Characterization of the pharmacokinetics of entrectinib and its active M5 metabolite in healthy volunteers and patients with solid tumors.

ABSTRACT:

Background

Entrectinib is an oral, CNS-active, potent inhibitor of tyrosine receptor kinases A/B/C, tyrosine kinase ROS proto-oncogene 1, and anaplastic lymphoma kinase approved for use in patients with solid tumors. We describe 3 clinical studies, including one investigating the single/multiple dose pharmacokinetics of entrectinib in patients and two studies in healthy volunteers investigating the absorption/distribution/metabolism/excretion (ADME) of entrectinib, its relative bioavailability, and effect of food on pharmacokinetics.

Methods

The patient study is open-label with dose-escalation and expansion phases. Volunteers received entrectinib (100-400 mg/m², and 600-800 mg) once daily with food in continuous 28-day cycles. In the ADME study, volunteers receive

SUBMITTER: Meneses-Lorente G 

PROVIDER: S-EPMC8068699 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature