Palbociclib overcomes afatinib resistance in non-small cell lung cancer

Biomed Pharmacother. 2019 Jan:109:1750-1757. doi: 10.1016/j.biopha.2018.10.170. Epub 2018 Nov 21.

Abstract

As a Second generation tyrosine kinase inhibitor (TKI), afatinib is approved to treat advanved/metastatic EGFR-mutant NSCLC (non-small cell lung cancer). However, the clinical application of afatinib is limited via acquired resistance. It has been revealed that CDK4/6 inhibitors hinder proliferation of cells and bring about differentiation as well as death of multiple malignant cells not only in vivo but also in vitro. Our research investigated whether a combination of Palbociclib with afatinib treatment was able to reverse acquired resistance with regard to NSCLC cells. The findings of our research demonstrated that combined Palbociclib and afatinib treatment exerted synergism in decreasing survival of cells with acquired resistance. Furthermore, combined Palbociclib with afatinib attenuated resistance that brings about recurrence of malignancies in xenografts with acquired resistance. In summary, the combination of Palbociclib and afatinib serves as an innovative strategy to reverse the acquired AR in pulmonary malignancies.

Keywords: Afatinib; Drug resistance; NSCLC cells; Palbociclib; RB.

MeSH terms

  • Afatinib / pharmacology*
  • Afatinib / therapeutic use
  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Carcinoma, Non-Small-Cell Lung / drug therapy
  • Carcinoma, Non-Small-Cell Lung / pathology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Proliferation / physiology
  • Dose-Response Relationship, Drug
  • Drug Resistance, Neoplasm / drug effects*
  • Drug Resistance, Neoplasm / physiology
  • Female
  • Humans
  • Lung Neoplasms / drug therapy
  • Lung Neoplasms / pathology*
  • Mice
  • Mice, Nude
  • Piperazines / pharmacology*
  • Piperazines / therapeutic use
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use
  • Pyridines / pharmacology*
  • Pyridines / therapeutic use
  • Tumor Burden / drug effects
  • Tumor Burden / physiology
  • Xenograft Model Antitumor Assays / methods

Substances

  • Antineoplastic Agents
  • Piperazines
  • Protein Kinase Inhibitors
  • Pyridines
  • Afatinib
  • palbociclib