Tyrosine kinase inhibition to improve anthracycline-based chemotherapy efficacy in T-cell lymphoma

Br J Cancer. 2019 Oct;121(7):567-577. doi: 10.1038/s41416-019-0557-8. Epub 2019 Sep 2.

Abstract

Background: Anthracycline-containing regimens, namely cyclophosphamide, doxorubicin, vincristine and prednisone (CHOP) or CHOEP (CHOP + etoposide), represent the current standard of care for patients with newly diagnosed peripheral T-cell lymphomas (PTCLs), although responses are unsatisfactory. In this study, we investigated the pathways able to mitigate the sensitivity to CHOP-based regimens in preclinical models of T-cell lymphoma (TCL) to select agents for the development of CHOP-based drug combinations.

Methods: We performed gene expression profiling of malignant T-cell lines exposed to CHOEP; flow cytometry was employed to study the effects of drug combinations on cell viability, cell cycle distribution, apoptosis and mitochondrial membrane depolarisation. Western blot analyses were performed to study cell signalling downstream of the T-cell receptor and apoptosis. The in vivo effect of the drug combination was tested in xenograft models.

Results: We highlighted a modulation of tyrosine kinases belonging to the T-cell receptor pathway upon chemotherapy that provided the rationale for combining the tyrosine kinase inhibitor dasatinib with CHOEP. Dasatinib improves CHOEP activity and reduces viability in vitro. Furthermore, combination treatment results in tumour growth inhibition in in vivo xenograft mouse models.

Conclusions: Our data provide the rationale for clinical testing of the dasatinib-CHOEP combination in patients with T-cell lymphoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / administration & dosage
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Apoptosis
  • Cell Cycle / drug effects
  • Cell Survival
  • Cyclophosphamide / administration & dosage
  • Dasatinib / administration & dosage
  • Doxorubicin / administration & dosage
  • Drug Administration Schedule
  • Drug Synergism
  • Etoposide / administration & dosage
  • Gene Expression / drug effects
  • Gene Expression Profiling
  • Humans
  • Jurkat Cells
  • Lymphoma, T-Cell / drug therapy*
  • Lymphoma, T-Cell / genetics
  • Lymphoma, T-Cell / metabolism
  • Mice, Inbred NOD
  • Mice, SCID
  • Prednisone / administration & dosage
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Protein-Tyrosine Kinases / metabolism
  • Proto-Oncogene Proteins c-fyn / genetics
  • Receptors, Antigen, T-Cell / drug effects*
  • Receptors, Antigen, T-Cell / metabolism
  • Treatment Outcome
  • Up-Regulation / drug effects
  • Vincristine / administration & dosage
  • rhoA GTP-Binding Protein / genetics

Substances

  • Protein Kinase Inhibitors
  • Receptors, Antigen, T-Cell
  • RHOA protein, human
  • Vincristine
  • Etoposide
  • Doxorubicin
  • Cyclophosphamide
  • Protein-Tyrosine Kinases
  • FYN protein, human
  • Proto-Oncogene Proteins c-fyn
  • rhoA GTP-Binding Protein
  • Dasatinib
  • Prednisone

Supplementary concepts

  • CHOP protocol