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Preclinical antitumor activity of CI-973,[SP-4-3-(R)]-[1,1-cyclobutanedicarboxylato(2-)] (2 methyl-1,4-butane-diamine-N,N′)platinum

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Summary

The antitumor activity of [SP-4-3-(R)]-[1,1-cyclobutanedicarboxylato-(2-)](2 methyl-1,4-butanediamine-N,N′)platinum (CI-973) was characterized in a number of preclinical model systems. CI-973 retained substantial activity in cisplatin resistant murine leukemia cell lines, in vitro and in vivo; in L1210 leukemia resistant to cisplatin in vivo, CI-973 retained as much activity as was found in animals bearing sensitive L1210 leukemia. When compared in five solid murine tumors in vivo, both CI-973 and cisplatin were approximately equivalent in activity. In one human colon tumor and one human non-small cell lung carcinoma tested as xenografts in immunodeficient mice, cisplatin and CI-973 were ineffective. In two other human non-small cell lung carcinomas tested in the same fashion, cisplatin did possess activity. CI-973 has entered phase I clinical trials.

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Authors and Affiliations

  1. Cancer Research Section, Parke-Davis Pharmaceutical, Research Division Warner-Lambert Company, 48105, Ann Arbor, MI, USA

    Alan J. Kraker, Charles W. Moore, Billy J. Roberts, Wilbur R. Leopold & William L. Elliott

Authors
  1. Alan J. Kraker
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  2. Charles W. Moore
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  3. Billy J. Roberts
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  4. Wilbur R. Leopold
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  5. William L. Elliott
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Additional information

A portion of this work was reported in a preliminary form at the 79th Annual Meeting of the American Association for Cancer Research, Proc. AACR 29:344, 1988.

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Kraker, A.J., Moore, C.W., Roberts, B.J. et al. Preclinical antitumor activity of CI-973,[SP-4-3-(R)]-[1,1-cyclobutanedicarboxylato(2-)] (2 methyl-1,4-butane-diamine-N,N′)platinum. Invest New Drugs 9, 1–8 (1991). https://doi.org/10.1007/BF00194538

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  • DOI: https://doi.org/10.1007/BF00194538

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