Clinical Trials

Numerous clinical trials spanning Phase 1 through Phase 3 evaluate the safety, pharmacokinetics, and therapeutic potential of vepdegestrant (ARV-471), with recruitment statuses ranging from active to completed. These studies primarily target locally advanced or metastatic ER+/HER2- breast cancer, while also investigating healthy participants, castration-resistant prostate cancer, and non-small cell lung cancer. Sponsored by organizations such as Pfizer, Arvinas, Carrick Therapeutics, and QuantumLeap Healthcare Collaborative, these umbrella and pharmacokinetic trials assess tolerability, antitumor activity, and drug-drug interactions.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01042379 RECRUITING
Breast Neoplasms; Breast Cancer; Breast Tumors; Angiosarcoma; TNBC - Triple-Negative Breast Cancer; HER2-positive Breast Cancer; HER2-negative Breast Cancer; Hormone Receptor Positive Tumor; Hormone Receptor Negative Tumor; Early-stage Breast Cancer; Locally Advanced Breast Cancer
QuantumLeap Healthcare Collaborative
 2010-03-01 PHASE2
NCT04606446 RECRUITING
Locally Advanced or Metastatic ER+ HER2- Breast Cancer; Locally Advanced or Metastatic Castration-resistant Prostate Cancer; Locally Advanced or Metastatic Non-small Cell Lung Cancer
Pfizer
 2020-11-16 PHASE2
NCT05548127 ACTIVE_NOT_RECRUITING
Breast Cancer
Pfizer
 2023-02-23 PHASE1; PHASE2
NCT06125522 ACTIVE_NOT_RECRUITING
Breast Cancer
Pfizer
 2024-01-10 PHASE1; PHASE2
NCT05909397 ACTIVE_NOT_RECRUITING
Breast Cancer
Pfizer
 2023-08-09 PHASE3
NCT05573555 ACTIVE_NOT_RECRUITING
Breast Cancer
Pfizer
 2023-03-01 PHASE1; PHASE2
NCT07231991 RECRUITING
Healthy Participants
Pfizer
 2025-11-18 PHASE1
NCT06206837 ACTIVE_NOT_RECRUITING
Breast Cancer
Pfizer
 2024-02-19 PHASE1; PHASE2
NCT06911788 COMPLETED
Healthy Participants
Pfizer
 2025-04-03 PHASE1
NCT06645938 COMPLETED
Healthy
Pfizer
 2024-10-16 PHASE1
NCT05654623 ACTIVE_NOT_RECRUITING
Advanced Breast Cancer
Pfizer
 2023-03-03 PHASE3
NCT04072952 COMPLETED
Breast Cancer
Arvinas Estrogen Receptor, Inc.
 2019-08-05 PHASE1; PHASE2
NCT06347861 COMPLETED
Healthy
Pfizer
 2024-04-02 PHASE1
NCT05549505 COMPLETED
Breast Cancer
Arvinas Inc.
 2023-02-15 PHASE2
NCT05501769 COMPLETED
Breast Cancer
Arvinas Estrogen Receptor, Inc.
 2022-09-08 PHASE1
NCT06275841 COMPLETED
Healthy
Pfizer
 2024-02-23 PHASE1
NCT06256510 COMPLETED
Healthy Participants
Pfizer
 2024-02-08 PHASE1
NCT05732428 COMPLETED
Breast Cancer
Pfizer
 2023-02-20 PHASE1
NCT06206837 Recruiting
Breast Cancer
Pfizer|Arvinas Estrogen Receptor Inc.
 2024-02-19 Phase 1|Phase 2
NCT06256510 Recruiting
Healthy Participants
Pfizer|Arvinas Estrogen Receptor Inc.
 2024-02-08 Phase 1
NCT06275841 Recruiting
Healthy
Pfizer|Arvinas Estrogen Receptor Inc.
 2024-02-23 Phase 1
NCT06125522 Recruiting
Breast Cancer
Pfizer|Arvinas Estrogen Receptor Inc.|Carrick Therapeutics Limited
 2024-01-10 Phase 1|Phase 2
NCT06005688 COMPLETED
Healthy Participants
Pfizer
 2023-08-18 PHASE1
NCT05930925 COMPLETED
Healthy
Pfizer
 2023-06-12 PHASE1
NCT05463952 ACTIVE_NOT_RECRUITING
Breast Neoplasms
Pfizer
 2022-08-16 PHASE1
NCT05538312 COMPLETED
Healthy
Pfizer
 2023-02-23 PHASE1
NCT05673889 COMPLETED
Healthy
Pfizer
 2023-01-27 PHASE1
NCT05652660 COMPLETED
Healthy
Pfizer
 2022-12-09 PHASE1

(data from https://clinicaltrials.gov, updated on 2026-05-06)

Check the Vepdegestrant (ARV-471) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Vepdegestrant (ARV-471) is an orally bioavailable proteolysis targeting chimera (PROTAC) that selectively binds the estrogen receptor and recruits an E3 ubiquitin ligase to induce proteasomal degradation of the target protein, thereby disrupting downstream estrogen-mediated transcriptional signaling. Consequently, this targeted receptor depletion suppresses estrogen-dependent cell proliferation, demonstrating direct therapeutic relevance for inhibiting tumor growth in patients with locally advanced or metastatic ER+/HER2- breast cancer.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.