METABOLISM AND PHARMACOKINETICS OF DIBROMODULCITOL (DBD, NSC-104800) IN MAN .1. METABOLITES OF DBD

Dibromodulcitol (DBD) labelled with 3H or 82Br was administered orally to patients with advanced cancer. Chromatographic studies on plasma and urine showed the presence of unchanged DBD and 10 metabolites. Steady excretion of 1,2:5,6-dianhydrogalactitol (DAG) the most active alkylating derivative, as a minor component of the urine for a few days, indicates its persistence at low levels in the systemic circulation. In the urine, 4% of the drug was excreted as unchanged DBD, 9% as bromoepoxy-dulcitol (BrEpD) and 25-30% in the form of unidentified bromine-containing metabolites. Administration of DBD results in the simultaneous presence of 3 main alkylating agents (DBD, Bromoepoxide and DAG) with different transport characteristics. The less reactive parent drug and the bromoepoxide may reach different sites and serve as depots from which DAG is gradually released in low concentrations. © 1979.