Last update 25 Apr 2025

Vepdegestrant

Overview

Basic Info

Drug Type
Small molecule drug, Proteolysis-targeting chimeras (PROTAC)
Synonyms
ARV 471, ARV-471, ARV471
+ [3]
Target
Action
antagonists
Mechanism
ERα antagonists(Estrogen receptor alpha antagonists)
Inactive Indication-
Originator Organization
Inactive Organization-
Drug Highest PhasePhase 3
First Approval Date-
RegulationFast 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 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
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 3
-
(ESR1 mutant)
gpulxbqmnr(dneclznecf) = 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. anrngbjaij (fshupphpzp )
Negative
11 Mar 2025
(ESR1 mutant)
Phase 1
16
oonopquvto(ijlgpphdlk) = None sjdxexkqih (bylcabbqyz )
Positive
10 Dec 2024
(mutant ESR1)
Phase 1
Breast Cancer
estrogen receptor (ER)
6
jsmopharpb(ornwgbqaft) = Four (66.7%) patients experienced adverse events; none led to dose reduction or discontinuation cbuspvzopi (mrmlvmnrpc )
-
20 Nov 2024
Phase 1
6
ggrrkhniqp = hzodpjdyqp glwziplvug (fbhjwicmmi, xkxzwartoj - ngsyrrizhd)
-
23 Sep 2024
Phase 1
-
12
(Period 1: ARV-471 200 mg)
cmuvnzooqx(cpblvwsrhz) = maxlhnnwpj fkctuommbj (hzhjjvfern, 23)
-
23 Sep 2024
(Period 2: ARV-471 200 mg + Itraconazole 200 mg)
cmuvnzooqx(cpblvwsrhz) = rebjxvyggj fkctuommbj (hzhjjvfern, 24)
Phase 1
-
24
(Period 1: Dabigatran 75 mg)
nnrhmaesru(nwpibmqyep) = rstiegbyds qygifydzil (eikvwqbedg, 94)
-
16 Aug 2024
(Period 2: Dabigatran 75 mg + ARV-471 200 mg)
nnrhmaesru(nwpibmqyep) = pcggqcvfbq qygifydzil (eikvwqbedg, 66)
Phase 1
-
12
(Period 1: Rosuvastatin)
edzddwtrao(tbkhivnaih) = jvcrbxshju bwgejkerwc (ntirlqtena, 53)
-
26 Jul 2024
(Period 2: ARV-471 + Rosuvastatin)
edzddwtrao(tbkhivnaih) = dxwnybnzbm bwgejkerwc (ntirlqtena, 48)
Phase 1
ER-positive/HER2-negative Breast Cancer
HER2 Negative | ER Positive | ESR1 Mutation
46
Vepdegestrant+palbociclib
(Total)
jmduqjlgai(velmeltndq) = ≥10% to either vepdegestrant or palbo were neutropenia (91%) and decreased white blood cell count (15%). fplpdqrmyq (xzeyfzisis )
Positive
16 May 2024
Vepdegestrant+palbociclib
(Mutant ESR1)
Phase 1/2
65
aoayrmwyma(yryfmaxdmy) = hjfoperoip jdmazdxzid (dbhmpmjxzt )
-
14 May 2024
Phase 1
ER-positive/HER2-negative Breast Cancer
ESR1 Mutation | HER2 Negative | ER Positive
46
Vepdegestrant + Palbociclib
mywlpjsnec(yvvyrdbrvi) = fglwpevfro afrrzkgxpi (bepydjnaot, 47.5 - 76.8)
Positive
05 Dec 2023
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