This study reports the pharmacokinetics and tissue distribution of a novel 
histone deacetylase and DNA methyltransferase inhibitor, psammaplin A (PsA), in 
mice. PsA concentrations were determined by a validated LC-MS/MS assay method 
(LLOQ 2 ng/mL). Following intravenous injection at a dose of 10 mg/kg in mice, 
PsA was rapidly eliminated, with the average half-life (t(1/2, λn)) of 9.9 ± 1.4 
min and the systemic clearance (CL(s)) of 925.1 ± 570.1 mL/min. The in vitro 
stability of PsA was determined in different tissue homogenates. The average 
degradation t(1/2) of PsA in blood, liver, kidney and lung was found relatively 
short (≤ 12.8 min). Concerning the in vivo tissue distribution characteristics, 
PsA was found to be highly distributed to lung tissues, with the lung-to-serum 
partition coefficients (K(p)) ranging from 49.9 to 60.2. In contrast, PsA 
concentrations in other tissues were either comparable with or less than serum 
concentrations. The high and specific lung targeting characteristics indicates 
that PsA has the potential to be developed as a lung cancer treatment agent.