Pharmacokinetic and safety evaluation of MB12066, an NQO1 substrate.

ABSTRACT:

Objective

This study evaluated the pharmacokinetics (PKs) and safety of a newly developed β-lapachone (MB12066) tablet, a natural NAD(P)H:quinone oxidoreductase 1 (NQO1) substrate, in healthy male volunteers.

Methods

In a randomized, double-blind, multiple-dose, two-treatment study, 100 mg MB12066 or placebo was given twice daily for 8 days to groups of eight or three fasted healthy male subjects, respectively, followed by serial blood sampling. Plasma concentrations for β-lapachone were determined using liquid chromatography-tandem mass spectrometry. PK parameters were obtained with non-compartmental analysis. Tolerability was assessed based on physical examinations, vital signs, clinical laboratory tests, and electrocardiograms.

Results

Following a single 100 mg MB1

SUBMITTER: Lee HW 

PROVIDER: S-EPMC5604554 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature