Synergistic antitumor effects of lenalidomide and rituximab on mantle cell lymphoma in vitro and in vivo

Am J Hematol. 2009 Sep;84(9):553-9. doi: 10.1002/ajh.21468.

Abstract

Rituximab (RTX), a chimeric anti-CD20 antibody, is associated with direct induction of apoptosis and antibody-dependent cell-mediated cytotoxicity (ADCC) with clinical efficacy in mantle cell lymphoma (MCL). Lenalidomide (LEN), a novel immunomodulatory agent, sensitizes tumor cells and enhances ADCC. Our study attempted to elucidate the mechanism of LEN-enhanced RTX-mediated cytotoxicity of MCL cells. We found that LEN and RTX induced growth inhibition of both cultured and fresh primary MCL cells. LEN enhanced RTX-induced apoptosis via upregulating phosphorylation of c-Jun N-terminal protein kinases (JNK), Bcl-2, Bad; increasing release of cytochrome-c; enhancing activation of caspase-3, -8, -9 and cleavage of PARP. Meanwhile, LEN activated NK cells and increased CD16 expression on CD56(low)CD16(+) NK cells. Whole PBMCs but not NK cell-depleted PBMCs treated with LEN augmented 30% of RTX-dependent cytotoxicity. Daily treatment with LEN increased NK cells by 10-folds in SCID mice, and combination of LEN and RTX decreased tumor burden and prolonged survival of MCL-bearing SCID mice. Taken together, our study demonstrates that LEN plus RTX provides a synergistically therapeutic effect on MCL cells by enhancing apoptosis and RTX-dependent NK cell-mediated cytotoxicity and may be an optimal combination in the clinical trial of relapsed or refractory MCL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / administration & dosage
  • Antibodies, Monoclonal / pharmacology
  • Antibodies, Monoclonal, Murine-Derived
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Apoptosis / drug effects
  • Apoptosis Regulatory Proteins / metabolism
  • Blood Cells / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Drug Synergism
  • Humans
  • Killer Cells, Natural / drug effects
  • Lenalidomide
  • Leukocytes, Mononuclear / drug effects
  • Lymphoma, Mantle-Cell / drug therapy*
  • Lymphoma, Mantle-Cell / pathology
  • MAP Kinase Kinase 4 / metabolism
  • Mice
  • Mice, SCID
  • Neoplasms, Experimental / drug therapy
  • Phosphorylation / drug effects
  • Rituximab
  • Thalidomide / administration & dosage
  • Thalidomide / analogs & derivatives
  • Thalidomide / pharmacology

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Murine-Derived
  • Apoptosis Regulatory Proteins
  • Rituximab
  • Thalidomide
  • MAP Kinase Kinase 4
  • Lenalidomide