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The activity of the lipophilic nucleoside derivatives elacytarabine and CP-4126 in a panel of tumor cell lines resistant to nucleoside analogues.

Abstract
The clinical activity of pyrimidine analogues (araC and gemcitabine) is impaired by different mechanisms of resistance and several efforts to overcome this problem have been undertaken. Elacytarabine (CP-4055, araC-5'elaidic acid ester) and CP-4126 (gemcitabine-5'elaidic acid ester) are lipophilic fatty acid derivatives of the nucleoside analogues araC and gemcitabine, respectively, that are currently investigated in clinical trials in solid tumors and hematological malignancies. Here, we present results on the activity of elacytarabine and CP-4126 in a panel of tumor cell lines that are resistant to araC and gemcitabine and we discuss the potential use of these agents in the treatment of patients with drug resistance phenotypes. We conclude that elacytarabine and CP-4126 are active in cells with deficient nucleoside membrane transport and altered mismatch repair. These results should be taking into consideration for future clinical development of elacyatrabine and CP-4126.
AuthorsMarit Liland Sandvold, Carlos Galmarini, Finn Myhren, Godefridus Peters
JournalNucleosides, nucleotides & nucleic acids (Nucleosides Nucleotides Nucleic Acids) Vol. 29 Issue 4-6 Pg. 386-93 (Jun 2010) ISSN: 1532-2335 [Electronic] United States
PMID20544524 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • CP 4126
  • Pyrimidines
  • Cytarabine
  • Deoxycytidine
  • 5'-oleoyl cytarabine
  • pyrimidine
Topics
  • Antineoplastic Agents (chemistry, pharmacology)
  • Caco-2 Cells
  • Cell Line, Tumor
  • Cytarabine (analogs & derivatives, pharmacology)
  • Deoxycytidine (analogs & derivatives, pharmacology)
  • Drug Resistance, Neoplasm (drug effects)
  • HT29 Cells
  • Humans
  • Pyrimidines (chemistry, pharmacology)

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