Invivo pharmacokinetics of the antitumor agent 4,6-benzylidene-d-glucose (bg) and a deuterated analog 4,6-benzylidene-d1-d-glucose (p-1013) in mice, rats and dogs.

In vivo pharmacokinetics of the antitumour agent 4,6-benzylidene-D-glucose (BG) and a deuterated analog 4,6-benzylidene-d1-D-glucose (P-1013) were investigated in athymic mice, Beagle dogs and Wistar rats following i.v. administration of the compounds. Reverse-phase high performance liquid chromatography (HPLC) was used to quantitate drug and metabolite content in plasma samples. No difference in the half-life (t1/2) for BG and P-1013 was observed in any of the three species, the half-lives were on the order of 10 min. Metabolism of BG and P-1013 leads to formation of undeuterated and deuterated 1,3-benzylidene-D-glucitol, respectively, as the only detectable metabolites. The half-lives of these metabolites were also measured and were found to differ between rats given undeuterated and deuterated drug. In mice and dogs the t1/2 was the same for deuterated and undeuterated 1,3-benzylidene-D-glucitol.