title: Ceftaroline: a comprehensive update.
abstract: Ceftaroline is a novel broad-spectrum cephalosporin antibiotic currently under US Food and Drug Administration (FDA) review for a new drug application (NDA), filed by Cerexa, Inc. (a wholly owned subsidiary of Forest Laboratories), for the treatment of complicated skin and skin-structure infections (cSSSIs) and community-associated pneumonia (CAP). The antibiotic acts by binding to penicillin-binding proteins in bacteria, consistent with other β-lactams. The antimicrobial spectrum of ceftaroline ranges from aerobic and anaerobic Gram-positive bacteria, including drug-resistant isolates of staphylococci, i.e. heterogeneous vancomycin-intermediate Staphylococcus aureus (hVISA), vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA), to anaerobic Gram-negative pathogens such as Moraxella catarrhalis and Haemophilus influenzae (including β-lactamase-positive strains), as well as bacteria with multiple resistance phenotypes. Ceftaroline fosamil is the prodrug that is rapidly dephosphorylated by in vivo plasma phosphatases to the active drug ceftaroline, which follows a two-compartmental pharmacokinetic model and is eliminated primarily by renal excretion, with a plasma half-life of ca. 2.5 h. Ceftaroline is well tolerated, which is consistent with its good safety profile similar to other cephalosporins in clinical trials. Thus, it would be a promising drug to fight multidrug-resistant superbugs such as S. aureus and Streptococcus pneumoniae for the treatment of cSSSIs and CAP.
authors.affiliation: Department of Pharmaceutical Chemistry, Rajendra Institute of Technology & Sciences, 4th Mile Stone, Hisar Road, Sirsa 125055, Haryana, India. darpkaush@yahoo.com
authors.forename: Darpan
authors.initials: D
authors.lastname: Kaushik
authors.forename: Sudeep
authors.initials: S
authors.lastname: Rathi
authors.forename: Ankit
authors.initials: A
authors.lastname: Jain
mesh_terms: D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D001419:Bacteria / Q000187:drug effects*; D002511:Cephalosporins / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D017277:Drug Approval; D006801:Humans; D018410:Pneumonia, Bacterial / Q000188:drug therapy*; D011355:Prodrugs / Q000378:metabolism; D017192:Skin Diseases, Bacterial / Q000188:drug therapy*; D018461:Soft Tissue Infections / Q000188:drug therapy*; D014481:United States; D000097583:Ceftaroline
chemical_list: D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D011355:Prodrugs; D000097583:Ceftaroline