U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C22H20N8O5S4
Molecular Weight 604.71
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of CEFTAROLINE

SMILES

CCO/N=C(/c1nc(=N)s[nH]1)\C(=N[C@]2([H])C(=O)N3C(=C(CS[C@]23[H])Sc4nc(cs4)-c5cc[n+](C)cc5)C(=O)[O-])O

InChI

InChIKey=RGFBRLNVZCCMSV-BIRGHMBHSA-N
InChI=1S/C22H20N8O5S4/c1-3-35-27-13(16-26-21(23)39-28-16)17(31)25-14-18(32)30-15(20(33)34)12(9-36-19(14)30)38-22-24-11(8-37-22)10-4-6-29(2)7-5-10/h4-8,14,19H,3,9H2,1-2H3,(H3-,23,25,26,28,31,33,34)/b27-13-/t14-,19-/m1/s1

HIDE SMILES / InChI
Ceftaroline is a fifth-generation broad-spectrum cephalosporin with potent antimicrobial activity against Gram-positive and Gram-negative pathogens. Ceftaroline is the bioactive metabolite of ceftaroline fosamil, an N-phosphonoamino water-soluble cephalosporin prodrug, which is rapidly converted in vivo upon the hydrolysis of the phosphonate group by plasma phosphatises. Ceftaroline fosamil is being developed by Forest Laboratories, under a license from Takeda. In 2010, the U.S. Food and Drug Administration (FDA) approved ceftaroline fosamil for use in the treatment of acute bacterial skin and skin structure infections as well as community-acquired pneumonia. Ceftaroline has bactericidal activity against methicillin-resistant Staphylococcus aureus, therefore serving as an attractive alternative agent for the treatment of methicillin-resistant Staphylococcus aureus bacteremia when approved agents are contraindicated or treatment failures have occurred. Like other β-lactams, ceftaroline’s mechanism of action is mediated by binding to the penicillin-binding protein (PBP), the enzyme mediating the cross-linking transpeptidation of the peptidoglycan which are the terminal steps in completing formation of the bacterial cell wall. MRSA strains have a mutated PBP2a which prohibits β-lactam antibiotics from accessing its active site that mediates the transpeptidation reaction. Ceftaroline possesses an ethoxyimino side-chain mimicking a portion of a cell wall structure, which acts as a “Trojan horse”, allosterically opening and facilitating access to the active site of the PBP2a. Based on clinical trial data to date, ceftaroline appears to be safe and well-tolerated. Since ceftaroline is a cephalosporin, it has caused serious hypersensitivity reactions in patients who are allergic to cephalosporins and among some patients with penicillin allergies.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
TEFLARO

Approved Use

Teflaro is indicated in adult and pediatric patients 2 months of age and older for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Grampositive and Gram-negative microorganisms: Staphylococcus aureus (including methicillin-susceptible and -resistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, and Klebsiella oxytoca. 1.2 Community-Acquired Bacterial Pneumonia Teflaro is indicated in adult and pediatric patients 2 months of age and older for the treatment of community-acquired bacterial pneumonia (CABP) caused by susceptible isolates of the following Grampositive and Gram-negative microorganisms: Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible isolates only), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, and Escherichia coli.

Launch Date

1.28831036E12
Curative
TEFLARO

Approved Use

Teflaro is indicated in adult and pediatric patients 2 months of age and older for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by susceptible isolates of the following Grampositive and Gram-negative microorganisms: Staphylococcus aureus (including methicillin-susceptible and -resistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, and Klebsiella oxytoca. 1.2 Community-Acquired Bacterial Pneumonia Teflaro is indicated in adult and pediatric patients 2 months of age and older for the treatment of community-acquired bacterial pneumonia (CABP) caused by susceptible isolates of the following Grampositive and Gram-negative microorganisms: Streptococcus pneumoniae (including cases with concurrent bacteremia), Staphylococcus aureus (methicillin-susceptible isolates only), Haemophilus influenzae, Klebsiella pneumoniae, Klebsiella oxytoca, and Escherichia coli.

Launch Date

1.28831036E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
22.3 mg/L
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CEFTAROLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
51.9 mg × h/L
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CEFTAROLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.1 h
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CEFTAROLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
20%
600 mg single, intravenous
dose: 600 mg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
CEFTAROLINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Disc. AE: Drug eruption, Cardiac failure...
AEs leading to
discontinuation/dose reduction:
Drug eruption (1%)
Cardiac failure (0.4%)
Nausea (0.4%)
Rash (0.4%)
Generalized rash (0.4%)
Rash maculo-papular (0.4%)
Urticaria (0.4%)
Abdominal infection (0.2%)
Acne (0.2%)
ALT increased (0.2%)
Application site erythema (0.2%)
Ascites (0.2%)
AST increased (0.2%)
Blood alkaline phosphatase increased (0.2%)
Cough (0.2%)
Dermatitis allergic (0.2%)
Diarrhoea (0.2%)
Drug hypersensitivity (0.2%)
Dyspnoea (0.2%)
Oedema generalized (0.2%)
Hepatic enzyme increased (0.2%)
Hyperhidrosis (0.2%)
Hypokalaemia (0.2%)
Necrotizing fasciitis (0.2%)
Osteomyelitis (0.2%)
Osteomyelitis acute (0.2%)
Palpitations (0.2%)
Pleural effusion (0.2%)
Pneumonia (0.2%)
Pyrexia (0.2%)
Rash papular (0.2%)
Rash pruritic (0.2%)
Toxic epidermal necrolysis (0.2%)
Vomiting (0.2%)
Sources: Page: p.1089
2000 mg single, intravenous
Highest studied dose
Dose: 2000 mg
Route: intravenous
Route: single
Dose: 2000 mg
Sources: Page: p.95
unhealthy
n = 236
Health Status: unhealthy
Condition: Bacterial skin and soft tissue infections
Population Size: 236
Sources: Page: p.95
600 mg 2 times / day multiple, intravenous
Recommended
Dose: 600 mg, 2 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.1
unhealthy
n = 1300
Health Status: unhealthy
Condition: Acute bacterial skin and skin structure infections|Community-acquired bacterial pneumonia
Sex: M+F
Population Size: 1300
Sources: Page: p.1
Disc. AE: Hypersensitivity...
AEs leading to
discontinuation/dose reduction:
Hypersensitivity (0.3%)
Sources: Page: p.1
600 mg 2 times / day multiple, intravenous
Recommended
Dose: 600 mg, 2 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.1
unhealthy
Health Status: unhealthy
Condition: Acute bacterial skin and skin structure infections|Community-acquired bacterial pneumonia
Sources: Page: p.1
Disc. AE: Hypersensitivity, Diarrhea, Clostridium difficile...
AEs leading to
discontinuation/dose reduction:
Hypersensitivity (serious)
Diarrhea, Clostridium difficile
Seroconversion test
Sources: Page: p.1
AEs

AEs

AESignificanceDosePopulation
ALT increased 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
AST increased 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Abdominal infection 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Acne 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Application site erythema 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Ascites 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Blood alkaline phosphatase increased 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Cough 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Dermatitis allergic 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Diarrhoea 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Drug hypersensitivity 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Dyspnoea 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Hepatic enzyme increased 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Hyperhidrosis 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Hypokalaemia 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Necrotizing fasciitis 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Oedema generalized 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Osteomyelitis acute 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Osteomyelitis 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Palpitations 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Pleural effusion 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Pneumonia 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Pyrexia 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Rash papular 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Rash pruritic 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Toxic epidermal necrolysis 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Vomiting 0.2%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Cardiac failure 0.4%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Generalized rash 0.4%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Nausea 0.4%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Rash maculo-papular 0.4%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Rash 0.4%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Urticaria 0.4%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Drug eruption 1%
Disc. AE
600 mg 3 times / day multiple, intravenous
Highest studied dose
Dose: 600 mg, 3 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 3 times / day
Sources: Page: p.1089
unhealthy, 52.6 (16.51)
n = 506
Health Status: unhealthy
Condition: Complicated bacterial skin and soft tissue infections
Age Group: 52.6 (16.51)
Sex: M+F
Population Size: 506
Sources: Page: p.1089
Hypersensitivity 0.3%
Disc. AE
600 mg 2 times / day multiple, intravenous
Recommended
Dose: 600 mg, 2 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.1
unhealthy
n = 1300
Health Status: unhealthy
Condition: Acute bacterial skin and skin structure infections|Community-acquired bacterial pneumonia
Sex: M+F
Population Size: 1300
Sources: Page: p.1
Diarrhea, Clostridium difficile Disc. AE
600 mg 2 times / day multiple, intravenous
Recommended
Dose: 600 mg, 2 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.1
unhealthy
Health Status: unhealthy
Condition: Acute bacterial skin and skin structure infections|Community-acquired bacterial pneumonia
Sources: Page: p.1
Seroconversion test Disc. AE
600 mg 2 times / day multiple, intravenous
Recommended
Dose: 600 mg, 2 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.1
unhealthy
Health Status: unhealthy
Condition: Acute bacterial skin and skin structure infections|Community-acquired bacterial pneumonia
Sources: Page: p.1
Hypersensitivity serious
Disc. AE
600 mg 2 times / day multiple, intravenous
Recommended
Dose: 600 mg, 2 times / day
Route: intravenous
Route: multiple
Dose: 600 mg, 2 times / day
Sources: Page: p.1
unhealthy
Health Status: unhealthy
Condition: Acute bacterial skin and skin structure infections|Community-acquired bacterial pneumonia
Sources: Page: p.1
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
Tox targets
PubMed

PubMed

TitleDatePubMed
Pharmacodynamics of ceftaroline against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
2013 Jun
Patents

Sample Use Guides

Adult patients > 18 years of age: 600 mg every 12 hours by IV infusion administered over 5 to 60 min (2.1)  Pediatric patients from 2 years to < 18 years of age weighing ≤ 33 kg: 12 mg/kg every 8 hours by IV infusion administered over 5 to 60 min. Pediatric patients from 2 years to < 18 years of age weighing > 33 kg: 400 mg every 8 hours or 600 mg every 12 hours by IV infusion administered over 5 to 60 min. (2.2)  Pediatric patients from 2 months to < 2 years of age: 8 mg/kg every 8 hours by IV infusion administered over 5 to 60 min (2.2)  Dosage adjustment is required in adult patients with creatinine clearance (CrCl) < 50 mL/min and in End-stage Renal Disease (ESRD) including hemodialysis (2.3)
Route of Administration: Intravenous
Ceftaroline was very active overall against 799 S. pneumoniae (MIC(50/90,) ≤ 0.008/0.12 ug/mL) and inhibited 100.0% of all isolates at a MIC ≤ 0.5 ug/mL. Ceftaroline was very potent against penicillin-resistant (CLSI oral penicillin V breakpoints) and -intermediate S. pneumoniae (MIC(50/90), 0.12/0.25 and 0.03/0.12 ug/mL, respectively), but potency was lower than observed against penicillin-susceptible isolates (MIC(50/90), ≤ 0.008/≤ 0.008 ug/mL). Ceftaroline was also very active (MIC(50/90), ≤ 0.008/0.015 ug/mL) against 515 Haemophilus influenzae, including β-lactamase-producing strains (MIC(50/90), 0.015/0.06 ug/mL). Ceftaroline also demonstrated good activity against 205 Moraxella catarrhalis isolates (MIC(50/90), 0.06/0.12 ug/mL).
Name Type Language
CEFTAROLINE
MI   VANDF   WHO-DD  
Common Name English
CEFTAROLINE [MI]
Common Name English
CEFTAROLINE [WHO-DD]
Common Name English
T-91825
Code English
CEFTAROLINE [VANDF]
Common Name English
PYRIDINIUM, 4-(2-(((6R,7R)-7-(((2Z)-2-(5-AMINO-1,2,4-THIADIAZOL-3-YL)-2-(ETHOXYIMINO)-1-OXOETHYL)AMINO)-2-CARBOXY-8-OXO-5-THIA-1-AZABICYCLO(4.2.0)OCT-2-EN-3-YL)THIO)-4-THIAZOLYL)-1-METHYL-, INNER SALT
Common Name English
T 91825
Code English
Classification Tree Code System Code
LIVERTOX 170
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
NDF-RT N0000175488
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
Code System Code Type Description
MERCK INDEX
M3217
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY Merck Index
EVMPD
SUB31649
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
PUBCHEM
9938701
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
CAS
189345-04-8
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
EPA CompTox
189345-04-8
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
MESH
C490727
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
LACTMED
Ceftaroline
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
RXCUI
1040005
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY RxNorm
WIKIPEDIA
Ceftaroline
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY
FDA UNII
H36Z0FHR8K
Created by admin on Sat Jun 26 04:15:25 UTC 2021 , Edited by admin on Sat Jun 26 04:15:25 UTC 2021
PRIMARY