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Influence of 1-ß-D-Arabinofuranosylcytosine Conjugates of Lipids on the Growth and Metastasis of Lewis Lung Carcinoma

Division of Hematology and Oncology, Department of Medicine, Emory University School of Medicine, Atlanta, Georgia [W. E. B., A. R., W. R. V.]; Division of Hematology and Oncology, Department of Medicine I [S. D., H. D. S., J. R.] and Department of Medical Statitics and Epidemiology [R. B.], Technische Universität München, 8000 Munich 80, Federal Republic of Germany; Department of Neurosurgery, Roswell Park Memorial Institute, Buffalo, New York, [C. I. H.]

Five different lipid conjugates of 1-ß-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.

¹ Recipient of Grant Be 822/2–4 and a Heisenberg-Stipendium from Deutsche Forschungsgemeinschaft. To whom requests for reprints should be addressed, at Division of Hematology/Oncology, Department of Medicine, Emory University School of Medicine, 718 Woodruff Memorial Building, Atlanta, GA 30322.

² Recipient of Grant CA 29850-04 Al from the National Cancer Institute.

Received 4/ 2/87. Revised 7/15/87. Revised 10/29/87. Accepted 11/18/87.

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