Potent effects of roniciclib alone and with sorafenib against well-differentiated thyroid cancer

Endocr Relat Cancer. 2018 Oct;25(10):853-864. doi: 10.1530/ERC-18-0150. Epub 2018 Jun 12.

Abstract

Activation of cyclin-dependent kinase activity is frequently observed in many human cancers; therefore, cyclin-dependent kinases that promote cell cycle transition and cell proliferation may be potential targets in the treatment of malignancy. The therapeutic effects of roniciclib, a cyclin-dependent kinase inhibitor for papillary and follicular thyroid cancer (designated as well-differentiated thyroid cancer), were investigated in this study. Roniciclib inhibited cell proliferation in two papillary and two follicular thyroid cancer cell lines in a dose-dependent manner. Roniciclib activated caspase-3 activity and induced apoptosis. Cell cycle progression was arrested in the G2/M phase. Roniciclib treatment in vivo retarded the growth of two well-differentiated thyroid tumors in xenograft models in a dose-dependent fashion. Furthermore, the combination of roniciclib with sorafenib was more effective than either single treatment in a follicular thyroid cancer xenograft model. Acceptable safety profiles appeared in animals treated with either roniciclib alone or roniciclib and sorafenib combination therapy. These findings support roniciclib as a potential drug for the treatment of patients with well-differentiated thyroid cancer.

Keywords: cyclin-dependent kinase; roniciclib; well-differentiated thyroid cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Caspase 3 / metabolism
  • Cell Cycle / drug effects*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Humans
  • Phosphorylation / drug effects
  • Pyrimidines / pharmacology*
  • Signal Transduction / drug effects
  • Sorafenib / pharmacology*
  • Sulfoxides / pharmacology*
  • Thyroid Neoplasms / metabolism
  • Thyroid Neoplasms / pathology*

Substances

  • Antineoplastic Agents
  • Pyrimidines
  • Sulfoxides
  • roniciclib
  • Sorafenib
  • Caspase 3