Integrated population pharmacokinetics of etirinotecan pegol and its four metabolites in cancer patients with solid tumors.

ABSTRACT: PURPOSE:Etirinotecan pegol (EP), a long-acting topoisomerase-1 inhibitor, is a polyethylene glycol conjugate of irinotecan, with an intended indication for treatment of breast cancer with brain metastases. The objective of this study was to develop a population pharmacokinetic (popPK) model of EP and four of its metabolites (irinotecan, SN38, SN38-glucuronide, and APC) and determine covariates affecting their pharmacokinetics. METHODS:Data from 83 cancer patients enrolled in phase 1 studies were used. The model was developed in two stages: (1) concentration-time data were analyzed with a 3-analyte model for EP, irinotecan, and SN38; and (2) a 5-analyte model developed based on expansion of 3-analyte model to include concentration-time data for SN38 glucuronide and APC with parameter values

SUBMITTER: Sy SKB 

PROVIDER: S-EPMC5907632 | biostudies-literature | 2018 May

REPOSITORIES: biostudies-literature