First FDA-approved PROTAC: Vepdegestrant moves targeted protein degradation into oncology practice
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REFERENCES
[1] Bekes M., Langley D.R., and Crews C.M. (2022). PROTAC targeted protein degraders: the past is prologue. Nat. Rev. Drug Discov. 21:181−200. DOI:10.1038/s41573-021-00371-6 [2] Campone M., De Laurentiis M., Jhaveri K., et al. (2025). Vepdegestrant, a PROTAC estrogen receptor degrader, in advanced breast cancer. N. Engl. J. Med. 393:556−568. DOI:10.1056/NEJMoa2505725 [3] Mullard A. (2026). First PROTAC gains FDA approval, bolstering targeted protein degradation and induced proximity ambitions. Nat. Rev. Drug Discov. 25:411. DOI:10.1038/d41573-026-00078-6 -
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Hu Z., Xu Z. and Peng X. (2026). First FDA-approved PROTAC: Vepdegestrant moves targeted protein degradation into oncology practice. The Innovation Drug Discovery 1:100020. https://doi.org/10.59717/j.xinn-drugdisc.2026.100020
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Hu Z., Xu Z. and Peng X. (2026). First FDA-approved PROTAC: Vepdegestrant moves targeted protein degradation into oncology practice. The Innovation Drug Discovery 1:100020. https://doi.org/10.59717/j.xinn-drugdisc.2026.100020
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Figure 1.
The approval of VEPPANU (vepdegestrant), an oral estrogen receptor degrader jointly developed by Arvinas and Pfizer, marks the first FDA-approved PROTAC therapy
