Pharmacokinetics and safety of erlotinib and its metabolite OSI-420 in infants and children with primary brain tumors.

ABSTRACT:

Purpose

Erlotinib (Tarceva^®), a potent small molecule inhibitor of the epidermal growth factor receptor tyrosine kinase, has been evaluated to treat infants and children with primary brain tumors. The pharmacokinetics of erlotinib and its primary metabolite OSI-420 were characterized and exposure-safety associations were investigated.

Methods

This analysis involved patients enrolled in two clinical studies and receiving oral erlotinib once daily as part of treatment. Single-dose and steady-state erlotinib and OSI-420 plasma concentrations were assayed using HPLC-MS/MS methods. Population pharmacokinetic modeling and univariate covariate analysis evaluating demographic, clinical and selected CYP3A5, CYP3A4, ABCB1, and ABCG2 genotypes were performed. Associations be

SUBMITTER: Reddick SJ 

PROVIDER: S-EPMC6773504 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature