BCL-2 and BTK inhibitors for chronic lymphocytic leukemia: current treatments and overcoming resistance

Expert Rev Hematol. 2024 Nov;17(11):781-796. doi: 10.1080/17474086.2024.2410003. Epub 2024 Oct 6.

Abstract

Introduction: In the last decade, BTK inhibitors and the BCL-2 inhibitor venetoclax have replaced immunochemotherapy in the treatment of CLL.

Areas covered: This review describes the use of BTK inhibitors and BCL2 inhibitors in the treatment of naive and relapsed or refractory CLL, with particular attention to the mechanisms of resistance. It also addresses the management of double-refractory patients, and the discovery of novel drugs. The corpus of papers was obtained by a search of the PubMed and Google Scholar databases for articles in English.

Expert opinion: Covalent BTK inhibitors and venetoclax are commonly recommended for previously-untreated and relapsed/refractory CLL. However, resistance to both drug classes can develop over time. As such, double-refractory patients are difficult to manage and novel approaches are urgently needed.

Keywords: BCL2 inhibitors; BTK degraders; BTK inhibitors; CLL; PI3k inhibitors; cellular therapies; refractory; relapsed.

Publication types

  • Review

MeSH terms

  • Agammaglobulinaemia Tyrosine Kinase* / antagonists & inhibitors
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Bridged Bicyclo Compounds, Heterocyclic* / therapeutic use
  • Drug Resistance, Neoplasm*
  • Humans
  • Leukemia, Lymphocytic, Chronic, B-Cell* / drug therapy
  • Proto-Oncogene Proteins c-bcl-2* / antagonists & inhibitors
  • Proto-Oncogene Proteins c-bcl-2* / metabolism
  • Sulfonamides* / therapeutic use
  • Tyrosine Kinase Inhibitors* / pharmacology
  • Tyrosine Kinase Inhibitors* / therapeutic use

Substances

  • Agammaglobulinaemia Tyrosine Kinase
  • Antineoplastic Agents
  • BCL2 protein, human
  • Bridged Bicyclo Compounds, Heterocyclic
  • BTK protein, human
  • Proto-Oncogene Proteins c-bcl-2
  • Sulfonamides
  • venetoclax
  • Tyrosine Kinase Inhibitors