RAD001 (everolimus) inhibits tumour growth in xenograft models of human hepatocellular carcinoma

J Cell Mol Med. 2009 Jul;13(7):1371-80. doi: 10.1111/j.1582-4934.2008.00364.x. Epub 2008 May 7.

Abstract

Hepatocellular carcinoma (HCC) is the fifth most common malignancy worldwide and highly resistant to available chemotherapies. Mammalian target of rapamycin (mTOR) functions to regulate protein translation, angiogenesis and cell cycle progression in many cancers including HCC. In the present study, subcutaneous patient-derived HCC xenografts were used to study the effects of an mTOR inhibitor, RAD001 (everolimus), on tumour growth, apoptosis and angiogenesis. We report that oral administration of RAD001 to mice bearing patient-derived HCC xenografts resulted in a dose-dependent inhibition of tumour growth. RAD001-induced growth suppression was associated with inactivation of downstream targets of mTOR, reduction in VEGF expression and microvessel density, inhibition of cell proliferation, up-regulation of p27(Kip1) and down-regulation of p21(Cip1/Waf1), Cdk-6, Cdk-2, Cdk-4, cdc-25C, cyclin B1 and c-Myc. Our data indicate that the mTOR pathway plays an important role in angiogenesis, cell cycle progression and proliferation of liver cancer cells. Our study provides a strong rationale for clinical investigation of mTOR inhibitor RAD001 in patients with HCC.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis
  • Body Weight
  • Carcinoma, Hepatocellular / blood
  • Carcinoma, Hepatocellular / drug therapy*
  • Cell Cycle Proteins / metabolism
  • Cell Proliferation
  • Everolimus
  • Humans
  • Liver Neoplasms / blood
  • Liver Neoplasms / drug therapy*
  • Male
  • Mice
  • Mice, SCID
  • Microvessels / pathology
  • Phosphorylation
  • Protein Kinases / metabolism
  • Sirolimus / analogs & derivatives*
  • Sirolimus / therapeutic use
  • TOR Serine-Threonine Kinases
  • Vascular Endothelial Growth Factor A / blood
  • Xenograft Model Antitumor Assays*

Substances

  • Cell Cycle Proteins
  • Vascular Endothelial Growth Factor A
  • Everolimus
  • Protein Kinases
  • MTOR protein, human
  • mTOR protein, mouse
  • TOR Serine-Threonine Kinases
  • Sirolimus