Product Description
An orally available selective androgen receptor (AR)-targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. Bavdegalutamide is composed of an AR ligand attached to an E3 ligase recognition moiety. Upon oral administration, bavdegalutamide targets and binds to the AR ligand binding domain. E3 ligase is recruited to the AR by the E3 ligase recognition moiety and the AR target protein is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome. This prevents the expression of AR target genes and halts AR-mediated signaling. This results in an inhibition of proliferation in AR-overexpressing tumor cells. In addition, the degradation of the AR protein releases the ARV-110 is released and can bind to additional AR target proteins. AR plays a key role in the proliferation of castration-resistant prostate cancer cells (CRPC). (Sourced from: https://www.cancer.gov/publications/dictionaries/cancer-drug/def/bavdegalutamide?redirect=true)
Mechanisms of Action: AR Degrader
Novel Mechanism: Yes
Modality: Small Molecule
Route of Administration: Oral
FDA Designation: *
Approval Status: Not Approved
Approved Countries: None
Approved Indications: None
Known Adverse Events: None
Company: Arvinas
Company Location: Eastern America
Company CEO: John Houston
Additional Commercial Interests: None
Clinical Description
Countries in Clinic: Canada, France, United Kingdom, United States
Active Clinical Trial Count: 2
Recent & Upcoming Milestones
Highest Development Phases
Phase 2: Prostate Cancer
Trial ID |
Trial |
Phase |
Trial Status |
Disease |
Primary Completion Date |
Probability of Success |
Latest Trial Update Date |
Data Updated |
|---|---|---|---|---|---|---|---|---|
NCT05177042 |
ARV-110-mCRPC-103 | P1 |
Completed |
Prostate Cancer |
2024-07-02 |
12% |
2025-07-26 |
Primary Endpoints|Study Completion Date|Treatments|Trial Status |
NCT03888612 |
mCRPC | P2 |
Completed |
Prostate Cancer |
2024-04-29 |
12% |
2025-03-18 |
Patient Enrollment|Primary Completion Date|Primary Endpoints|Treatments|Trial Status |
Recent News Events
Date |
Type |
Title |
|---|---|---|
|
04/29/2024 |
PubMed |
Protein degraders - from thalidomide to new PROTACs. |
|
05/23/2024 |
News Article |
Arvinas Announces Upcoming Presentations at the 2024 American Society of Clinical Oncology Annual Congress |
|
05/16/2024 |
News Article |
Arvinas and Pfizer Announce Updated Clinical Data from Phase 1b Trial of Vepdegestrant in Combination with Palbociclib (IBRANCEĀ®) |
|
05/09/2024 |
News Article |
Arvinas Announces Upcoming Vepdegestrant Poster Presentations at the 2024 European Society for Medical Oncology (ESMO) Breast Cancer Annual Congress |
|
05/02/2024 |
News Article |
Arvinas to Present at Upcoming Investor Conferences |
|
04/01/2024 |
PubMed |
Developing a Novel Enzalutamide-Resistant Prostate Cancer Model via AR F877L Mutation in LNCaP Cells. |
|
08/01/2023 |
PubMed |
Industry perspective on the nonclinical safety assessment of heterobifunctional degraders. |
