Combination of rituximab and mammalian target of rapamycin inhibitor everolimus (RAD001) in diffuse large B-cell lymphoma

Leuk Lymphoma. 2014 May;55(5):1151-7. doi: 10.3109/10428194.2013.823492. Epub 2013 Aug 28.

Abstract

Abstract We evaluated the efficacy of the anti-CD20 monoclonal antibody rituximab in combination with the mammalian target of rapamycin (mTOR) inhibitor everolimus for treating diffuse large B-cell lymphoma (DLBCL). The combination of rituximab and everolimus was more effective for inhibiting cell growth compared with single-agent therapy. An increase in G0/G1 cell cycle arrest and an increased population of cells in apoptosis were observed in the combination treatment group. The addition of rituximab reduced the overexpression of p-AKT caused by the negative feedback loop of everolimus and had an enhanced effect on inhibition of mTOR signaling, thus providing a rationale for this synergistic effect. Furthermore, combination treatment was also more effective than treatment with either agent alone for inhibiting the growth of DLBCL xenografts. Our study provides preclinical evidence and a theoretical basis for combination therapy with rituximab and everolimus in DLBCL.

MeSH terms

  • Animals
  • Antibodies, Monoclonal, Murine-Derived / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Apoptosis
  • Cell Cycle / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Disease Models, Animal
  • Drug Synergism
  • Everolimus
  • Humans
  • Lymphoma, Large B-Cell, Diffuse / drug therapy
  • Lymphoma, Large B-Cell, Diffuse / metabolism*
  • Lymphoma, Large B-Cell, Diffuse / pathology*
  • Mice
  • Mice, Nude
  • Rituximab
  • Signal Transduction / drug effects
  • Sirolimus / analogs & derivatives*
  • Sirolimus / pharmacology
  • TOR Serine-Threonine Kinases / antagonists & inhibitors*
  • TOR Serine-Threonine Kinases / metabolism
  • Tumor Burden
  • Xenograft Model Antitumor Assays

Substances

  • Antibodies, Monoclonal, Murine-Derived
  • Antineoplastic Agents
  • Rituximab
  • Everolimus
  • TOR Serine-Threonine Kinases
  • Sirolimus