Application of novel quantitative bioanalytical methods for pharmacokinetic and pharmacokinetic/pharmacodynamic assessments of antisense oligonucleotides.

The development of antisense therapeutic agents has required the development of a number of novel bioanalytical methods for their quantitation. The success of these methods has enabled characterization of the pharmacokinetic and pharmacokinetic/ pharmacodynamic behavior of antisense agents. Specific quantitative bioanalytical methods addressed in this review include radiotracer methods, high-performance liquid chromatography (HPLC) methods, capillary gel electrophoresis with UV detection or with laser-induced fluorescence detection, matrix-assisted laser-induced desorption/ionization mass spectrometry, HPLC-mass spectrometry, and hybridization-based enzyme-linked immunosorbent assays. The most important bioanalytical techniques have been summarized in view of their general and specific features, the possibilities and extent of their application, and characteristics of operation and limitations.