Therapeutic activity of 1-beta-D-arabinofuranosylcytosine conjugates of lipids in WEHI-3B leukemia in mice.

Two new conjugates of 1-beta-D-arabinofuranosylcytosine (ara-C) and lipids were tested for therapeutic activity in myelomonocytic WEHI-3B leukemia in mice. Both conjugates were superior to equimolar mixtures of their respective parent compounds and to ara-C alone. IP treatment was found effective after either IP or IV transplantation of the leukemia. The thioether-linked lipid conjugate ara-CDP-D,L-PTBA showed considerably higher efficacy than the ester-linked lipid conjugate ara-CDP-L-dipalmitin. The optimal therapeutic regimen of ara-CDP-D,L-PTBA consisted of 60 mg/kg given IP qd 1-5 after transplantation of the WEHI-3B leukemia.