{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,9]],"date-time":"2026-09-09T20:36:30Z","timestamp":1788986190130,"version":"build-2803163510"},"reference-count":19,"publisher":"American Society for Microbiology","issue":"4","license":[{"start":{"date-parts":[[2006,4,1]],"date-time":"2006-04-01T00:00:00Z","timestamp":1143849600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2006,4]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n                  <jats:p>\n                    PPI-0903 is a new cephalosporin with broad-spectrum activity, including beta-lactam-resistant\n                    <jats:italic>Streptococcus pneumoniae<\/jats:italic>\n                    and\n                    <jats:italic>Staphylococcus aureus<\/jats:italic>\n                    . We used the neutropenic murine thigh and lung infection models to examine the pharmacodynamic characteristics of PPI-0903. Serum drug levels following four fourfold-escalating single doses of PPI-0903 were measured by microbiologic assay. In vivo postantibiotic effects (PAEs) were determined after doses of 1.56, 6.25, 25, and 100 mg\/kg of body weight in mice infected with\n                    <jats:italic>S. pneumoniae<\/jats:italic>\n                    ATCC 10813,\n                    <jats:italic>S. aureus<\/jats:italic>\n                    ATCC 29213, or\n                    <jats:italic>Escherichia coli<\/jats:italic>\n                    ATCC 25922. Dose fractionation studies over a 24-h dose range of 0.39 to 1,600 mg\/kg were administered every 3, 6, 12, or 24 hours. Nonlinear regression analysis was used to determine which pharmacokinetic-pharmacodynamic (PK-PD) index (total and free 65% drug) best correlated with CFU\/thigh at 24 h. Similar to other beta-lactam antibiotics, PPI-0903 produced short to modest in vivo PAEs with either\n                    <jats:italic>S. pneumoniae<\/jats:italic>\n                    or\n                    <jats:italic>E. coli<\/jats:italic>\n                    . The percent time that serum concentrations were above the MIC (%T&gt;MIC) was the PK-PD index that best correlated with efficacy (\n                    <jats:italic>R<\/jats:italic>\n                    <jats:sup>2<\/jats:sup>\n                    = 84 to 88% for the three organisms, compared with 9 to 41% for peak\/MIC and 30 to 82% for the area under the concentration-time curve\/MIC). In subsequent studies we used the neutropenic murine thigh infection model to determine if the magnitude of the free-drug %T&gt;MIC needed for efficacy of PPI-0903 varied among pathogens (including resistant strains). Mice infected with one of five isolates of\n                    <jats:italic>S. pneumoniae<\/jats:italic>\n                    , four isolates of\n                    <jats:italic>S. aureus<\/jats:italic>\n                    , or four gram-negative bacilli were treated for 24 h with 0.10 to 400 mg\/kg of PPI-0903 every 6 h. A sigmoid dose-response model was used to estimate the doses (mg\/kg\/24 h) required to achieve a net bacteriostatic affect over 24 h and to produce a reduction in the burden of organisms from the start of therapy by 1 and 2 log\n                    <jats:sub>10<\/jats:sub>\n                    CFU\/thigh. MICs ranged from 0.008 to 1 \u03bcg\/ml. Mean free-drug %T&gt;MICs \u00b1 the standard deviation associated with the static effect endpoint for\n                    <jats:italic>S. pneumoniae<\/jats:italic>\n                    ,\n                    <jats:italic>S. aureus<\/jats:italic>\n                    , and gram-negative isolates were 39 \u00b1 9, 26 \u00b1 8, and 32 \u00b1 6, respectively. Methicillin and penicillin resistance did not alter the magnitude of free-drug %T&gt;MIC required for efficacy. The free-drug %T&gt;MIC necessary for efficacy was slightly reduced in animals with normal neutrophil counts. Treatment effect was similar in both the thigh and lung infection models. The pharmacodynamic characteristics of PPI-0903 are similar to those of other compounds within the cephalosporin class.\n                  <\/jats:p>","DOI":"10.1128\/aac.50.4.1376-1383.2006","type":"journal-article","created":{"date-parts":[[2006,3,28]],"date-time":"2006-03-28T17:03:12Z","timestamp":1143565392000},"page":"1376-1383","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":126,"title":["Pharmacodynamics of a New Cephalosporin, PPI-0903 (TAK-599), Active against Methicillin-Resistant\n                    <i>Staphylococcus aureus<\/i>\n                    in Murine Thigh and Lung Infection Models: Identification of an In Vivo Pharmacokinetic-Pharmacodynamic Target"],"prefix":"10.1128","volume":"50","author":[{"given":"D.","family":"Andes","sequence":"first","affiliation":[{"name":"Department of Medicine, Section of Infectious Diseases, University of Wisconsin School of Medicine, Madison, Wisconsin"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"W. A.","family":"Craig","sequence":"additional","affiliation":[{"name":"Department of Medicine, Section of Infectious Diseases, University of Wisconsin School of Medicine, Madison, Wisconsin"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"235","reference":[{"key":"e_1_3_1_2_2","first-page":"463","volume":"7","year":"1997","unstructured":"Ambrose, P. G., R. Quintiliani, and N. Chin. 1997. Continuous vs intermittent infusion of cefuroxime for the treatment of community-acquired pneumonia. Infect. Dis. Clin. Pract.7:463-470.","journal-title":"Infect. Dis. Clin. 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