A New Era in ER+ Breast Cancer: Best-in-Class Oral Selective Estrogen Receptor Degrader (SERD) Designed as an Endocrine Backbone Treatment
Pengcheng Shao
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.
Topics & Concepts
Estrogen receptorContext (archaeology)ChemistrySmall moleculeBreast cancerSelective estrogen receptor modulatorEndocrine systemEstrogenComputational biologyCancerCancer researchPharmacologyInternal medicineMedicineBiochemistryHormoneBiologyPaleontologyEstrogen and related hormone effectsFerrocene Chemistry and ApplicationsAdvanced Breast Cancer Therapies