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Ceftaroline fosamil

ceftaroline fosamil, ceftaroline fosamil acetate
Ceftaroline fosamil INN /sɛfˈtæroʊliːn/, brand name Teflaro in the US and Zinforo in Europe, is a fifth-generation cephalosporin antibiotic It is active against methicillin-resistant Staphylococcus aureus MRSA and other Gram-positive bacteria It retains some activity of later-generation cephalosporins having broad-spectrum activity against Gram-negative bacteria, but its effectiveness is relatively much weaker It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection

Ceftaroline is being developed by Forest Laboratories, under a license from Takeda Ceftaroline has received approval from the US Food and Drug Administration for the treatment of community-acquired bacterial pneumonia and acute bacterial skin infections on October 29, 2010 In vitro studies show it has a similar spectrum to ceftobiprole, the only other fifth-generation cephalosporin to date, although no head-to-head clinical trials have been conducted Ceftaroline and ceftobiprole are on an unnamed subclass of cephalosporins by the Clinical and Laboratory Standards Institute CLSI


  • 1 Clinical use
  • 2 Safety
  • 3 Contraindications
  • 4 Warnings and precautions
    • 41 Hypersensitivity reactions
    • 42 Clostridium difficile-associated diarrhea
    • 43 Development of drug-resistant bacteria
    • 44 Direct Coombs test seroconversion
    • 45 Interactions
    • 46 Use in specific populations
  • 5 Side effects
  • 6 Chemistry
  • 7 References

Clinical use

Main article: Cephalosporin

Ceftaroline is a novel cephalosporin with activity against MRSA with phase III clinical trials for complicated skin and skin structure infections with reported non-inferior efficacy against MRSA compared to vancomycin and aztreonam In 2009, ceftaroline had completed phase-III clinical trials for community-acquired pneumonia comparing it against ceftriaxone with non-inferior results and similar adverse reaction profile However, only results for phase-II clinical trials in treatment of complicated skin and skin structure infections have been published Sept 2009 : Phase III trials results reported On September 8, 2010, the FDA Advisory Committee recommended approval for the treatment of community acquired bacterial pneumonia and complicated skin and skin structure infections In Oct 2010, the FDA approval was gained for community-acquired bacterial pneumonia and acute bacterial skin and skin structure infections, including MRSA


The clinical studies indicated ceftaroline was well tolerated The overall rate of adverse events was comparable between the two treatment groups The CANVAS I and CANVAS II trials evaluated ceftaroline monotherapy versus vancomycin plus aztreonam in adult patients with complicated skin and skin structure infections caused by Gram-positive and Gram-negative bacteria The overall discontinuation rate for ceftaroline-treated patients was 27% compared to a rate of 37% for the comparator group-treated patients The most common adverse reactions occurring in > 2% of patients receiving ceftaroline in the pooled phase-III clinical trials were diarrhea, nausea, and rash:


  • Known serious hypersensitivity to ceftaroline or other members of the cephalosporin class
  • Anaphylaxis and anaphylactoid reactions

Warnings and precautions

The warnings and precautions associated with ceftaroline include:

Hypersensitivity reactions

Serious hypersensitivity anaphylactic reactions and serious skin reactions have been reported with beta-lactam antibiotics, including ceftaroline Exercise caution in patients with known hypersensitivity to beta-lactam antibiotics including ceftaroline Before therapy with ceftaroline is instituted, careful inquiry about previous hypersensitivity reactions to other cephalosporins, penicillins, or carbapenems should be made If this product is to be given to penicillin- or other beta-lactam-allergic patients, caution should be exercised because cross sensitivity among beta-lactam antibacterial agents has been clearly established If an allergic reaction to ceftaroline occurs, the drug should be discontinued Serious acute hypersensitivity reactions require emergency treatment with epinephrine and other emergency measures, that may include airway management, oxygen, intravenous fluids, antihistamines, corticosteroids, and vasopressors as clinically indicated

Clostridium difficile-associated diarrhea

Clostridium difficile-associated diarrhea CDAD has been reported for nearly all antibacterial agents including ceftaroline, and may range in severity from mild diarrhea to fatal colitis Careful medical history is necessary because CDAD has been reported to occur more than two months after the administration of antibacterial agents If CDAD is suspected or confirmed, antibacterials not directed against C difficile should be discontinued, if possible

Development of drug-resistant bacteria

Prescribing ceftaroline in the absence of a proven or strongly suspected bacterial infection is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria

Direct Coombs test seroconversion

In the pooled phase-III CABP trials, 51/520 98% of patients treated with ceftaroline compared to 24/534 45% of patients treated with ceftriaxone seroconverted from a negative to a positive direct Coombs' test result No clinical adverse reactions representing hemolytic anemia were reported in any treatment group If anemia develops during or after treatment with ceftaroline, drug-induced hemolytic anemia should be considered If drug-induced hemolytic anemia is suspected, discontinuation of ceftaroline should be considered and supportive care should be administered to the patient if clinically indicated


No clinical drug-drug interaction studies have been conducted with ceftaroline fosamil In vitro studies in human liver microsomes indicated that neither ceftaroline fosamil nor ceftaroline inhibits the major cytochrome P450 isoenzymes Therefore, neither ceftaroline fosamil nor ceftaroline is expected to inhibit or induce the clearance of drugs that are metabolized by these metabolic pathways in a clinically relevant manner

Use in specific populations

For pregnant or nursing mothers, ceftaroline fosamil should be used only if the potential benefit outweighs the potential risk to the fetus or child Safety and effectiveness in pediatric patients has not been studied

Because elderly patients 65 years of age or older are more likely to have decreased renal function and ceftaroline is excreted primarily by the kidney, care should be taken in dose selection in this age group as in younger patients with impaired renal function Dosage adjustment is required in patients with moderately 30 to ‰¤ 50 mL/min or severely < 30 mL/min impaired renal function

The pharmacokinetics of ceftaroline in patients with hepatic impairment have not been established

Side effects

No adverse reactions occurred in greater than 5% of patients receiving ceftaroline The most common adverse reactions occurring in > 2% of patients receiving ceftaroline in the pooled phase-III clinical trials were:

  • Diarrhea
  • Nausea
  • Rash


Ceftaroline fosamil is used in form of the acetate It is a prodrug that is converted to active metabolite ceftaroline and inactive metabolite ceftaroline-M1 Initial in vitro and in vivo animal studies referred to ceftaroline fosamil acetate as PPI-0903

Characteristic of cephalosporins, ceftaroline has a bicyclic ring with four-member β-lactam ring fused to a six-member cephem ring Ceftaroline is thought to have activity against MRSA with its 1,3-thiazole ring


  1. ^ Duplessis, C; Crum-Cianflone, N F; Crum-Cianflone; Duplessis; Duplessis Feb 2011 "Ceftaroline: A New Cephalosporin with Activity against Methicillin-Resistant Staphylococcus aureus MRSA" Clinical Medicine Reviews in Therapeutics 3: a2466 doi:104137/CMRTS1637 PMC 3140339  PMID 21785568 
  2. ^ Karlowsky, James December 2010 "In Vitro Activity of Ceftaroline against Gram-Positive and Gram-Negative Pathogens Isolated from Patients in Canadian Hospitals in 2009" Antimicrob Agents Chemother 55: 2837–46 – via PMC 
  3. ^ Flamm, Robert Oct 2010 "Spectrum and potency of ceftaroline against leading pathogens causing community-acquired respiratory tract and skin and soft tissue infections in Latin America, 2010" Braz J Infect Dis 175: 564–72 – via SciELO 
  4. ^ a b P, Eckberg; Friedland HD; et al FOCUS 1 and 2: Randomized, Double-blinded, Multicenter Phase 3 Trials of the Efficacy and Safety of Ceftaroline CPT vs Ceftriaxone CRO in Community-acquired pneumonia CAP 2009 Interscience Conference on Antimicrobial Agents and Chemotherapy / Infectious Disease Society of America Conference 
  5. ^ a b R, Corey; Wilcox M; Talbot GH; et al CANVAS-1: Randomized, Double-blinded, Phase 3 Study P903-06 of the Efficacy and Safety of Ceftaroline vs Vancomycin plus Aztreonam in Complicated Skin and Skin Structure Infections cSSSI 2008 Interscience Conference on Antimicrobial Agents and Chemotherapy / Infectious Disease Society of America Conference 
  6. ^ a b Kanafani ZA, Corey GR February 2009 "Ceftaroline: a cephalosporin with expanded Gram-positive activity" Future Microbiology 4 1: 25–33 doi:102217/174609134125 PMID 19207097 
  7. ^ a b Parish D, Scheinfeld N February 2008 "Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection" Current Opinion in Investigational Drugs 9 2: 201–9 PMID 18246523 
  8. ^ "Forest Announces FDA Approval of TeflaroTM ceftaroline fosamil for the Treatment of Community-Acquired Bacterial Pneumonia and Acute Bacterial Skin and Skin Structure Infection" Press release Forest Laboratories 2010-10-29 Retrieved October 30, 2010 
  9. ^ Talbot GH, Thye D, Das A, Ge Y October 2007 "Phase 2 study of ceftaroline versus standard therapy in treatment of complicated skin and skin structure infections" Antimicrobial Agents and Chemotherapy 51 10: 3612–6 doi:101128/AAC00590-07 PMC 2043268  PMID 17682094 
  10. ^ "Forest Laboratories Presents Analysis of Two Positive Pivotal Phase III Studies of Ceftaroline for the Treatment of Community-Acquired Pneumonia CAP at ICAAC" Press release BUSINESS WIRE 2009-09-12 Retrieved 2009-10-19 
  11. ^ "New Drug Approvals" 2010-10-29 Retrieved 2010-11-08 
  12. ^ "FDA approves Teflaro for treatment of bacterial infections" 30 Oct 2010 
  13. ^ a b c d "Teflaro" 2010-10-29 Retrieved 2010-11-08 
  14. ^ Y, Ge; Floren L; Redman R; et al The pharmacokinetics and safety of ceftaroline PPI-0903 in healthy subjects receiving multiple-dose intravenous infusions 2006 Interscience Conference on Antimicrobial Agents and Chemotherapy / Infectious Disease Society of America Conference 
  15. ^ Yukihiro I, Junko B 2008 "Stability and Stabilization Studies of TAK-599 Ceftaroline Fosamil a Novel N-Phosphono Type Prodrug of Anti-methicillin Resistant Staphylococcus aureus Cephalosporin T-91825" Chem Pharm Bull 56 10: 1406–11 doi:101248/cpb561406 PMID 18827379 
  16. ^ Ishikawa t; Nobuyuki M; et al 2003 "TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: Synthesis, physicochemical and pharmacological properties" Bioorg Med Chem 11 11: 2427–2437 PMID 12735989 

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