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Updated: Mar 6, 2026
Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
Published on: March 17, 2016
Androgen Receptor Function and Androgen Receptor-Targeted Therapies in Breast Cancer: A Review
Miho Kono1,2, Takeo Fujii1,2, Bora Lim1,2
1Section of Translational Breast Cancer Research, Department of Breast Medical Oncology, The University of Texas MD Anderson Cancer Center, Houston.
Importance:
The androgen receptor (AR) pathway is emerging as a potential therapeutic target in breast cancer. To date, AR-targeted drugs have been approved only for treatment of prostate cancer; however, AR-targeted treatment for breast cancer is an area of active investigation. Through review of preclinical studies, retrospective clinical studies, and clinical trials, we examined the biology of AR and AR-related pathways, the potential for AR-targeted therapies in breast cancer, and potential biomarkers for AR-targeted treatments.
Observations:
The rate of AR positivity in breast cancer is about 60% to 80%. Biologically, the AR pathway has cross-talk with several other key signaling pathways, including the PI3K/Akt/mTOR and MAPK pathways, and with other receptors, including estrogen receptor and human epidermal growth factor receptor-2. The value of AR positivity as a prognostic marker has not yet been defined. Androgen receptor-targeted therapies, including AR agonists, AR antagonists, and PI3K inhibitors, have shown promising results in clinical trials in patients with breast cancer, and combinations of AR-targeted therapies with other agents have been investigated for overcoming resistance to AR-targeted therapies. Biomarkers to stratify patients according to the likelihood of response to AR-targeted drugs are yet to be established. Potential biomarkers of response to AR inhibitors include AR phosphorylation and AR gene expression.
Conclusions And Relevance:
Androgen receptor-targeted treatments for breast cancer are in development and have shown promising preliminary results. In-depth understanding of AR and AR-related signaling pathways would improve the treatment strategies for AR-positive breast cancer. Further preclinical and clinical studies of AR-targeted drugs alone and in combination with other drugs are justified and warranted to clarify the biology of AR and inform the development of AR-targeted therapies to improve survival outcome in patients with breast cancer.
Insights
Androgen receptor (AR) targeted therapies show promise for breast cancer treatment. Further research is needed to understand AR pathways and develop effective biomarkers for AR-positive breast cancer.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The androgen receptor (AR) pathway is a significant area of research for breast cancer therapy.
- AR-targeted drugs are currently approved for prostate cancer, with active investigation for breast cancer applications.
- Understanding AR biology and its related pathways is crucial for developing novel breast cancer treatments.
Purpose of the Study:
- To review the biology of the AR pathway in breast cancer.
- To examine the potential of AR-targeted therapies for breast cancer treatment.
- To identify potential biomarkers for predicting response to AR-targeted therapies.
Main Methods:
- Review of preclinical studies, retrospective clinical studies, and clinical trials.
- Analysis of AR pathway signaling and its cross-talk with other key pathways (PI3K/Akt/mTOR, MAPK) and receptors (ER, HER2).
- Evaluation of AR-targeted therapies, including agonists, antagonists, and PI3K inhibitors, and combination strategies.
Main Results:
- AR positivity is observed in 60% to 80% of breast cancers.
- AR-targeted therapies have demonstrated promising preliminary results in clinical trials.
- Combinations of AR-targeted therapies are being investigated to overcome resistance.
- Potential biomarkers for AR inhibitor response include AR phosphorylation and gene expression.
Conclusions:
- AR-targeted treatments for breast cancer are under development with encouraging early outcomes.
- A deeper understanding of AR signaling pathways is essential for optimizing treatment strategies in AR-positive breast cancer.
- Further preclinical and clinical studies are warranted to advance AR-targeted therapies and improve patient survival.
