENOUS NDA 28 sections