Lee HW, et al. - This trial aspired to probe 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 men. It was deduced that MB12066 was safe and well tolerated in healthy volunteers. No serious adverse events (AEs) were reported. A link was observed between the accumulation in plasma due to twice-daily administration with a 2.72 accumulation ratio.