Vepdegestrant

Summary

Vepdegestrant (CHEMBL5095210) is a phase-3 clinical-stage small molecule; indicated across 4 conditions including breast neoplasm and neoplasm.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Small molecule
• Indications: 4 conditions
• Clinical trials: 20
• Chemistry: 723.9 Da · C45H49N5O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5095210
Name	Vepdegestrant
Type	Small molecule
Max phase	3
FDA approved	no
PubChem CID	134562533
Molecular formula	C45H49N5O4
Molecular weight	723.9
InChIKey	TZZDVPMABRWKIZ-XMOGEVODSA-N

SMILES: C1CC2=C(C=CC(=C2)O)[C@H]([C@H]1C3=CC=CC=C3)C4=CC=C(C=C4)N5CCC(CC5)CN6CCN(CC6)C7=CC8=C(C=C7)C(=O)N(C8)[C@H]9CCC(=O)NC9=O

IUPAC name: (3S)-3-[6-[4-[[1-[4-[(1R,2S)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl]phenyl]piperidin-4-yl]methyl]piperazin-1-yl]-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione

Also known as: Arv 471, ARV-471, ARV-471 (PROTAC), ARV471, PF-07850327, Vepdegestrant, VEPDEGESTRANT, Vepdegrestrant

Patent coverage: 163 distinct patent families (336 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 264 (79%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Estrogen receptor, Protein cereblon/Estrogen receptor.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ESR1	9	EC50	1	nM	CHEMBL_ACT_25568144
ESR1	8.74	Ki	1.8	nM	CHEMBL_ACT_29105256
ESR1	8.7	EC50	2	nM	CHEMBL_ACT_24775636
ESR1	8.31	IC50	4.9	nM	CHEMBL_ACT_29106420

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

4 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
breast neoplasm	3	MONDO:0021100	EFO:0003869
neoplasm	2	MONDO:0005070	EFO:0000616
angiosarcoma	2	MONDO:0016982	EFO:0003968

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 20.

Phase distribution

Phase	Trials
PHASE1	10
PHASE1/PHASE2	5
PHASE2	3
PHASE3	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05654623	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Learn About a New Medicine Called Vepdegestrant (ARV-471, PF-07850327) in People Who Have Advanced Metastatic Breast Cancer
NCT05909397	PHASE3	ACTIVE_NOT_RECRUITING	Vepdegestrant (ARV-471/PF-07850327) + Palbociclib vs Letrozole + Palbociclib in ER(+)/HER2(-) Advanced Breast Cancer
NCT01042379	PHASE2	RECRUITING	I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
NCT04606446	PHASE2	RECRUITING	Study of PF-07248144 in Advanced or Metastatic Solid Tumors
NCT05548127	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer (Sub-Study A)
NCT05573555	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer (Sub-Study B)
NCT06125522	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer. (Sub-Study C)
NCT06206837	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Study to Learn About Vepdegestrant When Given With PF-07220060 to People With Advanced or Metastatic Breast Cancer.
NCT04072952	PHASE1/PHASE2	COMPLETED	A Phase 1/2 Trial of ARV-471 Alone and in Combination With Palbociclib (IBRANCE®) in Patients With ER+/HER2- Locally Advanced or Metastatic Breast Cancer
NCT05549505	PHASE2	COMPLETED	A Trial Using ARV-471 or Anastrozole in Post-Menopausal Women With Breast Cancer Prior to Surgery
NCT05463952	PHASE1	ACTIVE_NOT_RECRUITING	A Study to Learn About the Vepdegestrant (ARV-471, PF-07850327) in People With ER+/HER2- Locally Advanced or Metastatic Breast Cancer (BC)
NCT07231991	PHASE1	RECRUITING	A Study to Learn How the Body Processes the Study Medicine Called Vepdegestrant in People With Loss of Liver Function
NCT05538312	PHASE1	COMPLETED	A Study to Understand the Effect of Itraconazole on the Levels of a Study Medicine Called ARV-471 in Healthy Adults
NCT05652660	PHASE1	COMPLETED	A Study to Understand the Effect of a Study Medicine Called ARV-471 on Rosuvastatin in Healthy Adults
NCT05673889	PHASE1	COMPLETED	A Study to Understand the Effect of a Study Medicine Called ARV-471 on Dabigatran Etexilate in Healthy Adults
NCT05732428	PHASE1	COMPLETED	A Study to Learn About the Study Medicine Called Vepdegestrant (ARV-471, PF-07850327) in People With ER+/HER2- Advanced Breast Cancer in China
NCT06005688	PHASE1	COMPLETED	A Study to Understand the Effects of Carbamazepine on How Vepdegestrant is Processed in Healthy Participants
NCT06256510	PHASE1	COMPLETED	A Study to Learn If the Study Medicine Called Vepdegestrant Changes How the Body Processes the Other Study Medicine Called Midazolam
NCT06275841	PHASE1	COMPLETED	A Study to Learn If the Study Medicine Esomeprazole Changes How the Body Processes the Other Study Medicine Vepdegestrant
NCT06911788	PHASE1	COMPLETED	A Study to Learn How a Tablet Compared With an IV Infusion of the Study Medicine Called Vepdegestrant is Taken up Into the Blood in Healthy Adults

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).