relebactam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-lactamase inhibitors | 5342 | 1174018-99-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
RECARBRIO is a combination of imipenem/cilastatin and relebactam. Imipenem is a penem antibacterial drug, cilastatin sodium is a renal dehydropeptidase inhibitor, and relebactam is a beta lactamase inhibitor. Cilastatin limits the renal metabolism of imipenem and does not have antibacterial activity. The bactericidal activity of imipenem results from binding to PBP 2 and PBP 1B in Enterobacteriaceae and Pseudomonas aeruginosa and the subsequent inhibition of penicillin binding proteins (PBPs). Inhibition of PBPs leads to the disruption of bacterial cell wall synthesis. Imipenem is stable in the presence of some beta lactamases. Relebactam has no intrinsic antibacterial activity. Relebactam protects imipenem from degradation by certain serine beta lactamases such as Sulhydryl Variable (SHV), Temoneira (TEM), Cefotaximase-Munich 13 Reference ID: 4462927 (CTX-M), Enterobacter cloacae P99 (P99), Pseudomonas-derived cephalosporinase (PDC), and Klebsiella-pneumoniae carbapenemase (KPC)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 70 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 16, 2019 | FDA | MSD MERCK CO | |
| June 23, 2021 | PMDA | MSD K.K. |
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 | J01DH56 | 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 |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Infection caused by Pseudomonas aeruginosa strain resistant to carbapenem antimicrobial drugs | indication | 11218009 | |
| Pyelonephritis | indication | 45816000 | DOID:11400 |
| Urinary tract infectious disease | indication | 68566005 | |
| Infection caused by Escherichia coli strain resistant to carbapenem antimicrobial drugs | indication | 71057007 | |
| Infection caused by Serratia spp resistant to carbapenem antimicrobial drugs | indication | 71120004 | |
| Intestinal infection due to Pseudomonas | indication | 82930004 | |
| Intestinal infection due to E. coli | indication | 111839008 | |
| Infectious disease of abdomen | indication | 128070006 | |
| Pseudomonas gastrointestinal tract infection | indication | 266078006 | |
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Pseudomonas urinary tract infection | indication | 301013004 | |
| Infection caused by Enterococcus spp resistant to carbapenem antimicrobial drugs | indication | 406574007 | |
| Gastrointestinal infection caused by Klebsiella aerogenes | indication | 421429008 | |
| Infection caused by Klebsiella spp resistant to carbapenem antimicrobial drugs | indication | 721756002 | |
| Infection caused by Acinetobacter spp resistant to carbapenem antimicrobial drugs | indication | 840588006 | |
| Infection caused by Citrobacter spp resistant to carbapenem antimicrobial drugs | indication | 1137353009 | |
| Urinary tract infection caused by Klebsiella | indication | ||
| Complicated Genitourinary Tract Infection | 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 | 13.53 | acidic |
| pKa2 | 9.75 | Basic |
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;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | 8487093 | Nov. 19, 2029 | TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTIONS (CIAI) |
| EQ 500MG BASE/VIAL;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | 8487093 | Nov. 19, 2029 | TREATMENT OF COMPLICATED URINARY TRACT INFECTIONS, INCLUDING PYELONEPHRITIS (CUTI) |
| EQ 500MG BASE/VIAL;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | 8487093 | Nov. 19, 2029 | 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;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | July 16, 2024 | NEW CHEMICAL ENTITY |
| EQ 500MG BASE/VIAL;500MG/VIAL;250MG/VIAL | RECARBRIO | MSD MERCK CO | N212819 | July 16, 2019 | RX | POWDER | INTRAVENOUS | July 16, 2029 | 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 | IC50 | 6.40 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | INHIBITOR | IC50 | 6.33 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | INHIBITOR | IC50 | 6.64 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | INHIBITOR | IC50 | 6.59 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | INHIBITOR | IC50 | 6.04 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-lactamase | Enzyme | IC50 | 6.33 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| Y1MYA2UHFL | UNII |
| C4317244 | UMLSCUI |
| CHEMBL3301605 | ChEMBL_ID |
| CHEMBL3112741 | ChEMBL_ID |
| 44129647 | PUBCHEM_CID |
| DB12377 | DRUGBANK_ID |
| D11621 | KEGG_DRUG |
| C000633884 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10852 | IUPHAR_LIGAND_ID |
| 018062 | NDDF |
| 789066008 | SNOMEDCT_US |
| 4039070 | VANDF |
| 1174020-13-3 | SECONDARY_CAS_RN |
| 2184137 | RXNORM |
| 321713 | MMSL |
| 37333 | MMSL |
| d09357 | MMSL |
| C568736 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
None