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Vepdegestrant · Veppanu, ARV-471

Small molecule (PROTAC degrader) · Degrader of estrogen receptor alpha (ESR1) · developed by Rigel Pharms

Approved FDA, May 2026

7 Registered trials

What is Vepdegestrant?

Vepdegestrant is an orally available PROTAC protein degrader that targets estrogen receptor alpha (ESR1). It binds the ER ligand binding domain and recruits E3 ligase to ubiquitinate and degrade ER alpha, decreasing ER-mediated signaling and halting proliferation in ER-overexpressing tumor cells.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as: Veppanu, ARV-471, PF-07850327, [oxoisoindolin-14C]ARV-471, [phenyl-14C]ARV-471
Drug type: Small molecule (PROTAC degrader)
Targets: estrogen receptor alpha (ESR1)
Mechanism: Degrader of estrogen receptor alpha (ESR1)
Pathways: ER-mediated signaling, proteasomal degradation
Therapy area: Oncology
Developer: Rigel Pharms
In trials of: ARVN
FDA status: Approved as Veppanu (May 1, 2026), NDA219835 · FDA label
UNII: WC1U3R1YMI

✅ FDA-approved uses

ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer

From the indications section of the FDA label (version of Jun 12, 2026). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trial	Phase	Condition	Status	Sponsor
NCT05909397	Phase 3	Breast Cancer	Active not recruiting	ARVN
NCT05654623	Phase 3	Advanced Breast Cancer	Active not recruiting	ARVN
NCT06206837	Phase 1/2	Breast Cancer	Active not recruiting	ARVN
NCT06911788	Phase 1	Healthy Participants	Completed	ARVN
NCT06645938	Phase 1	Healthy	Completed	ARVN
NCT06347861	Phase 1	Healthy	Completed	ARVN
NCT05930925	Phase 1	Healthy	Completed	ARVN

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Advanced Breast CancerHealthy

Other drugs acting on ESR1

Camizestrant FDA approved Ethinyl Estradiol/Levonorgestrel FDA approved Imlunestrant FDA approved Segesterone Acetate and Ethinyl Estradiol FDA approved Tamoxifen FDA approved Giredestrant Phase 1/2 Zuclomiphene Phase 2

Sources

Updated Oct 3, 2026.

Data: FDA (Drugs@FDA, Purple Book, DailyMed), NIH (NCI Thesaurus, GSRS, RxNorm), ClinicalTrials.gov • Informational purposes only, not medical or investment advice. • All drugs A–Z