Ceftazidime-Avibactam Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Across Adult Indications and Patient Subgroups

Clin Transl Sci. 2019 Mar;12(2):151-163. doi: 10.1111/cts.12585. Epub 2018 Sep 28.

Abstract

Ceftazidime-avibactam is a novel β-lactam/β-lactamase inhibitor combination for the treatment of serious infections caused by resistant gram-negative pathogens. Population pharmacokinetic (PopPK) models were built to incorporate pharmacokinetic (PK) data from five phase III trials in patients with complicated intra-abdominal infection (cIAI), complicated urinary tract infection (cUTI), or nosocomial (including ventilator-associated) pneumonia. Ceftazidime and avibactam pharmacokinetics were well-described by two-compartment disposition models, with creatinine clearance (CrCL) the key covariate determining clearance variability. Steady-state ceftazidime and avibactam exposure for most patient subgroups differed by ≤ 20% vs. healthy volunteers. Probability of PK/pharmacodynamic (PD) target attainment (free plasma ceftazidime > 8 mg/L and avibactam > 1 mg/L for ≥ 50% of dosing interval) was ≥ 94.9% in simulations for all patient subgroups, including indication and renal function categories. No exposure-microbiological response relationship was identified because target exposures were achieved in almost all patients. These modeling results support the approved ceftazidime-avibactam dosage regimens (2000-500 mg every 8 hours, adjusted for CrCL ≤ 50 mL/min).

Trial registration: ClinicalTrials.gov NCT01291602 NCT01430910 NCT01920399 NCT01499290 NCT01500239 NCT01726023 NCT01644643 NCT01595438 NCT01599806 NCT01808092 NCT01624246.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Bacterial Agents / therapeutic use
  • Azabicyclo Compounds / pharmacology*
  • Azabicyclo Compounds / therapeutic use
  • Ceftazidime / pharmacology*
  • Ceftazidime / therapeutic use
  • Clinical Trials, Phase III as Topic
  • Creatinine / blood
  • Creatinine / metabolism
  • Datasets as Topic
  • Dose-Response Relationship, Drug
  • Drug Combinations
  • Female
  • Humans
  • Male
  • Middle Aged
  • Models, Biological*
  • Pneumonia, Ventilator-Associated / drug therapy
  • Renal Elimination
  • Urinary Tract Infections / blood
  • Urinary Tract Infections / drug therapy
  • Young Adult

Substances

  • Anti-Bacterial Agents
  • Azabicyclo Compounds
  • Drug Combinations
  • avibactam, ceftazidime drug combination
  • Ceftazidime
  • Creatinine

Associated data

  • ClinicalTrials.gov/NCT01291602
  • ClinicalTrials.gov/NCT01430910
  • ClinicalTrials.gov/NCT01920399
  • ClinicalTrials.gov/NCT01499290
  • ClinicalTrials.gov/NCT01500239
  • ClinicalTrials.gov/NCT01726023
  • ClinicalTrials.gov/NCT01644643
  • ClinicalTrials.gov/NCT01595438
  • ClinicalTrials.gov/NCT01599806
  • ClinicalTrials.gov/NCT01808092
  • ClinicalTrials.gov/NCT01624246