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The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer.

Drug discovery today - 1 Sept 2026

Lin Xin, Xiang Hua, Luo Guoshun

Abstract excerpt

The 2026 FDA approval of vepdegestrant (ARV-471), an oral proteolysis-targeting chimera (PROTAC) that targets the estrogen receptor α (ERα), represents a historic milestone for targeted protein degradation. Unlike selective estrogen receptor degraders that operate via occupancy-driven destabilization, vepdegestrant catalytically recruits the CRBN E3 ligase to ERα, inducing its ubiquitination and proteasomal...

Read the complete abstract on PubMed

Topics

Humans
Estrogen Receptor alpha
Proteolysis Targeting Chimera
Breast Neoplasms
Female
Mutation
Drug Approval

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

United States

Animals

Source

Identifiers

PMID: 42603649
DOI: 10.1016/j.drudis.2026.104772

Genes

ESR1
CRBN

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 25 Oct 2026.

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The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer.PMID 42603649Read ↗

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Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer CellsSemantic proximity Read ↗

Two-Stage Strategy for Development of Proteolysis Targeting Chimeras and its Application for Estrogen Receptor DegradersSemantic proximity Read ↗

Targeting Unique Ligand Binding Domain Structural Features Downregulates DKK1 in Y537S ESR1 Mutant Breast Cancer CellsSemantic proximity Read ↗

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Mdm2 targeting via PROteolysis TArgeting Chimeras (PROTAC) is efficient in p53 wildtype, p53-mutated, and abemaciclib-resistant estrogen receptor-positive cell lines and superior to mdm2 inhibition.Semantic proximity Read ↗

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