Discovery and Chemical Development of Amcenestrant: An Oral Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer

This chapter describes the research program that led to the discovery of amcenestrant, an oral selective estrogen receptor degrader for the treatment of patients with estrogen receptor positive breast cancer. We discuss the medicinal chemistry strategy that led to the selection of this clinical candidate. Additionally, we describe the optimized synthetic route that provided the final process for multikilogram preparations.