Population Pharmacokinetics of Durvalumab in Cancer Patients and Association With Longitudinal Biomarkers of Disease Status

Clin Pharmacol Ther. 2018 Apr;103(4):631-642. doi: 10.1002/cpt.982. Epub 2018 Feb 2.

Abstract

The objectives of this analysis were to develop a population pharmacokinetics (PK) model of durvalumab, an anti-PD-L1 antibody, and quantify the impact of baseline and time-varying patient/disease characteristics on PK. Pooled data from two studies (1,409 patients providing 7,407 PK samples) were analyzed with nonlinear mixed effects modeling. Durvalumab PK was best described by a two-compartment model with both linear and nonlinear clearances. Three candidate models were evaluated: a time-invariant clearance (CL) model, an empirical time-varying CL model, and a semimechanistic time-varying CL model incorporating longitudinal covariates related to disease status (tumor shrinkage and albumin). The data supported a slight decrease in durvalumab clearance with time and suggested that it may be associated with a decrease in nonspecific protein catabolic rate among cancer patients who benefit from therapy. No covariates were clinically relevant, indicating no need for dose adjustment. Simulations indicated similar overall PK exposures following weight-based and flat-dosing regimens.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antibodies, Monoclonal / pharmacokinetics*
  • Antineoplastic Agents, Immunological / pharmacokinetics
  • B7-H1 Antigen / immunology
  • Computer Simulation
  • Drug Dosage Calculations*
  • Female
  • Humans
  • Male
  • Metabolic Clearance Rate*
  • Middle Aged
  • Models, Biological
  • Neoplasm Staging
  • Neoplasms / classification
  • Neoplasms / drug therapy*
  • Neoplasms / immunology
  • Neoplasms / pathology

Substances

  • Antibodies, Monoclonal
  • Antineoplastic Agents, Immunological
  • B7-H1 Antigen
  • CD274 protein, human
  • durvalumab