Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H21N8O8PS4.C2H4O2.H2O |
Molecular Weight | 762.752 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.CC(O)=O.[H][C@]12SCC(SC3=NC(=CS3)C4=CC=[N+](C)C=C4)=C(N1C(=O)[C@H]2NC(=O)C(=N/OCC)\C5=NSC(NP(O)([O-])=O)=N5)C(O)=O
InChI
InChIKey=KRWPPVCZNGQQHZ-IINIBMQSSA-N
InChI=1S/C22H21N8O8PS4.C2H4O2.H2O/c1-3-38-26-13(16-25-21(43-28-16)27-39(35,36)37)17(31)24-14-18(32)30-15(20(33)34)12(9-40-19(14)30)42-22-23-11(8-41-22)10-4-6-29(2)7-5-10;1-2(3)4;/h4-8,14,19H,3,9H2,1-2H3,(H4-,24,25,27,28,31,33,34,35,36,37);1H3,(H,3,4);1H2/b26-13-;;/t14-,19-;;/m1../s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19441869 | https://www.ncbi.nlm.nih.gov/pubmed/28702467 | https://www.ncbi.nlm.nih.gov/pubmed/28179245 | https://www.ncbi.nlm.nih.gov/pubmed/30897759https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000Lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/25347329 | https://www.teflaro.com/ | https://www.ncbi.nlm.nih.gov/pubmed/21482565
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19441869 | https://www.ncbi.nlm.nih.gov/pubmed/28702467 | https://www.ncbi.nlm.nih.gov/pubmed/28179245 | https://www.ncbi.nlm.nih.gov/pubmed/30897759https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000Lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/25347329 | https://www.teflaro.com/ | https://www.ncbi.nlm.nih.gov/pubmed/21482565
Ceftaroline fosamil is a 5th generation cephalosporin with an in vitro spectrum of activity including Streptococcus agalactiae, penicillin- and cephalosporin-resistant S. pneumoniae, S. pyogenes, methicillin-susceptible S. aureus and methicillin-resistant S. aureus, Haemophilus influenzae, Klebsiella oxytoca, K. pneumoniae and Moraxella catarrhalis. Ceftaroline fosamil (TAK-599 or PPI-0903), the prodrug of the active metabolite, ceftaroline, was synthesized by Takeda Pharmaceutical Co., Ltd and developed by Cerexa, Inc. and Forest Laboratories, Inc. It is currently approved by the FDA for the treatment of acute bacterial skin and skin structure infections (ABSSSI) and community-acquired bacterial pneumonia (CABP) in adults. Ceftaroline fosamil is marketed under the brand name TEFLARO®, 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 Gram-positive and Gram-negative microorganisms: Staphylococcus aureus (including methicillin-susceptible and ‑resistant isolates), Streptococcus pyogenes, Streptococcus agalactiae, Escherichia coli, Klebsiella pneumoniae, and Klebsiella oxytoca. TEFLARO is also 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 Gram-positive 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. Ceftaroline provides in vitro bactericidal activity against methicillin-, vancomycin-, daptomycin-, and linezolid-resistant Gram-positive organisms and select Gram-negative pathogens. The pharmacodynamics of ceftaroline is similar to other β-lactam agents. Ceftaroline exhibits a favorable adverse effect profile and is generally well tolerated. The bactericidal action of ceftaroline is mediated through binding to essential penicillin-binding
proteins (PBPs). Ceftaroline is bactericidal against S. aureus due to its affinity for PBP2a and against
Streptococcus pneumoniae due to its affinity for PBP2x.
Originator
Sources: http://adisinsight.springer.com/drugs/800018104 | https://www.ncbi.nlm.nih.gov/pubmed/21482565
Curator's Comment: # Takeda
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3512 |
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Target ID: CHEMBL1255141 |
|||
Target ID: CHEMBL6188 |
|||
Target ID: CHEMBL2565 |
|||
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | TEFLARO Approved UseTeflaro 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 Date2010 |
|||
Curative | TEFLARO Approved UseTeflaro 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 Date2010 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
22.3 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27044549/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
51.9 mg × h/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27044549/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27044549/ |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
20% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27044549/ |
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
Dose | Population | Adverse 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%) Sources: Page: p.1089Cardiac 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%) |
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) Sources: Page: p.1Diarrhea, Clostridium difficile Seroconversion test |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: (ClinPharm) 11, 58-59, 188-196 |
no | |||
Page: (ClinPharm) 11, 58-59, 188-196 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000ClinPharmR.pdf#page=81 Page: (ClinPharm) 79-81 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000ClinPharmR.pdf#page=81 Page: (ClinPharm) 79-81 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000ClinPharmR.pdf#page=81 Page: (ClinPharm) 79-81 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000ClinPharmR.pdf#page=81 Page: (ClinPharm) 79-81 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000ClinPharmR.pdf#page=81 Page: (ClinPharm) 79-81 |
no | |||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2010/200327Orig1s000ClinPharmR.pdf#page=81 Page: (ClinPharm) 79-81 |
no | |||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely |
Drug as victim
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://www.allergan.com/assets/pdf/teflaro_pi
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23146404
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).
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C357
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P9VXV1408Y
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DTXSID10193134
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1743286
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CHEMBL501122
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1210978-33-8
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100000155873
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1134503-56-2
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C96703
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400827-55-6
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SUB129872
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DBSALT001808
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m3217
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16007393
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1442644-01-0
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866021-48-9
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ACTIVE MOIETY
SUBSTANCE RECORD