In vivo Metabolism of Nifurtimox and the Drug-Drug Interaction Potential Including its Major Metabolites.

ABSTRACT:

Background

Nifurtimox is an effective treatment for patients with Chagas disease, but knowledge of its biotransformation and excretion is limited.

Objective

This study aimed to better understand the fate of oral nifurtimox in vivo.

Methods

We investigated the exposure and excretion pathways of [¹⁴C]-labeled nifurtimox and its metabolites in rats. We then quantified the prominent metabolites and nifurtimox in the urine and plasma of patients receiving nifurtimox using LC-HRMS with reference standards and quantified these compounds in rat plasma after a single, high dose of nifurtimox. We also investigated potential drug-drug interactions (DDIs) of these compounds in vitro.

Results

In rats, orally administered nifurtimox was rapidly absor

SUBMITTER: Schulz SI 

PROVIDER: S-EPMC10661964 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature