TAK-599, also known as Ceftaroline fosamil 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.
Chemical Formula: C24H25N8O10PS4
Exact Mass: 684.01028
Molecular Weight: 744.72
Elemental Analysis: C, 38.71; H, 3.38; N, 15.05; O, 21.48; P, 4.16; S, 17.22
Chemical Name: 4-(2-(((6R,7R)-2-carboxy-7-((Z)-2-(ethoxyimino)-2-(5-(phosphonoamino)-1,2,4-thiadiazol-3-yl)acetamido)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl)thio)thiazol-4-yl)-1-methylpyridin-1-ium acetate
InChi Code: InChI=1S/C22H21N8O8PS4.C2H4O2/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)/b26-13-;/t14-,19-;/m1./s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
TAK-599 is effective against all 10 MRSA isolates used in the dose-ranging studies and requires approximately 17 to 43% fT>MIC (the percentage of time that free drug concentrations remain above the MIC) to produce a 1-log10 kill. The TAK-599 treatment results in mean reductions of 1.1 to 2.4 log10 CFU, with no relationship to the TAK-599 MIC. The use of high inocula does not affect the TAK-599 efficacy against the three strains tested, with mean decreases of 2.0 to 3.0 log10 CFU.
Yang L, Sunzel M, Xu P, Edeki T, Wilson D, Li J, Li H. Evaluation of the pharmacokinetics and safety of single and multiple ceftaroline fosamil infusions in healthy Chinese and Western subjects. Int J Clin Pharmacol Ther. 2015 Jul 8. [Epub ahead of print] PubMed PMID: 26152131.
Shandurenko IN. [New antibiotic in treatment of surgical infection: the first experience]. Khirurgiia (Mosk). 2015;(3):81-3. Russian. PubMed PMID: 26031957.
Rashid MU, Rosenborg S, Panagiotidis G, Löfdal KS, Weintraub A, Nord CE. Ecological Effect of Ceftaroline-Avibactam on the Normal Human Intestinal Microbiota. Antimicrob Agents Chemother. 2015 May 18. pii: AAC.00530-15. [Epub ahead of print] PubMed PMID: 25987638.
Kaye KS, Udeani G, Cole P, Friedland HD. Ceftaroline fosamil for the treatment of hospital-acquired pneumonia and ventilator-associated pneumonia. Hosp Pract (1995). 2015 May 8:1-6. [Epub ahead of print] PubMed PMID: 25956849.
Kiang TK, Wilby KJ, Ensom MH. A Critical Review on the Clinical Pharmacokinetics, Pharmacodynamics, and Clinical Trials of Ceftaroline. Clin Pharmacokinet. 2015 May 5. [Epub ahead of print] PubMed PMID: 25940827.
Maggiore C, Vazquez JA, Guervil DJ, Ramani A, Jandourek A, Cole P, Friedland HD. Ceftaroline fosamil for the treatment of community-acquired bacterial pneumonia in the intensive care unit. Ther Clin Risk Manag. 2015 Apr 2;11:557-63. doi: 10.2147/TCRM.S75191. eCollection 2015. PubMed PMID: 25897240; PubMed Central PMCID: PMC4397928.
Justo JA, Mayer SM, Pai MP, Soriano MM, Danziger LH, Novak RM, Rodvold KA. Pharmacokinetics of Ceftaroline in Normal Body Weight and Obese (Classes I, II, and III) Healthy Adult Subjects. Antimicrob Agents Chemother. 2015 Jul;59(7):3956-65. doi: 10.1128/AAC.00498-15. Epub 2015 Apr 20. PubMed PMID: 25896707; PubMed Central PMCID: PMC4468711.
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