Focus On: Oligonucleotides, Radiolabelling and Metabolism
The design and application of oligonucleotides as therapeutic agents requires a basic understanding of their pharmacokinetic properties and bio-distribution. Radiolabelled tracers play an essential role in developing such an understanding. Pharmaron is the largest provider of custom radiosynthesis services using 14C and tritium and has the capability to synthesize radiolabelled oligonucleotides using traditional and automated synthetic methods.
Pharmaron can assess ADME properties of radiolabelled oligonucleotides by conducting pharmacokinetic, excretion balance and biodistribution studies, including quantitative whole body autoradiography (QWBA) and micro autoradiography (MARG), and has recently demonstrated that high quality pharmacokinetic and tissue distribution data can be obtained following radiolabelling of oligonucleotides with tritium. The PK and tissue disposition of potent oligonucleotides radiolabelled with 14C can also be determined using AMS detection. Pharmaron (formerly Xceleron) developed a novel assay combining different methods of chromatography of separation and detection, SPE, UPLC, AMS, to provide high quality PK data for parent 14C-oligonucleotide in plasma, urine and tissues such as liver and kidney.