N-Trifluoroacetyladriamycin-14-valerate (
AD 32) is an analog of
doxorubicin whose chemico-physical characteristics are nontypical compared to the parent compound. Its most interesting feature is the lack of capacity to intercalate with
DNA; thus, its mechanism of action as an antitumoral
drug is still unknown. The N-trifluoroacetyl bond on the
glycoside moiety is very stable and does not easily undergo enzymatic hydrolysis. Conversely, the
valerate ester is split very rapidly by tissue and blood
hydrolases. In this paper we present a kinetic study on
AD 32, and we additionally follow the formation and disappearance of its metabolite,
N-trifluoroacetyladriamycin (
AD 41). Peak levels, areas under the curve, and beta-half-lives of
AD 32 and
AD 41 after an iv injection of 80 mg/kg of
AD 32 to
Lewis lung carcinoma-bearing mice are presented. The results indicated very rapid disappearance of
AD 32 from blood and tissues, whereas AD 42 persisted for much longer. Moreover, all of the tissues taken into consideration were able to hydrolyze
AD 32 to
AD 41, suggesting that this compound plays an important role in the antitumoral activity of
AD 32.