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The safety and efficacy of this agent(s), or use in this setting, has not been established or is subject to confirmation. For an agent(s) whose safety and efficacy has not been established or confirmed, future regulatory approval or commercial availability is not guaranteed.

Vepdegestrant (ARV-471)*

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Vepdegestrant (ARV-471)*

Vepdegestrant is an investigational compound. Its safety and efficacy have not been established. * Vepdegestrant is being co-developed with Arvinas.

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Overview + Rationale

RATIONALE FOR CANCER TARGET

Worldwide, female breast cancer has now surpassed lung cancer as the most commonly diagnosed cancer

  • ~310,720 women are expected to be diagnosed with invasive breast cancer in the US in 20241
  • Metastatic breast cancer accounts for ~6% of newly diagnosed cases

Estrogen receptor (ER)-positive breast cancers make up ~80% of all breast cancers2

There is an unmet need for patients with ER-positive breast cancers who progress on endocrine therapy and CDK 4/6 inhibitors3

 

Mechanism of Action

  • PROteolysis TArgeting Chimera (PROTAC) protein degraders are heterobifunctional molecules that consist of a ligand for a target protein (the ER for vepdegestrant) and another ligand, which serves as a substrate for an E3 ubiquitin ligase complex
  • Upon binding to ER, the PROTAC vepdegestrant has shown to recruit an E3 ubiquitin ligase complex, which marks ER with ubiquitin tags for proteasomal degradation

Stage of Development

small icon representing breast cancer

ER+/HER2- Metastatic Breast Cancer

Phase 1 Monotherapy§

Phase 1 Combination

Phase 1B/2 Combination§

Phase 3 Monotherapy§
This information is current as of November 10th 2025.

* Vepdegestrant is being co-developed with Arvinas, § Closed to Enrollment

REFERENCES:  1.American Cancer Society, Inc. https://www.cancer.org/cancer/types/breast-cancer/about/how-common-is-breast-cancer.html. Accessed August 27, 2024;  2. Malmgren, J.A., Breast Cancer Res Treat (2018) 167:579–590; 3. National Cancer Institute, Hormone Therapy for Breast Cancer. https://www.cancer.gov/types/breast/breast-hormone-therapy-fact-sheet. Accessed August 27, 2024; 4. ClinicalTrials.gov https://clinicaltrials.gov/study/NCT04606446;  https://clinicaltrials.gov/study/NCT05463952;  https://clinicaltrials.gov/study/NCT05548127; https://clinicaltrials.gov/study/NCT05573555; https://clinicaltrials.gov/study/NCT06125522; https://clinicaltrials.gov/study/NCT06206837; https://clinicaltrials.gov/study/NCT05654623 Accessed October 13, 2025.5. Hamilton EP, et al. Future Oncol. 2024 Jul 29:1-10. doi: 10.1080/14796694.2024.2377530. 6. Hanker A et al. Cancer Cell, Volume 37, Issue 4, 2020, Pages 496-513.