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Leveraging Antiprogestins in the Treatment of Metastatic Breast Cancer. Endocrinology 2021 Aug 01;162(8)



Pubmed ID




Scopus ID

2-s2.0-85111784651 (requires institutional sign-in at Scopus site)   4 Citations


Although incurable, the prognosis for patients with metastatic breast cancer (MBC) has considerably improved with the approvals of multiple targeted and cytotoxic therapies. For hormone receptor-positive (HR+), ie, estrogen receptor and progesterone receptor positive (ER+/PgR+) and human epidermal growth factor receptor-2 negative (ie, ERBB2 gene nonamplified or HER2-) MBC, current approved treatment options include palliative endocrine therapy (ET), cyclin-dependent kinase (CDK 4/6) inhibitors, mTOR inhibitors, and PI3 kinase inhibitors. Most treatments target ER+ disease regardless of PgR status. Although the presence of PgR is crucial for ER+ cell proliferation in both normal and malignant mammary tissue, currently, there are no approved treatments that specifically target PgR. Recent literature has demonstrated the potential of antiprogestins in the treatment of MBC both in preclinical and clinical studies. Antiprogestins, including selective PgR modulators (SPRMs) that act as PgR antagonists, are a promising class of therapeutics for overcoming endocrine resistance in patients who develop activating estrogen receptor 1 (ESR1) and phosphatidylinositol 3-kinase (PI3K) gene mutations after prior endocrine therapy. Herein, we summarize the role of PgR and antiprogestins in the treatment of MBC. Other aspects on the use of functional imaging, clinical trials incorporating novel antiprogestins, and potential treatment combinations to overcome endocrine resistance will be briefly discussed.

Author List

Kamaraju S, Fowler AM, Weil E, Wisinski KB, Truong TH, Lehr M, Chaudhary LN, Cheng YC, Chitambar CR, Rui H, Yee D, Lange C


Lubna N. Chaudhary MD Associate Professor in the Medicine department at Medical College of Wisconsin
Sailaja Kamaraju MD Associate Professor in the Medicine department at Medical College of Wisconsin

MESH terms used to index this publication - Major topics in bold

Antineoplastic Agents
Breast Neoplasms
Clinical Trials as Topic
Receptors, Progesterone