An evaluation of palbociclib as a breast cancer treatment option: a current update

Expert Opin Pharmacother. 2021 Feb;22(3):281-290. doi: 10.1080/14656566.2020.1838485. Epub 2020 Nov 16.

Abstract

Introduction: Patients with hormone receptor-positive/HER2-negative (HR+/HER2-) metastatic breast cancer have benefitted from treatment with palbociclib, a cyclin-dependent kinase (CDK) 4/6 inhibitor capable of selectively targeting mechanisms of cell cycle progression that contribute to tumor cell proliferation. Palbociclib use in this setting demonstrates improved progression-free survival when given in combination with aromatase inhibitors or fulvestrant.

Areas covered: The authors describe the current state of research surrounding palbociclib use in breast cancer, present evidence supporting a role for palbociclib in additional subtypes of metastatic breast cancer such as HER2-positive (HER2+) and triple-negative, report ongoing clinical trials aimed at expanding the scope of use for palbociclib, and discuss expected clinical results that will better inform decisions on including palbociclib as a part of breast cancer treatment strategies.

Expert opinion: Preclinical and clinical studies have shown promising evidence for palbociclib use in metastatic HER2+ and androgen receptor-expressing triple-negative breast cancer but mixed results in the adjuvant/neoadjuvant setting, where differences may only be detectable in high-risk disease. Palbociclib combinations may constitute viable replacements for chemotherapy in the neoadjuvant setting as part of de-escalation strategies. Investigation into synergy of palbociclib with immunotherapies is also ongoing based on non-canonical effects of CDK4/6 inhibition on the tumor immune microenvironment.

Keywords: Adjuvant therapy; CDK4/6 inhibitors; HER2-positive breast cancer; HR+HER2- breast cancer; breast cancer; clinical trials; metastatic breast cancer; neoadjuvant therapy; palbociclib; triple-negative breast cancer.

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols
  • Breast Neoplasms* / drug therapy
  • Cyclin-Dependent Kinase 4
  • Humans
  • Piperazines / therapeutic use
  • Protein Kinase Inhibitors / therapeutic use
  • Pyridines / therapeutic use
  • Receptor, ErbB-2
  • Tumor Microenvironment

Substances

  • Piperazines
  • Protein Kinase Inhibitors
  • Pyridines
  • Receptor, ErbB-2
  • Cyclin-Dependent Kinase 4
  • palbociclib