VEPPANU™ (vepdegestrant): A First-in-Class FDA-Approved Breast Cancer Treatment Using PROTAC Technology

Jul 27, 2026

What is it prescribed for?

VEPPANU is prescribed for adults with estrogen receptor (ER)-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer whose disease has worsened after at least one type of endocrine therapy. Breast cancer cells in this subtype depend on estrogen signals to grow. Over time, many tumors develop ESR1 mutations, which can make standard hormone therapies stop working. Patients with these mutations often have fewer treatment options once resistance develops. VEPPANU is important because it introduces an entirely new treatment approach for hormone-resistant breast cancer. The FDA approved VEPPANU on May 1, 2026.

What is the name of the drug and what does it do?

The medication is VEPPANU™ (vepdegestrant), an oral targeted cancer therapy taken by mouth. It is the first FDA-approved PROTAC (proteolysis-targeting chimera) therapy, a new type of medicine designed to destroy harmful proteins inside cancer cells instead of only blocking them. VEPPANU specifically targets the estrogen receptor, which many breast cancers use to survive and grow. By removing these receptors, the drug helps slow cancer progression in patients whose tumors no longer respond well to standard endocrine therapy.

How does it work?

VEPPANU works differently from traditional hormone therapies. It is a heterobifunctional protein degrader, also called a PROTAC. Instead of simply attaching to the estrogen receptor and blocking it, VEPPANU marks the receptor for destruction by the cell’s natural protein recycling system.

This process:

  • Removes estrogen receptors from cancer cells
  • Reduces estrogen-driven tumor growth
  • Helps overcome resistance caused by ESR1 mutations

Because it destroys the receptor itself, VEPPANU may remain effective even when older endocrine therapies stop working.

What did the research discover?

VEPPANU was studied in the VERITAC-2 clinical trial, which compared the drug with fulvestrant in patients with advanced breast cancer containing ESR1 mutations. Patients taking VEPPANU had improved progression-free survival, meaning their cancer stayed controlled longer before worsening.

Research also showed:

  • More tumors responded to VEPPANU than fulvestrant
  • Some patients experienced longer disease stabilization
  • Benefits were especially important in endocrine-resistant cancer

The approval marked a major milestone because VEPPANU became the first FDA-approved PROTAC therapy in medicine.

What are some of the side effects?

Common side effects included:

  • Fatigue
  • Nausea
  • Muscle or joint pain
  • Decreased appetite
  • Constipation

Laboratory abnormalities were also reported, including:

  • Low white blood cell counts
  • Increased liver enzyme levels
  • Low potassium levels
  • QT interval prolongation on ECG testing

Patients receiving VEPPANU require regular blood work and monitoring during treatment.

What are the dosage recommendations and how is it prescribed?

VEPPANU is taken by mouth as a tablet once daily. The exact dose may depend on tolerability and side effects. Treatment continues as long as the cancer remains controlled and side effects stay manageable. Doctors monitor patients closely with blood tests and imaging studies during therapy.

Because VEPPANU targets ESR1-mutated cancer, patients must first undergo testing with an FDA-authorized diagnostic test to confirm the mutation before treatment begins.

Source:

VEPPANU™ (vepdegestrant) tablets, for oral use [prescribing information]. New Haven (CT): Arvinas Operations, Inc.; 2026. Available from: https://www.arvinas.com/wp-content/uploads/2026/05/NDA-219835_Approval-Rx-ONLY.pdf. Accessed by: June 6, 2026.

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