Exploring the feasibility of using the DBS technique for metabolite radioprofiling.

BACKGROUND

The dried blood spots (DBS) technique has been actively evaluated as plasma replacement for monitoring drug exposure to support drug development in preclinical/clinical pharmacokinetic and toxicokinetic studies. Plasma samples from some of these studies are typically used for metabolite profiling and identification and for determination of disproportionate metabolites between safety species and humans to address metabolites in safety testing issues. The objectives of this study were to explore the feasibility of using the DBS technique for a metabolism study and to compare metabolite radioprofiles between DBS, plasma and whole blood samples.

RESULTS

The radioactivity extraction recovery in DBS samples was similar or better than that in plasma or whole blood. The metabolite radioprofiles in AUC pooled DBS samples using FTA(®) and FTA(®) Elute cards were comparable to those in AUC pooled plasma and whole blood.

CONCLUSION

It is feasible to use DBS as an alternative matrix to plasma for in vivo metabolite radioprofiling studies for SA-1.