In vitro cytotoxicity of nelarabine, clofarabine and flavopiridol in paediatric acute lymphoblastic leukaemia

Br J Haematol. 2007 Apr;137(2):109-16. doi: 10.1111/j.1365-2141.2007.06527.x.

Abstract

The in vitro efficacies of three new drugs--clofarabine (CLOF), nelarabine (NEL) and flavopiridol (FP) - were assessed in a panel of acute lymphoblastic leukaemia (ALL) cell lines. The 50% inhibitory concentration (IC50) for CLOF across all lines was 188-fold lower than that of NEL. B-lineage, but not T-lineage lines, were >7-fold more sensitive to CLOF than cytosine arabinoside (ARAC). NEL IC50 was 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells were eightfold more sensitive to NEL than B-lineage but there was considerable overlap. FP was more potent in vitro than glucocorticoids and thiopurines and at doses that recent phase I experience predicts will translate into clinical efficacy. Potential cross-resistance of CLOF, NEL and FP was observed with many front-line ALL therapeutics but not methotrexate or thiopurines. Methotrexate sensitivity was inversely related to that of NEL and FP. Whilst NEL was particularly effective in T-ALL, a subset of patients with B-lineage ALL might also be sensitive. CLOF appeared to be marginally more effective in B-lineage than T-ALL and has a distinct resistance profile that may prove useful in combination with other compounds. FP should be widely effective in ALL if sufficient plasma levels can be achieved clinically.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine Nucleotides / pharmacology
  • Antineoplastic Agents / pharmacology*
  • Arabinonucleosides / pharmacology
  • Burkitt Lymphoma / pathology
  • Child
  • Clofarabine
  • Dose-Response Relationship, Drug
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Flavonoids / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Leukemia-Lymphoma, Adult T-Cell / pathology
  • Piperidines / pharmacology
  • Precursor Cell Lymphoblastic Leukemia-Lymphoma / pathology*
  • Tumor Cells, Cultured

Substances

  • Adenine Nucleotides
  • Antineoplastic Agents
  • Arabinonucleosides
  • Flavonoids
  • Piperidines
  • alvocidib
  • nelarabine
  • Clofarabine