Potential synergistic anti-tumor activity between lenalidomide and sorafenib in hepatocellular carcinoma

J Gastroenterol Hepatol. 2014 Dec;29(12):2021-31. doi: 10.1111/jgh.12708.

Abstract

Background and aim: The immune modulatory drug lenalidomide has shown promising anti-tumor activity in a clinical trial of patients with advanced hepatocellular carcinoma (HCC). The present study explored whether lenalidomide can enhance the anti-tumor activity of sorafenib, the standard molecular targeted therapy for HCC.

Methods: The anti-tumor efficacy of single-agent or combination treatment was measured by change in tumor volume and animal survival using an orthotopic liver cancer model. Distribution of T-cell subpopulations in tumor-infiltrating lymphocytes (TILs) and splenocytes derived from tumor-implanted mice was measured by flow cytometry. Depletion of relevant T-cell subpopulations or cytokines was done by co-administration of relevant antibodies with study drug treatment. Tumor cell apoptosis and tumor angiogenesis were measured by transferase deoxytidyl uridine end labeling assay and immunohistochemical study, respectively.

Results: Combination of sorafenib and lenalidomide produced significant synergistic anti-tumor efficacy in terms of tumor growth delay and animal survival. This synergistic effect was associated with a significant increase in interferon-γ expressing CD8(+) lymphocytes in TILs and a significantly higher number of granzyme- or perforin-expressing CD8(+) T cells, compared with vehicle- or single-agent treatment groups. Combination treatment significantly increased apoptotic tumor cells and vascular normalization in tumor tissue. The synergistic anti-tumor effect was abolished after CD8 depletion.

Conclusions: Lenalidomide can enhance the anti-tumor effects of sorafenib in HCC through its immune modulatory effects, and CD8(+) TILs play an important role in the anti-tumor synergism.

Keywords: immune modulatory; lenalidomide; sorafenib; tumor-infiltrating lymphocytes; vascular normalization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use*
  • CD8-Positive T-Lymphocytes / immunology
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / immunology
  • Carcinoma, Hepatocellular / pathology*
  • Disease Models, Animal
  • Drug Synergism
  • Drug Therapy, Combination
  • Humans
  • Immunologic Factors / pharmacology*
  • Immunologic Factors / therapeutic use*
  • Interferon-gamma
  • Lenalidomide
  • Liver Neoplasms / drug therapy*
  • Liver Neoplasms / immunology
  • Liver Neoplasms / pathology*
  • Mice
  • Niacinamide / analogs & derivatives*
  • Niacinamide / pharmacology
  • Niacinamide / therapeutic use
  • Phenylurea Compounds / pharmacology*
  • Phenylurea Compounds / therapeutic use*
  • Sorafenib
  • T-Lymphocyte Subsets
  • Thalidomide / analogs & derivatives*
  • Thalidomide / pharmacology
  • Thalidomide / therapeutic use

Substances

  • Antineoplastic Agents
  • Immunologic Factors
  • Phenylurea Compounds
  • Niacinamide
  • Thalidomide
  • Interferon-gamma
  • Sorafenib
  • Lenalidomide