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 to fulvestrant, which correlated with improved tumor growth inhibition, suggesting vepdegestrant could be a more effective backbone ET for patients with ER+/HER2- breast cancer.