Anti-BCL2 Phosphorothioate G3139 Clinical Pharmacology: Plasma Levels During Contwous Subcutaneous Infusion by HPLC Assay

Abstract An HPLC assay has been developed to determine plasma levels of G3139 - a 18mer phosphorothioate oligonucleotide currently in Phase I clinical studies. The assay utilizes anion exchange microchromatography, aqueous LiBr gradient elution, and UV absorbance detection. Minimum sensitivity of approximately 0.2 μg/ml plasma, or 35 nM of G3139, has been achieved. Analysis of preliminary clinical samples indicates subcutaneous infusion of G3139 at 2 mg/kg/day gives rise to steady state plasma levels of 1–2 μg/ml.