Drug-drug interactions that alter the exposure of glucuronidated drugs: Scope, UDP-glucuronosyltransferase (UGT) enzyme selectivity, mechanisms (inhibition and …

JO Miners, TM Polasek, JA Hulin, A Rowland… - Pharmacology & …, 2023 - Elsevier
Drug-drug interactions (DDIs) arising from the perturbation of drug metabolising enzyme
activities represent both a clinical problem and a potential economic loss for the …

Identifying the Reactive Metabolites of Tyrosine Kinase Inhibitor Pexidartinib In Vitro Using LC–MS-Based Metabolomic Approaches

X Qin, Y Wang, KR MacKenzie… - Chemical Research …, 2023 - ACS Publications
Pexidartinib (PEX, TURALIO), a selective and potent inhibitor of the macrophage colony-
stimulating factor-1 receptor, has been approved for the treatment of tenosynovial giant cell …

An open‐label study to explore the optimal design of CYP3A drug–drug interaction clinical trials in healthy Chinese people

J Chen, J Li, J Wu, Y Song, L Li… - Pharmacology …, 2024 - Wiley Online Library
A drug–drug interaction (DDI) trial of cytochrome P450 3A (CYP3A) is a necessary part of
early‐phase trials of drugs mainly metabolized by this enzyme, but CYP3A DDI clinical trials …

Physiologically Based Pharmacokinetic Absorption Model for Pexidartinib to Evaluate the Impact of Meal Contents and Intake Timing on Drug Exposure

S Nakayama, V Lukacova, S Tanabe… - Clinical …, 2024 - Wiley Online Library
Pexidartinib is a systemic treatment for patients with tenosynovial giant cell tumor not
amenable to surgery. Oral absorption of pexidartinib is affected by food; administration with …

Pexidartinib Triggers the Risk of Drug-drug Interactions by Inhibiting UDP-glucuronosyltransferase in vitro

Y Liu, Z Wang, X Lv, H Yin, L Jiang… - Authorea Preprints, 2023 - advance.sagepub.com
Pexidartinib is the first FDA approved drug for adult patients with tenosynovial giant cell
tumor that are not amenable to improvement with surgery. In vitro data has showed …