After a CDK4/6 Inhibitor: State of the Art in Hormone Receptor-Positive Metastatic Breast Cancer

Am Soc Clin Oncol Educ Book. 2025 Jun;45(3):e473372. doi: 10.1200/EDBK-25-473372. Epub 2025 Jun 20.

Abstract

CDK 4/6 inhibitors (CDK4/6i) remain part of the standard first-line treatment for patients with hormone receptor-positive metastatic breast cancer, offering demonstrable improvements in both progression-free survival and overall survival. However, resistance inevitably develops, and the optimal treatment sequencing after CDK4/6i progression remains undefined. Tumor heterogeneity and diverse resistance mechanisms-including alterations in ESR1 and PIK3CA-complicate treatment decisions in the post-CDK4/6i setting. Genomic profiling has helped to characterize these and other clinically relevant alterations, uncovering new avenues for therapeutic intervention. Building on these insights, a growing number of novel endocrine agents, phosphoinositide-3-kinase/AKT pathway-targeted therapies, and antibody-drug conjugates (ADCs) have demonstrated efficacy in biomarker-selected populations and are reshaping the treatment landscape beyond CDK4/6i progression. This chapter reviews current standards of care, emerging therapeutic options, and evolving combination strategies across biomarker-defined subgroups. We also highlight how ongoing clinical trials and advances in molecular profiling are informing personalized approaches to overcome endocrine resistance and improve patient outcomes.

Publication types

  • Review

MeSH terms

  • Biomarkers, Tumor
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / metabolism
  • Breast Neoplasms* / pathology
  • Cyclin-Dependent Kinase 4* / antagonists & inhibitors
  • Cyclin-Dependent Kinase 6* / antagonists & inhibitors
  • Drug Resistance, Neoplasm
  • Female
  • Humans
  • Molecular Targeted Therapy
  • Neoplasm Metastasis
  • Protein Kinase Inhibitors* / pharmacology
  • Protein Kinase Inhibitors* / therapeutic use
  • Receptors, Estrogen* / metabolism
  • Receptors, Progesterone / metabolism

Substances

  • Cyclin-Dependent Kinase 4
  • Cyclin-Dependent Kinase 6
  • Protein Kinase Inhibitors
  • CDK6 protein, human
  • Receptors, Progesterone
  • CDK4 protein, human
  • Receptors, Estrogen
  • Biomarkers, Tumor