Trametinib boosts palbociclib's efficacy in breast cancer via autophagy inhibition

Oncol Res. 2024 Jun 20;32(7):1197-1207. doi: 10.32604/or.2024.046139. eCollection 2024.

Abstract

Breast cancer, a predominant global health issue, requires ongoing exploration of new therapeutic strategies. Palbociclib (PAL), a well-known cyclin-dependent kinase (CDK) inhibitor, plays a critical role in breast cancer treatment. While its efficacy is recognized, the interplay between PAL and cellular autophagy, particularly in the context of the RAF/MEK/ERK signaling pathway, remains insufficiently explored. This study investigates PAL's inhibitory effects on breast cancer using both in vitro (MCF7 and MDA-MB-468 cells) and in vivo (tumor-bearing nude mice) models. Aimed at elucidating the impact of PAL on autophagic processes and exploring the potential of combining it with trametinib (TRA), an MEK inhibitor, our research seeks to address the challenge of PAL-induced drug resistance. Our findings reveal that PAL significantly decreases the viability of MCF7 and MDA-MB-468 cells and reduces tumor size in mice while showing minimal cytotoxicity in MCF10A cells. However, PAL also induces protective autophagy, potentially leading to drug resistance via the RAF/MEK/ERK pathway activation. Introducing TRA effectively neutralized this autophagy, enhancing PAL's anti-tumor efficacy. A combination of PAL and TRA synergistically reduced cell viability and proliferation, and in vivo studies showed notable tumor size reduction. In conclusion, the PAL and TRA combination emerges as a promising strategy for overcoming PAL-induced resistance, offering a new horizon in breast cancer treatment.

Keywords: MCF7; MDA-MB-468; Palbociclib; Protective autophagy; RAF/MEK/ERK; Trametinib.

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Autophagy* / drug effects
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / metabolism
  • Breast Neoplasms* / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Drug Resistance, Neoplasm / drug effects
  • Drug Synergism
  • Female
  • Humans
  • MAP Kinase Signaling System / drug effects
  • MCF-7 Cells
  • Mice
  • Mice, Nude
  • Piperazines* / pharmacology
  • Piperazines* / therapeutic use
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Pyridines* / pharmacology
  • Pyridines* / therapeutic use
  • Pyridones* / pharmacology
  • Pyridones* / therapeutic use
  • Pyrimidinones* / pharmacology
  • Pyrimidinones* / therapeutic use
  • Xenograft Model Antitumor Assays*

Substances

  • palbociclib
  • Pyridines
  • Pyridones
  • Pyrimidinones
  • trametinib
  • Piperazines
  • Protein Kinase Inhibitors