Antitumor effect of 1-beta-D-arabinofuranosylcytosine 5'-adamantoate (NSC 117614) in L1210 leukemic mice.

Abstract

The effects of a new derivative of 1-β-D-arabinofuranosylcytosine (ara-C), NSC 63878, 1-β-D-arabinofuranosylcytosine 5′-adamantoate, NSC 117614 (AdO-ara-C), on the survival of L1210 leukemic mice was studied. In all the treatment schedules investigated (single doses, short courses of daily doses, and widely spaced doses), AdO-ara-C was therapeutically more effective than ara-C. For a given total dose, the effectiveness of AdO-ara-C was relatively insensitive to the schedule used. Single dose therapy with AdO-ara-C was almost as effective as therapy with ara-C on an “optimum” schedule (courses of multiple closely spaced doses with appropriate intervals for host recovery). AdO-ara-C was effective when administered i.p. or s.c. The agent is active even when administered as much as 48 hr prior to tumor inoculation. This and other data ( e.g. , lack of reversal in vivo by deoxycytidine) suggest a sustained action effect. The results are discussed in terms of this hypothesis.