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The drug received an approvable letter from the United States Food and Drug Administration (FDA) in March 2008 and from Health Canada in June 2008 for the treatment of complicated skin and skin structure infections including diabetic foot infections. Ceftobiprole exerts its antibacterial activity by inhibiting the penicillin\u2010binding proteins (PBPs) involved in cell wall synthesis. It has an established stability against hydrolysis by many gram\u2010positive \u03b2\u2010lactamases and a higher affinity for various PBPs (such as PBP2a of MRSA or PBP2x of <jats:italic>Streptococcus pneumoniae)<\/jats:italic>, which leads to a wider spectrum of activity compared with older \u03b2\u2010lactams. Ceftobiprole activity does not cover extended\u2010spectrum \u03b2\u2010lactamase\u2010producing Enterobacteriaceae and some other pathogens, including <jats:italic>Enterococcus faecium<\/jats:italic> or <jats:italic>Acinetobacter baumanii<\/jats:italic>. Generally well tolerated, with nausea and taste disturbance being the most common adverse events, ceftobiprole appeared noninferior to empiric therapy in several clinical trials. Ceftobiprole is available only for intravenous administration; recommended dosage regimens have not been approved by the FDA as of this writing. However, based on the Canadian package insert, expected dosage recommendations are 500 mg as a 1\u2010hour intravenous infusion every 12 hours for the treatment of complicated skin and skin structure infections caused by certain gram\u2010positive pathogens, and 500 mg as a 2\u2010hour infusion every 8 hours when susceptible gram\u2010negative or both gram\u2010positive and susceptible gram\u2010negative pathogens are involved. Dosage adjustments are indicated for patients with moderate or severe renal impairment, and dosage recommendations are expected to be 500 or 250 mg, respectively, as a 2\u2010hour infusion every 12 hours. Several precautions regarding hypersensitivity and drug incompatibility are reported. Ceftobiprole represents a promising option for the treatment of mono\u2010 and polymicrobial infections caused by multidrug\u2010resistant gram\u2010positive and susceptible gram\u2010negative pathogens, but further toxicity and safety studies are warranted.<\/jats:p>","DOI":"10.1592\/phco.29.5.511","type":"journal-article","created":{"date-parts":[[2009,4,27]],"date-time":"2009-04-27T14:02:37Z","timestamp":1240840957000},"page":"511-525","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":19,"title":["Ceftobiprole: First Cephalosporin with Activity Against Methicillin\u2010Resistant <i>Staphylococcus aureus<\/i>"],"prefix":"10.1002","volume":"29","author":[{"given":"C\u00e9line","family":"Vidaillac","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Michael J.","family":"Rybak","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2012,1,6]]},"reference":[{"key":"e_1_2_1_2_2","doi-asserted-by":"publisher","DOI":"10.1086\/533590"},{"key":"e_1_2_1_3_2","doi-asserted-by":"publisher","DOI":"10.1086\/499367"},{"key":"e_1_2_1_4_2","doi-asserted-by":"publisher","DOI":"10.1556\/AMicr.55.2008.1.1"},{"key":"e_1_2_1_5_2","first-page":"57","article-title":"Deaths involving MRSA: England and Wales, 1993\u20132006","volume":"37","author":"Cowcroft N.","year":"2008","journal-title":"Health Stat Q"},{"key":"e_1_2_1_6_2","doi-asserted-by":"publisher","DOI":"10.3184\/003685002783238870"},{"key":"e_1_2_1_7_2","doi-asserted-by":"publisher","DOI":"10.1086\/533592"},{"key":"e_1_2_1_8_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.45.3.825-836.2001"},{"key":"e_1_2_1_9_2","doi-asserted-by":"publisher","DOI":"10.1128\/AAC.48.7.2570-2575.2004"},{"key":"e_1_2_1_10_2","doi-asserted-by":"publisher","DOI":"10.1016\/j.jpba.2007.06.002"},{"key":"e_1_2_1_11_2","unstructured":"Lovering A. 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