Assays were developed for determination of DE-310, a carboxymethyldextran polyalcohol conjugate of the topoisomerase I inhibitor DX-8951 (exatecan) and two enzymatic products (i.e. glycyl-DX-8951 and unconjugated DX-8951) in human whole blood, erythrocytes and saliva. Sample pretreatment involved a single protein-precipitation step, followed by a thermolysin-mediated deconjugation for the parent molecule. Separation of the compounds was achieved on an Inertsil ODS-80A column (150mm×4.6mm i.d.; 5μm PS), using isocratic elution. The column effluent was monitored at excitation and emission wavelengths of 375 and 445nm, respectively. Validation results indicated that the methods are accurate and precise at lower limits of quantitation of 0.5-6.9ng/ml. The methods were used to study the blood distribution and salivary concentrations in patients receiving DE-310.

Camptothecin, DE-310
dx.doi.org/10.1016/j.jchromb.2003.09.047, hdl.handle.net/1765/64223
Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Department of Medical Oncology

Soepenberg, O, de Bruijn, P.J, Verweij, J, Atsumi, R, & Sparreboom, A. (2004). Liquid chromatographic assays for DE-310, a novel camptothecin analog, and two major enzymatic products in human matrices. Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences, 799(1), 15–22. doi:10.1016/j.jchromb.2003.09.047