Development of a Commercial Manufacturing Process for Vepdegestrant, an Orally Bioavailable PROTAC Estrogen Receptor Degrader for the Treatment of Breast Cancer
Steve Avery(Pfizer (United States)), Jamie M. Buske(Pfizer (United States)), Doris Chen(Arvinas (United States)), Herman Chen(Arvinas (United States)), Xin Chen(Arvinas (United States)), Andrew R. Davidson(Pfizer (United States)), Jean‐Nicolas Desrosiers(Pfizer (United States)), Hanqing Dong(Arvinas (United States)), Noalle Fellah(Pfizer (United States)), David F. Fernández(Pfizer (United States)), John A. Grosso(Arvinas (United States)), Lu Han(Pfizer (United States)), Teri Shanklin Hochdorfer(Pfizer (United States)), Amber M. Johnson(Pfizer (United States)), Brian P. Jones(Pfizer (United States)), Maciej Kalinowski(Pfizer (United States)), Katherine D. Launer-Felty(Pfizer (United States)), Jorge López(Pfizer (United States)), Teresa W. Makowski(Pfizer (United States)), Carolyn Mastriano(Pfizer (United States)), Truong N. Nguyen(Pfizer (United States)), Nitinchandra D. Patel(Arvinas (United States)), Zhihui Peng(Pfizer (United States)), Tyler J. Potter(Pfizer (United States)), Robert P. Pritchard(Pfizer (United States)), Anil M. Rane(Pfizer (United States)), Max Reeve(Arvinas (United States)), Margaret C. Richins(Pfizer (United States)), Chase A. Salazar(Pfizer (United States)), John J. Salisbury(Pfizer (United States)), Robert S. Simpson(Arvinas (United States)), Liza Tabshey(Pfizer (United States)), Erin J. Tweed(Pfizer (United States)), Paul G. Wahome(Pfizer (United States)), Nancy Walsh-Sayles(Pfizer (United States)), Jordan A. Willie(Pfizer (United States)), Ethan Wood(Pfizer (United States))
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Abstract
A commercial process for vepdegestrant (1), the most advanced PROTAC protein degrader in human clinical trials, has been developed to support clinical and commercial needs. The process features an efficient convergent synthetic strategy through the final reductive amination of two advanced chiral intermediates, as well as several highly efficient telescoped processes and robust crystallization for purity control. The final commercial process of vepdegestrant (1) consists of seven proposed regulatory GMP steps with five isolations in an overall yield of 29%.
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