Ceftolozane/tazobactam pharmacokinetic/pharmacodynamic-derived dose justification for phase 3 studies in patients with nosocomial pneumonia

J Clin Pharmacol. 2016 Jan;56(1):56-66. doi: 10.1002/jcph.566. Epub 2015 Aug 25.

Abstract

Ceftolozane/tazobactam is an antipseudomonal antibacterial approved for the treatment of complicated urinary tract infections (cUTIs) and complicated intra-abdominal infections (cIAIs) and in phase 3 clinical development for treatment of nosocomial pneumonia. A population pharmacokinetic (PK) model with the plasma-to-epithelial lining fluid (ELF) kinetics of ceftolozane/tazobactam was used to justify dosing regimens for patients with nosocomial pneumonia in phase 3 studies. Monte Carlo simulations were performed to determine ceftolozane/tazobactam dosing regimens with a > 90% probability of target attainment (PTA) for a range of pharmacokinetic/pharmacodynamic targets at relevant minimum inhibitory concentrations (MICs) for key pathogens in nosocomial pneumonia. With a plasma-to-ELF penetration ratio of approximately 50%, as observed from an ELF PK study, a doubling of the current dose regimens for different renal functions that are approved for cUTIs and cIAIs is needed to achieve > 90% PTA for nosocomial pneumonia. For example, a 3-g dose of ceftolozane/tazobactam for nosocomial pneumonia patients with normal renal function is needed to achieve a > 90% PTA (actual 98%) for the 1-log kill target against pathogens with an MIC of ≤ 8 mg/L in ELF, compared with the 1.5-g dose approved for cIAIs and cUTIs.

Keywords: Pseudomonas aeruginosa; ceftolozane/tazobactam; dose justification; epithelial lining fluid; nosocomial pneumonia; probability of target attainment.

Publication types

  • Clinical Trial, Phase III
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics*
  • Anti-Bacterial Agents / pharmacology*
  • Bronchoalveolar Lavage Fluid / chemistry
  • Cephalosporins / blood
  • Cephalosporins / pharmacokinetics*
  • Cephalosporins / pharmacology*
  • Cross Infection / drug therapy
  • Cross Infection / metabolism
  • Drug Combinations
  • Female
  • Humans
  • Male
  • Microbial Sensitivity Tests
  • Middle Aged
  • Models, Biological
  • Monte Carlo Method
  • Penicillanic Acid / analogs & derivatives*
  • Penicillanic Acid / blood
  • Penicillanic Acid / pharmacokinetics
  • Penicillanic Acid / pharmacology
  • Pneumonia / drug therapy
  • Pneumonia / metabolism
  • Tazobactam
  • Young Adult

Substances

  • Anti-Bacterial Agents
  • Cephalosporins
  • Drug Combinations
  • ceftolozane
  • Penicillanic Acid
  • Tazobactam