avibactam Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-lactamase inhibitors | 4946 | 1192500-31-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a non-beta-lactam beta-lactamase inhibitor that inactivates some beta-lactamases and protects ceftazidime from degradation by certain beta-lactamases
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 25, 2015 | FDA | CEREXA INC |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Off label use | 60.08 | 55.39 | 37 | 337 | 379804 | 46305884 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Pathogen resistance | 160.71 | 71.43 | 38 | 710 | 8372 | 29943358 |
| Drug resistance | 89.65 | 71.43 | 29 | 719 | 20104 | 29931626 |
| Septic shock | 81.92 | 71.43 | 37 | 711 | 63570 | 29888160 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA MoA | N0000000202 | beta Lactamase Inhibitors |
| MeSH PA | D000900 | Anti-Bacterial Agents |
| MeSH PA | D000890 | Anti-Infective Agents |
| MeSH PA | D065093 | beta-Lactamase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| FDA EPC | N0000175930 | beta Lactamase Inhibitor |
| CHEBI has role | CHEBI:33281 | antibiotics |
| CHEBI has role | CHEBI:35625 | beta-lactamase inhibitors |
| CHEBI has role | CHEBI:36047 | antibacterial drugs |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pyelonephritis | indication | 45816000 | DOID:11400 |
| Infectious disease of abdomen | indication | 128070006 | |
| Bacterial urinary infection | indication | 312124009 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.64 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 0.5GM BASE;2GM/VIAL | AVYCAZ | ALLERGAN | N206494 | Feb. 25, 2015 | RX | POWDER | INTRAVENOUS | Feb. 25, 2020 | NEW CHEMICAL ENTITY |
| EQ 0.5GM BASE;2GM/VIAL | AVYCAZ | ALLERGAN | N206494 | Feb. 25, 2015 | RX | POWDER | INTRAVENOUS | Feb. 25, 2025 | 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 | INHIBITOR | Kd | 8.15 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | INHIBITOR | Kd | 8.70 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | INHIBITOR | Kd | 6.18 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| 7352665165 | UNII |
| D10340 | KEGG_DRUG |
| 4034342 | VUID |
| N0000191549 | NUI |
| 1192491-61-4 | SECONDARY_CAS_RN |
| 4034342 | VANDF |
| C1527648 | UMLSCUI |
| CHEBI:85984 | CHEBI |
| FYG | PDB_CHEM_ID |
| CHEMBL1689063 | ChEMBL_ID |
| CHEMBL2107817 | ChEMBL_ID |
| DB09060 | DRUGBANK_ID |
| 9835049 | PUBCHEM_CID |
| 8972 | INN_ID |
| C543519 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10761 | IUPHAR_LIGAND_ID |
| 1603833 | RXNORM |
| 30974 | MMSL |
| d08357 | MMSL |
| 015925 | NDDF |
| 015926 | NDDF |
| 715180004 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| AVYCAZ | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0456-2700 | POWDER, FOR SOLUTION | 0.50 g | INTRAVENOUS | NDA | 28 sections |