relebactam 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:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 16, 2019 | FDA | MSD MERCK CO |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
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 (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pyelonephritis | indication | 45816000 | DOID:11400 |
| Urinary tract infectious disease | indication | 68566005 | |
| 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 | |
| Gastrointestinal infection caused by Klebsiella aerogenes | indication | 421429008 | |
| Complicated Genitourinary Tract Infection | indication | ||
| Urinary tract infection caused by Klebsiella | indication |
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)
None
Orange Book exclusivity data (new drug applications)
None
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 |
External reference:
| ID | Source |
|---|---|
| 1174020-13-3 | SECONDARY_CAS_RN |
| 4039070 | VANDF |
| C5196210 | UMLSCUI |
| CHEMBL3301605 | ChEMBL_ID |
| CHEMBL3112741 | ChEMBL_ID |
| D11621 | KEGG_DRUG |
| DB12377 | DRUGBANK_ID |
| 10852 | IUPHAR_LIGAND_ID |
| C000633884 | MESH_SUPPLEMENTAL_RECORD_UI |
| C568736 | MESH_SUPPLEMENTAL_RECORD_UI |
| Y1MYA2UHFL | UNII |
| 44129647 | PUBCHEM_CID |
| 2184137 | RXNORM |
| 321713 | MMSL |
| 37333 | MMSL |
| d09357 | MMSL |
| 018062 | NDDF |
| 789066008 | SNOMEDCT_US |
Pharmaceutical products:
None