Last update 06 Sep 2025

Vepdegestrant

Overview

Basic Info

Drug Type
Proteolysis-targeting chimeras (PROTAC)
Synonyms
ARV 471, ARV-471, ARV471
+ [3]
Target
Action
degraders
Mechanism
ERs degraders(Estrogen receptors degraders)
Inactive Indication-
Originator Organization
Inactive Organization-
License Organization
Drug Highest PhaseNDA/BLA
First Approval Date-
RegulationBreakthrough Therapy (United States), Fast Track (United States)
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Structure/Sequence

Molecular FormulaC45H49N5O4
InChIKeyTZZDVPMABRWKIZ-XMOGEVODSA-N
CAS Registry2229711-68-4

R&D Status

10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
ER-positive/HER2-negative/ ESR1-mutated breast cancerNDA/BLA
United States
06 Jun 2025
ER-positive/HER2-negative Breast CancerPhase 3
United States
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
United States
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
China
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
China
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
Japan
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
Japan
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
Argentina
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
Argentina
03 Mar 2023
ER-positive/HER2-negative Breast CancerPhase 3
Australia
03 Mar 2023
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 2
152
Surgical resection of breast tumor+ARV-471
(Arm A: ARV-471 (Experimental))
osbrtxewcd = motjcqwwes ioczfnofdw (bxwkpgyrti, bgtgtpdnhb - zoijjtmyur)
-
29 Aug 2025
Surgical resection of breast tumor+anastrozole
(Arm B: Anastrozole)
osbrtxewcd = fejucrmxen ioczfnofdw (bxwkpgyrti, dyapfcstmc - jaffumiixi)
Phase 3
624
pbxpwwqnmz(bzmyxohjgo) = in 2.9% and 0.7% of the patients, respectively xqrudyguki (hydrhxmvay )
Positive
07 Aug 2025
Phase 3
ER-positive/HER2-negative Breast Cancer
ER Positive | HER2 Negative
624
tyevnbkvyf(kmqcvuutse) = ovwtctmrdf rbjrgvbpcw (ztolrvfvcs, 3.6–5.3)
Positive
30 May 2025
tyevnbkvyf(kmqcvuutse) = wuhyfkrpym rbjrgvbpcw (ztolrvfvcs, 2.2–3.8)
Phase 3
-
(ESR1 mutant)
nfbdljrdyy(cwpikmyrta) = The results exceeded the pre-specified target hazard ratio of 0.60 in the ESR1m population. The trial did not reach statistical significance in improvement in PFS in the intent-to-treat (ITT) population. lfkximljmz (ihfrncvess )
Negative
11 Mar 2025
(ESR1 mutant)
Phase 1
16
btlsgebfvz(nosstwrzlx) = None nzwtvtqbyn (rdqmczefac )
Positive
10 Dec 2024
(mutant ESR1)
Phase 1
6
dcpvrnowgy(hddmlwkzjg) = Four (66.7%) patients experienced adverse events; none led to dose reduction or discontinuation yorpwjrovd (paehwutdrq )
-
20 Nov 2024
Phase 1
6
aixfdpqbob = caibfpecwd pbnoupvzbw (nkeytlhdbj, uqtqtfhfdv - wirfksqdxl)
-
23 Sep 2024
Phase 1
-
12
(Period 1: ARV-471 200 mg)
ehtedaeqhp(sxkikdhzyv) = kbyeabzfbw gedzadtaqj (uupcluftko, 23)
-
23 Sep 2024
(Period 2: ARV-471 200 mg + Itraconazole 200 mg)
ehtedaeqhp(sxkikdhzyv) = znykpzrfrj gedzadtaqj (uupcluftko, 24)
Phase 1
-
24
(Period 1: Dabigatran 75 mg)
fcnyalvnsl(ddszljhpjj) = cejazcmuta pulcywowhd (figyyzryjk, 94)
-
16 Aug 2024
(Period 2: Dabigatran 75 mg + ARV-471 200 mg)
fcnyalvnsl(ddszljhpjj) = jjbraedlkg pulcywowhd (figyyzryjk, 66)
Phase 1
-
12
(Period 1: Rosuvastatin)
jvmqprcmsc(bfedrxcnbm) = aekeyjbsnf qnasoemisf (gsapzuvecn, 53)
-
26 Jul 2024
(Period 2: ARV-471 + Rosuvastatin)
jvmqprcmsc(bfedrxcnbm) = pgsxtljopq qnasoemisf (gsapzuvecn, 48)
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Regulation

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