Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models.
Sheryl M GoughJohn J FlanaganJessica L F TehMonica AndreoliEmma RousseauMelissa PannoneMark BookbinderRyan WillardKim DavenportElizabeth BortolonGregory CadelinaDeborah GordonJennifer PizzanoJennifer MacalusoLeofal SotoJohn P CorradiKatherine M DigianantonioIeva DrulyteAlicia MorganConnor QuinnMiklós BékésCaterina FerraroXin ChenGan WangHanqing DongJing WangDavid R LangleyJohn HoustonRichard GedrichIan C TaylorPublished in: Clinical cancer research : an official journal of the American Association for Cancer Research (2024)
Vepdegestrant achieved greater ER degradation in vivo compared with fulvestrant, which correlated with improved TGI, suggesting vepdegestrant could be a more effective backbone ET for patients with ER+/HER2- breast cancer.