Population PK Modeling and Target Attainment Simulations to Support Dosing of Ceftaroline Fosamil in Pediatric Patients With Acute Bacterial Skin and Skin Structure Infections and Community-Acquired Bacterial Pneumonia

J Clin Pharmacol. 2017 Mar;57(3):345-355. doi: 10.1002/jcph.809. Epub 2016 Sep 27.

Abstract

Ceftaroline, the active form of the prodrug ceftaroline fosamil, is approved for use in adults with community-acquired bacterial pneumonia (CABP) or acute bacterial skin and skin structure infections (ABSSSI) in the United States and for similar indications in Europe. Pharmacokinetic (PK) data from 5 pediatric (birth to <18 years) studies of ceftaroline fosamil were combined with PK data from adults to update a population PK model for ceftaroline and ceftaroline fosamil. This model, based on a data set including 305 children, was used to conduct simulations to estimate ceftaroline exposures and percentage of time that free drug concentrations were above the minimum inhibitory concentration (%fT>MIC) for pediatric dose regimens. With dose regimens of 8 mg/kg every 8 hours (q8h) in children aged 2 months to <2 years and 12 mg/kg (up to a maximum of 400 mg) q8h in children aged 2 years to <18 years or 600 mg q12h in children aged 12 to <18 years, >90% of children were predicted to achieve a target of 36% fT>MIC at an MIC of 2 mg/L, and >97% were predicted to achieve 44% fT>MIC at an MIC of 1 mg/L. Thus, high PK/pharmacodynamic target attainment would be maintained in children for targets associated with 1-log kill of Staphylococcus aureus and Streptococcus pneumoniae. The predicted ceftaroline exposures for these dose regimens were similar to those in adults given 600 mg q12h ceftaroline fosamil. This work contributed to the approval of dose regimens for children aged 2 months to <18 years by the FDA and EMA, which are presented.

Keywords: ABSSSI; CABP; ceftaroline fosamil; pediatric; pharmacodynamic; population pharmacokinetics.

MeSH terms

  • Acute Disease
  • Adolescent
  • Anti-Bacterial Agents / pharmacokinetics*
  • Anti-Bacterial Agents / pharmacology
  • Anti-Bacterial Agents / therapeutic use*
  • Ceftaroline
  • Cephalosporins / pharmacokinetics*
  • Cephalosporins / pharmacology
  • Cephalosporins / therapeutic use*
  • Child
  • Child, Preschool
  • Clinical Trials as Topic
  • Community-Acquired Infections
  • Computer Simulation
  • Female
  • Humans
  • Infant
  • Male
  • Microbial Sensitivity Tests
  • Models, Biological
  • Pneumonia, Bacterial / drug therapy*
  • Skin Diseases, Bacterial / drug therapy*
  • Staphylococcus aureus
  • Streptococcus pneumoniae

Substances

  • Anti-Bacterial Agents
  • Cephalosporins