cefiderocol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antibiotics, cefalosporanic acid derivatives | 5352 | 1225208-94-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Cefiderocol is a cephalosporin antibacterial with activity against Gram-negative aerobic bacteria. Cefiderocol functions as a siderophore and binds to extracellular free ferric iron. In addition to passive diffusion via porin channels, cefiderocol is actively transported across the outer cell membrane of bacteria into the periplasmic space using a siderophore iron uptake mechanism. Cefiderocol exerts bactericidal action by inhibiting cell wall biosynthesis through binding to penicillin-binding proteins (PBPs)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 100 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 |
|---|---|---|---|
| April 23, 2020 | EMA | Shionogi B.V. | |
| Nov. 14, 2019 | FDA | SHIONOGI 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 | J01DI04 | ANTIINFECTIVES FOR SYSTEMIC USE ANTIBACTERIALS FOR SYSTEMIC USE OTHER BETA-LACTAM ANTIBACTERIALS Other cephalosporins and penems |
| FDA CS | M0003827 | Cephalosporins |
| FDA EPC | N0000175488 | Cephalosporin Antibacterial |
| CHEBI has role | CHEBI:26672 | siderochromes |
| CHEBI has role | CHEBI:36047 | antibacterial drugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Pyelonephritis | indication | 45816000 | DOID:11400 |
| Urinary tract infectious disease | indication | 68566005 | |
| Escherichia coli urinary tract infection | indication | 301011002 | |
| Proteus urinary tract infection | indication | 301012009 | |
| Pseudomonas urinary tract infection | indication | 301013004 | |
| Bacterial urinary infection | indication | 312124009 | |
| Gram-Negative Bacterial Infections | indication | 371583007 | |
| 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 | 2.35 | acidic |
| pKa2 | 3.44 | acidic |
| pKa3 | 6.17 | acidic |
| pKa4 | 9.6 | acidic |
| pKa5 | 13.61 | acidic |
| pKa6 | 2.83 | 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 1GM BASE/VIAL | FETROJA | SHIONOGI INC | N209445 | Nov. 14, 2019 | RX | POWDER | INTRAVENOUS | 9238657 | Nov. 14, 2033 | METHOD OF TREATING BACTERIAL INFECTIONS |
| EQ 1GM BASE/VIAL | FETROJA | SHIONOGI INC | N209445 | Nov. 14, 2019 | RX | POWDER | INTRAVENOUS | 9238657 | Nov. 14, 2033 | METHOD OF TREATING COMPLICATED URINARY TRACT INFECTIONS (CUTI), INCLUDING PYELONEPHRITIS, COMPRISING ADMINISTERING CEFIDEROCOL SULFATE TOSYLATE |
| EQ 1GM BASE/VIAL | FETROJA | SHIONOGI INC | N209445 | Nov. 14, 2019 | RX | POWDER | INTRAVENOUS | 9238657 | Nov. 14, 2033 | METHOD OF TREATING HOSPITAL-ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP) COMPRISING ADMINISTERING CEFIDEROCOL SULFATE TOSYLATE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 1GM BASE/VIAL | FETROJA | SHIONOGI INC | N209445 | Nov. 14, 2019 | RX | POWDER | INTRAVENOUS | Sept. 25, 2023 | INDICATED IN PATIENTS 18 YEARS OF AGE AND OLDER FOR THE TREATMENT OF HOSPITAL ACQUIRED BACTERIAL PNEUMONIA AND VENTILATOR-ASSOCIATED BACTERIAL PNEUMONIA (HABP/VABP) CAUSED BY THE FOLLOWING SUSCEPTIBLE GRAM-NEGATIVE MICROORGANISMS: ACINETOBACTER BAUMANNII COMPLEX, ESCHERICHIA COLI, ENTEROBACTER CLOACAE COMPLEX, KLEBSIELLA PNEUMONIAE, PSEUDOMONAS AERUGINOSA, AND SERRATIA MARCESCENS |
| EQ 1GM BASE/VIAL | FETROJA | SHIONOGI INC | N209445 | Nov. 14, 2019 | RX | POWDER | INTRAVENOUS | Nov. 14, 2024 | NEW CHEMICAL ENTITY |
| EQ 1GM BASE/VIAL | FETROJA | SHIONOGI INC | N209445 | Nov. 14, 2019 | RX | POWDER | INTRAVENOUS | Nov. 14, 2029 | GENERATING ANTIBIOTIC INCENTIVES NOW |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Peptidoglycan synthase FtsI | Enzyme | INHIBITOR | IC50 | 7.40 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Penicillin-binding protein 1A | Enzyme | INHIBITOR | IC50 | 6.07 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Penicillin-binding protein 1A | Enzyme | INHIBITOR | IC50 | 5.48 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Penicillin-binding protein 1B | Enzyme | INHIBITOR | IC50 | 5.47 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Penicillin-binding protein 1A | Enzyme | INHIBITOR | IC50 | 5.98 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Penicillin-binding protein 1B | Enzyme | INHIBITOR | IC50 | 5.46 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Peptidoglycan D,D-transpeptidase MrdA | Enzyme | INHIBITOR | IC50 | 5.66 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Peptidoglycan D,D-transpeptidase MrdA | Enzyme | INHIBITOR | IC50 | 7.20 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Peptidoglycan D,D-transpeptidase FtsI | Enzyme | INHIBITOR | IC50 | 7.21 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Peptidoglycan D,D-transpeptidase FtsI | Enzyme | INHIBITOR | IC50 | 7.22 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Peptidoglycan D,D-transpeptidase FtsI | Enzyme | INHIBITOR | IC50 | 6.17 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Penicillin-binding protein 4 | Enzyme | INHIBITOR | IC50 | 5.44 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| SZ34OMG6E8 | UNII |
| 2135543-94-9 | SECONDARY_CAS_RN |
| C4548369 | UMLSCUI |
| CHEBI:140376 | CHEBI |
| CHEMBL3989974 | ChEMBL_ID |
| 77843966 | PUBCHEM_CID |
| DB14879 | DRUGBANK_ID |
| CHEMBL4297211 | ChEMBL_ID |
| D11302 | KEGG_DRUG |
| 10234 | INN_ID |
| 10776 | IUPHAR_LIGAND_ID |
| 018219 | NDDF |
| 018220 | NDDF |
| 1217151007 | SNOMEDCT_US |
| 830101009 | SNOMEDCT_US |
| 830161006 | SNOMEDCT_US |
| 4039174 | VANDF |
| 2265702 | RXNORM |
| 37832 | MMSL |
| d09462 | MMSL |
| C000612166 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Fetroja | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59630-266 | INJECTION, POWDER, FOR SOLUTION | 1 g | INTRAVENOUS | NDA | 31 sections |