A New Era in ER+ Breast Cancer: Best-in-Class Oral Selective Estrogen Receptor Degrader (SERD) Designed as an Endocrine Backbone Treatment.

ABSTRACT

There has been intense interest in developing orally bioavailable SERDs, energized by the recent discovery of treatment-resistant ESR1 mutations. Overcoming the two decades long challenge of combining all the desirable activities and properties into one molecule, GDC-9545 (giredestrant) was identified with an exceptional preclinical profile. This Viewpoint seeks to place this molecule in the historical context of previously reported oral SERDs and highlights the exciting clinical potential for a best-in-class oral SERD.