Pharmacometabolomics uncovers key metabolic changes in the first-in-human study of β-lapachone derivative.

ABSTRACT:

Introduction

WK0202, a β-lapachone derivative under clinical development, activates NAD(P)H quinone dehydrogenase 1 (NQO1), acting as a detoxifying and antioxidant agent. In this study, a metabolomics investigation of β-lapachone derivatives in humans is performed to characterize drug-induced alterations in endogenous metabolic pathways.

Objectives

This study investigated metabolic alterations induced by WK0202 administration and their potential association with its therapeutic mechanism and efficacy. Using targeted and untargeted metabolomics approaches, we identified potential pharmacodynamic biomarker candidates that may reflect the drug's activity and metabolic effects.

Methods

Plasma samples from healthy subjects who received multiple doses of WK0202 were compare

SUBMITTER: Jang Y 

PROVIDER: S-EPMC12364990 | biostudies-literature | 2025 Aug

REPOSITORIES: biostudies-literature