Five different lipid conjugates of 1-β-d-arabinofuranosylcytosine (ara-C) were tested for their therapeutic activity on the growth and metastasis of Lewis lung carcinoma (3-LL). Among 1 ester-linked lipid conjugate (Ara-CDP-l-dipalmitin), 3 1-O-alkyl-lipid conjugates (ara-CDP-d,l-PBA, ara-CDP-d,l-PCA, ara-CDP-d,l-MBA) and a thioether-lipid conjugate (ara-CDP-d,l-PTBA) ara-CDP-d,l-PTBA, ara-CDP-d,l-PBA, and ara-CDP-l-dipalmitin produced the strongest tumor growth inhibition and increase of surviving animals in C57Bl6-mice bearing i.p.-implanted 3-LL. Furthermore these conjugates were superior to the parent compounds alone, or equimolar mixtures of the alkyllysophospholipid derivatives ET-18-OCH3 and ara-C. Successful therapeutic regimen consisted of 80–100 mg conjugate/kg, given i.p. daily for five consecutive days.

Similar regimen injected shortly after the surgical removal of the primary tumor as adjuvant chemotherapy inhiibited the metastasis of 3-LL to the lungs of the animals as demonstrated by an increase of survival time and the number of surviving animals.

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©1988 American Association for Cancer Research.
1988
American Association for Cancer Research, Inc.