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Chemistry

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Also known as: Arv-471, Arv-471 (protac), Wc1u3r1ymi, 2229711-68-4, Arv471, (s)-3-(5-(4-((1-(4-(rel-(1r,2s)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
Molecular Formula
C45H49N5O4
Molecular Weight
723.9  g/mol
InChI Key
TZZDVPMABRWKIZ-XMOGEVODSA-N
FDA UNII
WC1U3R1YMI

Vepdegestrant
Vepdegestrant is an orally available hetero-bifunctional molecule and selective estrogen receptor (ER) alpha-targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Vepdegestrant is composed of an ER alpha ligand attached to an E3 ligase recognition moiety. Upon oral administration,vepdegestrant targets and binds to the ER ligand binding domain on ER alpha. E3 ligase is recruited to the ER by the E3 ligase recognition moiety and ER alpha is tagged by ubiquitin. This causes ubiquitination and degradation of ER alpha by the proteasome. This decreases ER alpha protein levels, decreases the expression of ER alpha-target genes and halts ER-mediated signaling. This results in an inhibition of proliferation in ER alpha-overexpressing tumor cells. In addition, the degradation of the ER alpha protein releases the ARV-471 and can bind to additional ER alpha target proteins. ER alpha is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation.
1 2D Structure

Vepdegestrant

2 Identification
2.1 Computed Descriptors
2.1.1 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
2.1.2 InChI
InChI=1S/C45H49N5O4/c51-37-12-15-39-33(27-37)8-13-38(31-4-2-1-3-5-31)43(39)32-6-9-35(10-7-32)48-20-18-30(19-21-48)28-47-22-24-49(25-23-47)36-11-14-40-34(26-36)29-50(45(40)54)41-16-17-42(52)46-44(41)53/h1-7,9-12,14-15,26-27,30,38,41,43,51H,8,13,16-25,28-29H2,(H,46,52,53)/t38-,41+,43+/m1/s1
2.1.3 InChI Key
TZZDVPMABRWKIZ-XMOGEVODSA-N
2.1.4 Canonical SMILES
C1CC2=C(C=CC(=C2)O)C(C1C3=CC=CC=C3)C4=CC=C(C=C4)N5CCC(CC5)CN6CCN(CC6)C7=CC8=C(C=C7)C(=O)N(C8)C9CCC(=O)NC9=O
2.1.5 Isomeric 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
2.2 Other Identifiers
2.2.1 UNII
WC1U3R1YMI
2.3 Synonyms
2.3.1 Depositor-Supplied Synonyms

1. Arv-471

2. Arv-471 (protac)

3. Wc1u3r1ymi

4. 2229711-68-4

5. Arv471

6. (s)-3-(5-(4-((1-(4-(rel-(1r,2s)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

7. 2614417-52-4

8. Vepdegestrant [inn]

9. Starbld0006985

10. Unii-wc1u3r1ymi

11. Arv 471

12. Arv 471 [who-dd]

13. Chembl5095210

14. Schembl20211870

15. Akos040757430

16. Ms-31245

17. Hy-138642

18. Cs-0159885

19. En300-37105519

20. (2(1)r,2(2)s,8(3)s)-2-hydroxy-2(1),2(2),2(3),2-tetrahydro-7(5,2)-isoindola-6(1,4)-piperazina-4(1,4),8(3)-dipiperidina-2(2,1)-naphthalena-1(1),3(1,4)-dibenzenaoctaphane-7(1),8(2),8(7(3)h)-trione

21. (3s)-3-(5-{4-[(1-{4-[(1r,2s)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl]phenyl}piperidin-4-yl)methyl]piperazin-1-yl}-1-oxo-2,3-dihydro-1h-isoindol-2-yl)piperidine-2,6-dione

22. (s)-3-(5-(4-((1-(4-((1r,2s)-6-hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione

23. 2,6-piperidinedione, 3-(1,3-dihydro-1-oxo-5-(4-((1-(4-((1r,2s)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl)phenyl)-4-piperidinyl)methyl)-1-piperazinyl)-2h-isoindol-2-yl)-, (3s)-

2.4 Create Date
2018-06-23
3 Chemical and Physical Properties
Molecular Weight 723.9 g/mol
Molecular Formula C45H49N5O4
XLogP36.4
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count7
Exact Mass g/mol
Monoisotopic Mass g/mol
Topological Polar Surface Area96.4
Heavy Atom Count54
Formal Charge0
Complexity1310
Isotope Atom Count0
Defined Atom Stereocenter Count3
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1

Drugs in Development

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Details:

ARV-471 (vepdegestrant) is an investigational PROTAC protein degrader designed to target and degrade the estrogen receptor. It is being evaluated for the treatment of ER+/HER2- breast cancer.


Lead Product(s): Vepdegestrant

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase IIIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable March 11, 2025

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01

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : ARV-471 (vepdegestrant) is an investigational PROTAC protein degrader designed to target and degrade the estrogen receptor. It is being evaluated for the treatment of ER+/HER2- breast cancer.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

March 11, 2025

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Details:

ARV-471 (vepdegestrant) is an investigational PROTAC protein degrader designed to target and degrade the estrogen receptor. It is being evaluated for the treatment of ER+/HER2- breast cancer.


Lead Product(s): Vepdegestrant,Abemaciclib

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase I/ Phase IIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable December 10, 2024

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02

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : ARV-471 (vepdegestrant) is an investigational PROTAC protein degrader designed to target and degrade the estrogen receptor. It is being evaluated for the treatment of ER+/HER2- breast cancer.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

December 10, 2024

blank

Details:

ARV-471 (vepdegestrant) is an oral bioavailable PROTAC protein degrader designed to target & degrade the estrogen receptor, currently in phase 3 trials for ER+/HER2- breast cancer treatment.


Lead Product(s): Vepdegestrant

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase IIIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable June 02, 2024

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03

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : ARV-471 (vepdegestrant) is an oral bioavailable PROTAC protein degrader designed to target & degrade the estrogen receptor, currently in phase 3 trials for ER+/HER2- breast cancer treatment.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

June 02, 2024

blank

Details:

ARV-471 (vepdegestrant) is an investigational PROTAC protein degrader designed to target and degrade the estrogen receptor. It is being evaluated for the treatment of ER+/HER2- breast cancer.


Lead Product(s): Vepdegestrant,Palbociclib

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase I/ Phase IIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable May 16, 2024

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04

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : ARV-471 (vepdegestrant) is an investigational PROTAC protein degrader designed to target and degrade the estrogen receptor. It is being evaluated for the treatment of ER+/HER2- breast cancer.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

May 16, 2024

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Details:

CT7001 (samuraciclib) is a first-in-class oral CDK7 inhibitor evaluated with ARV-471 (vepdegestrant) for ER+, HER2- metastatic breast cancer treatment.


Lead Product(s): Samuraciclib,Vepdegestrant

Therapeutic Area: Oncology Brand Name: CT7001

Study Phase: Phase I/ Phase IIProduct Type: Other Small Molecule

Sponsor: Inapplicable

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable February 14, 2024

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05

IOPC
Not Confirmed
IOPC
Not Confirmed

Details : CT7001 (samuraciclib) is a first-in-class oral CDK7 inhibitor evaluated with ARV-471 (vepdegestrant) for ER+, HER2- metastatic breast cancer treatment.

Product Name : CT7001

Product Type : Other Small Molecule

Upfront Cash : Inapplicable

February 14, 2024

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Details:

Arvinas expects to use net proceeds to advance its clinical development programs and preclinical pipeline, including ARV-471 (vepdegestrant), an investigational orally bioavailable PROTAC® protein degrader.


Lead Product(s): Vepdegestrant

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase IIIProduct Type: PROTACs

Sponsor: BofA Securities

Deal Size: $350.0 million Upfront Cash: Undisclosed

Deal Type: Private Placement November 27, 2023

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06

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : Arvinas expects to use net proceeds to advance its clinical development programs and preclinical pipeline, including ARV-471 (vepdegestrant), an investigational orally bioavailable PROTAC® protein degrader.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Undisclosed

November 27, 2023

blank

Details:

ARV-471 (vepdegestrant) is an investigational, orally bioavailable PROTAC® protein degrader designed to specifically target and degrade the estrogen receptor for the treatment of patients with early and locally advanced breast cancer.


Lead Product(s): Vepdegestrant

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase IIIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable July 31, 2023

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07

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : ARV-471 (vepdegestrant) is an investigational, orally bioavailable PROTAC® protein degrader designed to specifically target and degrade the estrogen receptor for the treatment of patients with early and locally advanced breast cancer.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

July 31, 2023

blank

Details:

ARV-471 is an investigational, orally-bioavailable PROTAC® protein degrader designed to specifically target and degrade the estrogen receptor (ER) for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.


Lead Product(s): Vepdegestrant,Palbociclib

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase I/ Phase IIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable November 22, 2022

blank

08

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : ARV-471 is an investigational, orally-bioavailable PROTAC® protein degrader designed to specifically target and degrade the estrogen receptor (ER) for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

November 22, 2022

blank

Details:

The results showed ARV-471 has the potential to become a first-in-category treatment, and a new standard of care, for ER+/HER2- breast cancer patients and showed clinical benefits including tumor shrinkage and good tolerability.


Lead Product(s): Vepdegestrant,Palbociclib

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase I/ Phase IIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: Inapplicable Upfront Cash: Inapplicable

Deal Type: Inapplicable October 10, 2021

blank

09

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : The results showed ARV-471 has the potential to become a first-in-category treatment, and a new standard of care, for ER+/HER2- breast cancer patients and showed clinical benefits including tumor shrinkage and good tolerability.

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : Inapplicable

October 10, 2021

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Details:

Collaboration combines Arvinas’ investigational estrogen receptor-targeting breast cancer therapy with Pfizer’s deep experience in breast oncology therapeutics. ARV-471 is currently in Phase 2 trial for patients with locally advanced/metastatic ER+/HER2- breast cancer.


Lead Product(s): Vepdegestrant,Palbociclib

Therapeutic Area: Oncology Brand Name: ARV-471

Study Phase: Phase I/ Phase IIProduct Type: PROTACs

Sponsor: Pfizer Inc

Deal Size: $2,050.0 million Upfront Cash: $650.0 million

Deal Type: Collaboration July 22, 2021

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10

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Arvinas

U.S.A
arrow
IOPC
Not Confirmed

Details : Collaboration combines Arvinas’ investigational estrogen receptor-targeting breast cancer therapy with Pfizer’s deep experience in breast oncology therapeutics. ARV-471 is currently in Phase 2 trial for patients with locally advanced/metastatic ER+/H...

Product Name : ARV-471

Product Type : PROTACs

Upfront Cash : $650.0 million

July 22, 2021

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