Targeting the Androgen Receptor in Breast Cancer

The selective AR modulator enobosarm showed activity in a small study of patients with ER-positive/AR-positive metastatic breast cancer.

Recent studies have shown that the androgen receptor (AR) is a tumor suppressor and AR agonists can lead to AR activation and antitumor activity in estrogen receptor (ER)–positive breast cancer (Nat Med 2021; 27:310). Selective AR modulators (SARMs) selectively bind to the AR without causing the virilizing effects associated with androgen therapy and AR antagonists. Enobosarm is an oral SARM that has demonstrated in vivo antitumor activity in ER-positive and ER-resistant disease.

In a multinational, randomized, open-label, phase 2 trial, researchers assessed the effects of enobosarm at two dose levels (9 mg or 18 mg daily) in 136 postmenopausal patients with ER-positive/AR-positive metastatic breast cancer. The median age was 60.5 years and …

Reviewing Author

William J. Gradishar, MD

Disclosures

Consultant/Advisory BoardLilly; AstraZeneca; Gilead

Grant/Research SupportBreast Cancer Research Foundation

Editorial BoardsClinical Breast Cancer; Oncology; Annals of Surgery; Breast Cancer Research and Treatment

Leadership Positions in Professional SocietiesNational Comprehensive Cancer Network (Chair, Breast Cancer Panel); American Board of Internal Medicine (Medical Oncology Board)