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FL118, a novel camptothecin derivative, is insensitive to ABCG2 expression and shows improved efficacy in comparison with irinotecan in colon and lung cancer models with ABCG2-induced resistance.

Molecular cancer | 2015

Irinotecan is a camptothecin analogue currently used in clinical practice to treat advanced colorectal cancer. However, acquired resistance mediated by the drug efflux pump ABCG2 is a recognized problem. We reported on a novel camptothecin analogue, FL118, which shows anticancer activity superior to irinotecan. In this study, we sought to investigate the potency of FL118 versus irinotecan or its active metabolite, SN-38, in both in vitro and in vivo models of human cancer with high ABCG2 activity. We also sought to assess the potency and ABCG2 affinity of several FL118 analogues with B-ring substitutions.

Pubmed ID: 25928015 RIS Download

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Associated grants

  • Agency: NCI NIH HHS, United States
    Id: R21 CA180764
  • Agency: NCI NIH HHS, United States
    Id: P30 CA016056
  • Agency: NCI NIH HHS, United States
    Id: CA176937
  • Agency: NCI NIH HHS, United States
    Id: CA180764
  • Agency: NCI NIH HHS, United States
    Id: CA016056
  • Agency: NCI NIH HHS, United States
    Id: R44 CA176937

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