Compound Detail
CHEMBL186
CEFEPIME 💊 Approved Drug
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💊 Approved Drug
CO/N=C(\C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[N+]3(C)CCCC3)CS[C@H]12)c1csc(N)n1
Basic Information
| ChEMBL ID | CHEMBL186 |
| Name | CEFEPIME |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | HVFLCNVBZFFHBT-ZKDACBOMSA-N |
| Therapeutic | ✓ Yes |
0
Targets
4
Activities
2
Assay Types
22
PK Parameters
20
Publications
6
Known Names
10
Indications
Molecular Properties
480.6
MW (Da)
-1.28
ALogP
10
HBA
2
HBD
150.0
PSA (Ų)
0.21
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1996 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Bacterial Infections Enterobacteriaceae Infections Pneumonia, Ventilator-Associated Pyelonephritis Shock, Septic Urinary Tract Infections Communicable Diseases Hematologic Neoplasms Kidney Diseases Osteomyelitis
ATC Classification
J01DE01
cefepime
Level 1: ANTIINFECTIVES FOR SYSTEMIC USE
Level 2: ANTIBACTERIALS FOR SYSTEMIC USE
Activity Summary
Ki 3 meas.
IC50 1 meas.
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 15800.0 | ng.hr.mL-1 | Mus musculus |
| CL | 2.2 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.2 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.6 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1.8 | mL.min-1.kg-1 | Macaca |
| CL | 2.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 2.2 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 2.2 | mL.min-1.kg-1 | Homo sapiens |
| CL | 11.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 7.6 | L/hr | Homo sapiens |
| CL | 6.0 | L/hr | Homo sapiens |
| CL | 10.8 | mL.min-1.kg-1 | Mus musculus |
| Fu | 0.78 | - | Homo sapiens |
| Fu | 0.78 | - | Homo sapiens |
| MRT | 2.1 | hr | Homo sapiens |
| T1/2 | 0.15 | hr | Mus musculus |
| T1/2 | 1.9 | hr | Homo sapiens |
| T1/2 | 0.39 | hr | Mus musculus |
| T1/2 | 2.0 | hr | Homo sapiens |
| Tmax | 0.125 | hr | Mus musculus |
| Vd | 0.206 | L.kg-1 | Homo sapiens |
| Vd | 23.0 | l | Homo sapiens |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 17261619 | 10.1128/aac.01278-06 | Pseudomonas aeruginosa | 100 |
| 19738025 | 10.1128/aac.00574-09 | Pseudomonas aeruginosa | 64 |
| 17591851 | 10.1128/aac.00218-07 | Beta-lactamase | 60 |
| 29336873 | 10.1016/j.bmcl.2018.01.006 | Escherichia coli | 45 |
| 19258272 | 10.1128/aac.01410-08 | Pseudomonas aeruginosa | 43 |
| 19805565 | 10.1128/aac.01099-09 | Klebsiella pneumoniae | 40 |
| 18591275 | 10.1128/aac.01684-07 | Acinetobacter baumannii | 40 |
| 18779357 | 10.1128/aac.00381-08 | Pseudomonas aeruginosa | 36 |
| 20606064 | 10.1128/aac.00060-10 | Pseudomonas aeruginosa | 35 |
| 19188376 | 10.1128/aac.01264-08 | Pseudomonas aeruginosa | 33 |
| 19164140 | 10.1128/aac.00822-08 | Klebsiella aerogenes | 31 |
| 19258280 | 10.1128/aac.01024-08 | Pseudomonas aeruginosa | 31 |
| 19001116 | 10.1128/aac.00746-08 | Klebsiella pneumoniae | 30 |
| 18809945 | 10.1128/aac.00707-08 | Pseudomonas aeruginosa | 28 |
| 17846127 | 10.1128/aac.01259-06 | Acinetobacter baumannii | 26 |
| 18443114 | 10.1128/aac.01658-07 | Escherichia coli | 26 |
| 20660683 | 10.1128/aac.01301-09 | Klebsiella pneumoniae | 26 |
| 17724156 | 10.1128/aac.01512-06 | Acinetobacter baumannii | 24 |
| 18725443 | 10.1128/aac.00712-08 | Streptococcus pneumoniae | 24 |
| 19433554 | 10.1128/aac.00018-09 | Pseudomonas aeruginosa | 22 |
Data from ChEMBL 36 via Core Engine