Enhanced efficacy of CKD-516 in combination with doxorubicin: pre-clinical evaluation using a hepatocellular carcinoma xenograft model

Anticancer Res. 2014 Apr;34(4):1715-22.

Abstract

Aim: To evaluate the anticancer efficacy of CKD-516, a novel vascular-disrupting agent, alone and in combination with doxorubicin in the treatment of hepatocellular carcinoma (HCC).

Materials and methods: In mice bearing luciferized HCC cells, therapeutic efficacy was assessed for seven days after single administration of CKD-516, doxorubicin, or combination of CKD-516 and doxorubicin.

Results: Bioluminescence-imaging (BLI) signals in the CKD-516 group abruptly decreased initially, but recovered at seven days after treatment. BLI signals in the doxorubicin group gradually decreased over the 7-day period. In the combination group, BLI signals were abruptly reduced and remained suppressed for the 7-day period. On histopathological examination, CKD-516-treated tumors showed extensive central necrosis, whereas the peripheral layers remained viable. Doxorubicin-treated tumors showed mild and scattered necrosis. Tumors from the combination group showed more extensive central and peripheral necrosis, with smaller viable peripheral layers than the CKD-516 group.

Conclusion: Combination therapy can have additive effects for treatment of HCC compared with CKD-516 or doxorubicin monotherapy.

Keywords: CKD-516; doxorubicin; hepatocellular carcinoma; tubulin-binding agents; vascular-disrupting agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Benzophenones / administration & dosage
  • Benzophenones / pharmacology*
  • Carcinoma, Hepatocellular / drug therapy
  • Carcinoma, Hepatocellular / pathology*
  • Cell Line, Tumor
  • Disease Models, Animal
  • Doxorubicin / administration & dosage
  • Doxorubicin / pharmacology*
  • Drug Evaluation, Preclinical
  • Drug Synergism
  • Humans
  • Liver Neoplasms / drug therapy
  • Liver Neoplasms / pathology*
  • Mice
  • Necrosis
  • Neovascularization, Pathologic / drug therapy
  • Tumor Burden / drug effects
  • Valine / administration & dosage
  • Valine / analogs & derivatives*
  • Valine / pharmacology
  • Xenograft Model Antitumor Assays

Substances

  • Benzophenones
  • N-(4-(3-(1H-1,2,4-triazol-1-yl)-4-(3,4,5-trimethoxybenzoyl)phenyl)thiazol-2-yl)-2-amino-3-methylbutanamide
  • Doxorubicin
  • Valine