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Francisco J. Esteva: Can PROTACs Beat ESR1 Mutations in Breast Cancer?
Jun 10, 2025, 19:16

Francisco J. Esteva: Can PROTACs Beat ESR1 Mutations in Breast Cancer?

Francisco J. Esteva, Chief of the Division of Hematology and Medical Oncology at Lenox Hill Hospital and a Professor of Medicine at the Zucker School of Medicine, shared a post on LinkedIn:

“Can PROTACs Beat ESR1 Mutations in Breast Cancer?

PROTACs (proteolysis-targeting chimeras) are designed to degrade the estrogen receptor itself. The VERITAC-2 trial showed promising results for ARV471 (vepdegestrant) in patients who previously progressed on endocrine therapy and have ESR1 mutations.

If approved by the FDA, this could mark a major shift in how we treat endocrine-resistant disease—offering patients a targeted, oral alternative that removes the receptor entirely rather than blocking it.

To learn more see video.”

Title: Vepdegestrant, a PROTAC Estrogen Receptor Degrader, in Advanced Breast Cancer

Authors: Mario Campone, Michelino De Laurentiis, Komal Jhaveri, Xichun Hu, Sylvain Ladoire, Anne Patsouris, Claudio Zamagni, Jiuwei Cui, Marina Cazzaniga, Timucin Cil, Katarzyna J. Jerzak, Christian Fuentes, Tetsuhiro Yoshinami, Alvaro Rodriguez-Lescure, Ahmet Sezer, Andrea Fontana, Valentina Guarneri, Andrea Molckovsky, Marie-Ange Mouret-Reynier, Umut Demirci, Yongqiang Zhang, Olga Valota, Dongrui R Lu, Marcella Martignoni, Janaki Parameswaran, Xin Zhi, Erika P. Hamilton

Read the Full Article.

Francisco J. Esteva

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