General
Preferred name
CEFTAROLINE FOSAMIL
Synonyms
CEFTAROLINE FOSAMIL ACETATE ()
Ceftaroline fosamil anhydrous ()
TAK-599 ()
PPI-0903 ()
TAK 599 ()
Ceftaroline Fosamil ()
Ppi-0903 monoacetate monohydrate ()
Ceftaroine ()
Teflaro ()
Ceftaroline fosamil monoacetate ()
Tak-599 monoacetate monohydrate ()
P&D ID
PD016226
CAS
866021-48-9
402741-13-3
229016-73-3
Tags
available
prodrug
drug
Approved by
FDA
First approval
2010
Drug Status
investigational
approved
Max Phase
Phase 4
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Ceftaroline fosamil is a fifth-generation cephalosporin prodrug which is hydrolysed to the active form, ceftaroline, in vivo. It has anti-MRSA activity . Ceftaroline was removed from the World Health Organization's List of Essential Medicines in 2019.
(GtoPdb)
TOXICITY
LD50/LC50:; Draize test, rabbit, eye: 100 mg/24H Moderate; Oral,; mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat:; LD50 = 980 mg/kg.
PHARMACODYNAMICS
The time that unbound plasma concentration of ceftaroline exceeds the minimum inhibitory concentration (MIC) of the infecting organism has been shown to best correlate with efficacy in a neutropenic murine thigh infection model with S. aureus and S. pneumoniae.; ; No significant effect on QTc (corrected QT interval) interval was detected at peak plasma concentration or at any other time.
DESCRIPTION
Ceftaroline fosamil is a cephalosporin antibacterial indicated for the treatment of adults with acute bacterial skin and soft tissue infections, including those caused by methicillin-resistant Staphylococcus aureus (MRSA).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
8
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
Guide to Pharmacology
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
40
Molecular Weight
684.01
Hydrogen Bond Acceptors
14
Hydrogen Bond Donors
4
Rotatable Bonds
11
Ring Count
5
Aromatic Ring Count
3
cLogP
-0.11
TPSA
223.24
Fraction CSP3
0.27
Chiral centers
2.0
Largest ring
6.0
QED
0.07
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Source data
