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Ceftaroline fosamil CAS: 400827-46-5

Category: Inhibitors
Product Name: Ceftaroline fosamil
Cat No: I000042
CAS No: 400827-46-5
Related CAS: 229016-73-3
Synonyms: Teflaro; Zinforo; TAK 599
Molecular Formula: 684.68
Molecular Weight: C22H21N8O8PS4
SMILES: O=C(C(N12)=C(SC3=NC(C4=CC=[N+](C)C=C4)=CS3)CS[C@]2([H])[C@H](NC(/C(C5=NSC(NP(O)(O)=O)=N5)=N\OCC)=O)C1=O)[O-]
InChI: InChI=1S/C22H21N8O8PS4/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/h4-8,14,19H,3,9H2,1-2H3,(H4-,24,25,27,28,31,33,34,35,36,37)/b26-13-/t14-,19-/m1/s1
Storage: RT
CAS 400827-46-5,Ceftaroline fosamil
  • Description

Ceftaroline fosamil(cas 400827-46-5), also known as TAK 599 and PPI 0903, is an advanced-generation cephalosporin antibiotic. It is active against methicillin-resistant Staphylococcus aureus (MRSA) and Gram-positive bacteria. It retains the activity of later-generation cephalosporins having broad-spectrum activity against Gram-negative bacteria. It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection.

  • Spec

Purity: >95%

  • References

1. Drugs. 2016 Nov;76(17):1659-1674.
Ceftaroline Fosamil: A Review in Complicated Skin and Soft Tissue Infections and Community-Acquired Pneumonia.
Scott LJ(1).
Author information:
(1)Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand. demail@springer.com.
Intravenous ceftaroline fosamil (Zinforo™), a prodrug that is rapidly converted to its active metabolite ceftaroline, is approved for use in adults and children (from 2 months of age) with complicated skin and soft tissue infections (cSSTIs) or community-acquired pneumonia (CAP). In several multinational trials, ceftaroline fosamil was an effective and generally well tolerated treatment in adult and paediatric patients with cSSTIs or CAP. In the phase 3 CANVAS trials, ceftaroline fosamil treatment was noninferior to vancomycin plus aztreonam in adults with cSSTIs. Based on a meta-analysis of three similarly designed, phase 3 trials (FOCUS 1, FOCUS 2 and an Asian trial), ceftaroline fosamil treatment was superior to ceftriaxone in adults with CAP of Pneumonia Outcomes Research Teams (PORT) risk class III or IV. Ceftaroline fosamil was also associated with high clinical cure rates in hospitalized children (aged 2 months to 17 years) with cSSTIs or CAP. With its broad spectrum of in vitro activity against clinically relevant Gram-positive [including methicillin-resistant Staphylococcus aureus (MRSA) and drug-resistant Streptococcus pneumoniae isolates] and Gram-negative pathogens implicated in cSSTIs and CAP, ceftaroline fosamil is an important treatment option for cSSTI and CAP in adults and children from the age of 2 months.
2. Expert Rev Anti Infect Ther. 2012 Oct;10(10):1087-103. doi: 10.1586/eri.12.112. Epub 2012 Nov 21.
Ceftaroline fosamil: a new cephalosporin active against resistant Gram-positive organisms including MRSA.
Garrison MW(1), Kawamura NM, Wen MM.
Author information:
(1)Washington State University College of Pharmacy, Spokane, WA 99210-1495, USA. garrism@wsu.edu
The growing prevalence of resistant Gram-positive pathogens such as methicillin-resistant Staphylococcus aureus continues to pose a dilemma to clinicians. With strains developing reduced susceptibility to vancomycin, effective and well-tolerated antibiotics to combat these resistant pathogens are needed. Ceftaroline is a new parenteral cephalosporin that has been available in the USA for almost 2 years. Similar to other cephalosporins, it is well tolerated with mostly mild adverse events; however, compared with existing parenteral cephalosporins, ceftaroline has the unique attribute of being bactericidal against resistant Gram-positive aerobes including both hospital- and community-acquired methicillin-resistant S. aureus, S. aureus strains with reduced susceptibility or complete resistance to vancomycin, and resistant Streptococcus pneumoniae including multidrug-resistant strains. Current indications in the USA and Europe include treatment of adults with complicated skin, skin-structure infections and community-acquired pneumonia. This paper will review the properties of ceftaroline, its spectrum of activity, clinical use, safety profile and future role.
3. J Antimicrob Chemother. 2011 Apr;66 Suppl 3:iii45-51. doi: 10.1093/jac/dkr098.
Review of ceftaroline fosamil microbiology: integrated FOCUS studies.
Critchley IA(1), Eckburg PB, Jandourek A, Biek D, Friedland HD, Thye DA.
Author information:
(1)Cerexa, Inc., Oakland, CA 94612, USA. icritchley@cerexa.com
Ceftaroline fosamil, the prodrug form of ceftaroline, is a novel broad-spectrum parenteral cephalosporin that exhibits antibacterial activity against typical respiratory pathogens such as Streptococcus pneumoniae, Haemophilus influenzae, Staphylococcus aureus and common Gram-negative pathogens. In particular, ceftaroline has activity against resistant Gram-positive cocci, including penicillin- and multidrug-resistant S. pneumoniae, as well as methicillin-resistant S. aureus. The activity of ceftaroline against these phenotypes is attributed to its ability to bind to modified penicillin-binding proteins with high affinity when compared with other β-lactams. The activity of ceftaroline is not compromised by the ability of H. influenzae to produce β-lactamase. Ceftaroline fosamil was compared with ceftriaxone for safety and efficacy in two randomized, double-blinded, controlled Phase III clinical trials for the treatment of community-acquired pneumonia (CAP). Microbiological assessments at baseline included respiratory specimen cultures, blood cultures, urinary antigen testing and atypical pathogen serology testing. By-subject and by-pathogen microbiological outcomes were assessed in the microbiologically evaluable population at the test-of-cure visit. The favourable microbiological response rates by subject for ceftaroline were 87.0% compared with 81.0% for ceftriaxone. The by-pathogen microbiological response rates of ceftaroline and ceftriaxone were 87.3% and 72.9% for S. pneumoniae, 83.3% and 85.0% for H. influenzae and 76.0% and 70.4% for S. aureus, respectively. Key baseline pathogens such as S. pneumoniae, H. influenzae and methicillin-susceptible S. aureus were susceptible to ceftaroline, with MIC(90)s of 0.03, 0.03 and 0.25 mg/L, respectively, supporting its utility as a promising new agent for treatment of CAP.
4. J Antimicrob Chemother. 2010 Nov;65 Suppl 4:iv9-16. doi: 10.1093/jac/dkq251.
Ceftaroline fosamil: a novel broad-spectrum cephalosporin with expanded anti-Gram-positive activity.
Biek D(1), Critchley IA, Riccobene TA, Thye DA.
Author information:
(1)Cerexa, Inc., Oakland, CA 94612, USA. ronald-jones@jmilabs.com
Ceftaroline fosamil is a novel cephalosporin with broad-spectrum activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative organisms. The activity of ceftaroline against MRSA is attributed to its ability to bind to penicillin-binding protein (PBP) 2a with high affinity and inhibit the biochemical activity of PBP 2a more efficiently than other presently available β-lactams. The activity of ceftaroline against MRSA and the β-haemolytic streptococci makes it an attractive monotherapy agent for the treatment of complicated skin and skin structure infections (cSSSIs). Recent profiling and surveillance studies have shown that ceftaroline is active against contemporary skin pathogens collected from US and European medical centres in 2008. The mean free drug %T  >  MIC (percentage of time the drug concentration remains above the MIC) needed for stasis ranged from 26% for S. aureus to 39% for S. pneumoniae in the murine thigh infection model. Pharmacokinetic and pharmacodynamic target attainment predictions for 600 mg of ceftaroline fosamil every 12 h showed that the mean %T  >  MICs for which plasma free-drug concentrations exceeded an MIC of 1 and 2 mg/L were 71% and 51% of the dosing interval, respectively. For a 40% T  >  MIC target, the predicted attainments for infections due to pathogens for which ceftaroline MICs were 1 or 2 mg/L were 100% and 90%, respectively. Clinical and microbiological successes of ceftaroline fosamil in treating cSSSIs were demonstrated in two Phase III clinical studies, in which 96.8% of all baseline cSSSI isolates from the microbiologically evaluable population were inhibited by ceftaroline at ≤ 2 mg/L. Ceftaroline fosamil is a promising broad-spectrum agent for the treatment of cSSSIs.

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