Synergistic effect of venetoclax and ibrutinib on ibrutinib-resistant ABC-type DLBCL cells

Braz J Med Biol Res. 2024 Oct 7:57:e13278. doi: 10.1590/1414-431X2024e13278. eCollection 2024.

Abstract

Despite the widespread use of R-CHOP therapy in diffuse large B-cell lymphoma (DLBCL), the therapeutic efficacy for this disease remains suboptimal, primarily due to the heterogeneity of refractory and/or relapsed diseases. To address this challenge, optimization of DLBCL treatment regimens has focused on the strategy of combining an additional drug "X" with R-CHOP to enhance efficacy. However, the failure of R-CHOP combined with the BTK inhibitor ibrutinib in treating ABC-type DLBCL patients has raised significant concerns regarding ibrutinib resistance. While some studies suggest that venetoclax may synergize with ibrutinib to kill ibrutinib-resistant cells, the underlying mechanisms remain unclear. Our study aimed to validate the enhanced tumor-suppressive effect of combining ibrutinib with venetoclax against ibrutinib-resistant cells and elucidate its potential mechanisms. Our experimental results demonstrated that ibrutinib-resistant cells exhibited significant cytotoxicity to the combination therapy of ibrutinib and venetoclax, inducing cell apoptosis through activation of the mitochondrial pathway and inhibition of aerobic respiration. Furthermore, we validated the inhibitory effect of this combination therapy on tumor growth in in vivo models. Therefore, our study proposes that the combination therapy of ibrutinib and venetoclax is a promising treatment strategy that can be applied in clinical practice for ABC-type DLBCL, offering a new solution to overcome the urgent challenge of ibrutinib resistance.

MeSH terms

  • Adenine* / analogs & derivatives
  • Adenine* / pharmacology
  • Adenine* / therapeutic use
  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Apoptosis* / drug effects
  • Bridged Bicyclo Compounds, Heterocyclic* / administration & dosage
  • Bridged Bicyclo Compounds, Heterocyclic* / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic* / therapeutic use
  • Cell Line, Tumor
  • Drug Resistance, Neoplasm* / drug effects
  • Drug Synergism*
  • Humans
  • Lymphoma, Large B-Cell, Diffuse* / drug therapy
  • Lymphoma, Large B-Cell, Diffuse* / pathology
  • Mice
  • Piperidines* / pharmacology
  • Pyrazoles* / pharmacology
  • Pyrimidines* / administration & dosage
  • Pyrimidines* / pharmacology
  • Pyrimidines* / therapeutic use
  • Sulfonamides* / administration & dosage
  • Sulfonamides* / pharmacology
  • Sulfonamides* / therapeutic use

Substances

  • ibrutinib
  • venetoclax
  • Bridged Bicyclo Compounds, Heterocyclic
  • Sulfonamides
  • Adenine
  • Piperidines
  • Pyrimidines
  • Pyrazoles
  • Antineoplastic Agents

Grants and funding

This research was supported by the Construction project for the Clinical Medicine Progression of Anhui Medical University in 2022 and the Key Project of Natural Science Fund for Colleges and Universities in Anhui Province (KJ2021A030 and KJ2021A033).