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vaborbactam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-lactamase inhibitors | 5253 | 1360457-46-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
| S (Water solubility) | 5.26 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.556 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.841 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.514 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.304 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 61.860 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 57.260 | % | High | 1 |
| herg | hERG pIC50 | 4.347 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.811 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.289 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 54.930 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1 | 40 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,EIF2AK3,GRK2,MAP2K6,PRKDC,STK33,TEK,TGFBR1 | 11 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.705 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 2.606 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 77.090 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.796 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 64.270 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 1.233 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 85.570 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 57.770 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 914.113 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 29, 2017 | FDA | REMPEX PHARMS 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:
| Source | Code | Description |
|---|---|---|
| ATC | J01DH52 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Carbapenems |
| 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:33282 | antibacterial agent |
| CHEBI has role | CHEBI:35441 | antiinfective agent |
Related Drugs by ATC class:
J01DH Carbapenems 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Urinary tract infection caused by Klebsiella | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.76 | acidic |
| pKa2 | 9.79 | acidic |
| pKa3 | 13.85 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 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 |
| 1GM/VIAL;1GM/VIAL | VABOMERE | REMPEX | N209776 | Aug. 29, 2017 | RX | POWDER | INTRAVENOUS | 12478606 | Jan. 8, 2038 | 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 | 11376237 | April 6, 2039 | 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 | 12533342 | April 6, 2039 | 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 |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Beta-lactamase | Enzyme | Ki | 7.25 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 1C75676F8V | UNII |
| 4036930 | VANDF |
| C4519317 | UMLSCUI |
| CHEBI:755318 | CHEBI |
| 4D6 | PDB_CHEM_ID |
| CHEMBL3317857 | ChEMBL_ID |
| 56649692 | PUBCHEM_CID |
| DB12107 | DRUGBANK_ID |
| D10998 | KEGG_DRUG |
| 10182 | INN_ID |
| C000626994 | MESH_SUPPLEMENTAL_RECORD_UI |
| C000599945 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10871 | IUPHAR_LIGAND_ID |
| 737669009 | SNOMEDCT_US |
| 33058 | MMSL |
| d08644 | MMSL |
| 017323 | NDDF |
| 1945213 | RXNORM |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| VABOMERE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 70842-120 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | NDA | 29 sections |