Vepdegestrant

• VEPPANU is indicated for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1) -mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy. VEPPANU is a heterobifunctional protein degrader indicated for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 ( ESR1) -mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy.ICD-10: C50.919

• None. None.contraindicated

Select patients for treatment with VEPPANU based on the presence of ESR1 mutation. (2.1) Recommended Dosage : 200 mg orally once daily with food. (2.2) Interruption, dose reduction, or permanent discontinuation may be required due to adverse reactions. (2.3) 2.1 Patient Selection Select patients for treatment of ER-positive, HER2-negative advanced or metastatic breast cancer with VEPPANU based on the presence of ESR1 mutation(s) in plasma specimen using an FDA-authorized test [see Indications and Usage ( 1 ) and Clinical Studies ( 14 )] . Information on FDA-authorized tests for detection of ESR1 mutations in breast cancer is available at: http://www.fda.gov/CompanionDiagnostics. 2.2 Recommended Dosage and Administration The recommended dosage of VEPPANU is 200 mg taken orally once daily with food [see Clinical Pharmacology ( 12.3 )] until disease progression or unacceptable toxicity. Swallow VEPPANU tablet(s) whole. Do not chew, crush, dissolve, or split prior to swallowing. Do not take VEPPANU tablets that are broken, cracked, or look damaged. If a patient misses a dose or vomits after taking a dose, the patient should take the next dose at the regularly scheduled time. 2.3 Dosage Modifications for Adverse Reactions The recommended dose reduction for adverse reactions is 100 mg orally once daily. Permanently discontinue VEPPANU in patients who are unable to tolerate 100 mg orally once daily. The recommended dosage modifications for VEPPANU for adverse reactions are provided in Table 1 and Table 2.

QTc Interval Prolongation : Monitor electrocardiograms (ECGs) and electrolytes prior to initiation of treatment with VEPPANU. Correct hypokalemia and hypomagnesemia prior to and during treatment. Repeat ECGs as clinically indicated. Withhold, reduce dose, or permanently discontinue VEPPANU based on severity. (5.1) Embryo-Fetal Toxicity : VEPPANU can cause fetal harm. Advise patients of the potential risk to a fetus and to use effective contraception. (5.2, 8.1, 8.3) 5.1 QTc Interval Prolongation VEPPANU can cause QT (QTc) interval prolongation [see Clinical Pharmacology ( 12.2 )] . In VERITAC-2, QTc interval prolongation was reported in 10% of patients; Grade 3 occurred in 1.6% of patients. The heart-rate corrected QTc interval using Fridericia’s method was greater than 500 msec in 1.6% of patients, and the increase from baseline QTc was greater than 60 msec in 2.6% of patients. VEPPANU dose reduction was required for 0.3% of patients due to QTc interval prolongation [see Adverse Reactions ( 6.1 )] . Correct electrolyte abnormalities, including hypokalemia and hypomagnesemia, prior to and during treatment with VEPPANU. Perform an ECG prior to initiation of treatment with VEPPANU, and do not initiate VEPPANU in patients with QTc > 470 msec. Repeat ECG approximately 4 weeks after initiating treatment and as clinically indicated. In patients with congenital long QTc syndrome, congestive heart failure, electrolyte abnormalities, or those who are taking medications known to prolong the QTc interval, additional ECG monitoring may be necessary.

The following clinically significant adverse reaction is described elsewhere in the labeling: QTc Interval Prolongation [see Warnings and Precautions ( 5.1 )] Most common ( > 10%) adverse reactions with VEPPANU, including laboratory abnormalities, were decreased white blood cells, increased AST, musculoskeletal pain, fatigue, decreased hemoglobin, decreased neutrophils, increased ALT, increased alkaline phosphatase, nausea, decreased blood potassium, increased bilirubin, decreased appetite, electrocardiogram QT prolonged, decreased platelets, and constipation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc at 1-877-702-7846 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of VEPPANU was evaluated in patients with ER-positive, HER2-negative, advanced or metastatic breast cancer following endocrine therapy in VERITAC-2 [see Clinical Studies (14)]. Patients received VEPPANU 200 mg orally once daily (N=312) or fulvestrant 500 mg intramuscularly on Days 1 and 15 of Cycle 1 and then on Day 1 of each subsequent 28-day cycle (N=307). Among patients who received VEPPANU, 33% were exposed for 6 months or longer and 6% were exposed for greater than one year. Serious adverse reactions occurred in 9% of patients who received VEPPANU.

Lactation : Advise not to breastfeed. (8.2) 8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, VEPPANU can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 ) ]. There are no available human data on the use of VEPPANU in pregnant women to inform the drug-associated risk. In an animal reproduction study, oral administration of vepdegestrant to pregnant rats during the period of organogenesis caused adverse developmental outcomes, including embryo-fetal mortality and structural abnormalities at maternal exposures below the recommended dose based on AUC ( see Data ). Advise pregnant women and females of reproductive potential of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In an embryo-fetal development study in pregnant rats, administration of oral doses of vepdegestrant up to 300 mg/kg/day during the period of organogenesis resulted in embryo-fetal mortality (increased resorptions, post-implantation loss and reduced number of live fetuses) at ≥30 mg/kg/day (approximately 0.3 times the human AUC at the recommended dose).

• May 1, 2026NDANDA219835Arvinas Operations

1. 1Fall1100%

The 10 most recently updated of 20 ClinicalTrials.gov registrations naming Vepdegestrant as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer. (Sub-Study C)
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 11 enrolled · Pfizer
  NCT06125522updated 2026-05-06
• Study of PF-07248144 in Advanced or Metastatic Solid Tumors
  Recruiting · Phase 2 · Interventional · 320 enrolled · Pfizer
  NCT04606446updated 2026-04-16
• A Phase 1/2 Trial of ARV-471 Alone and in Combination With Palbociclib (IBRANCE®) in Patients With ER+/HER2- Locally Advanced or Metastatic Breast Cancer
  Completed · Phase 1 · Phase 2 · Interventional · 217 enrolled · Arvinas Estrogen Receptor, Inc.
  NCT04072952updated 2026-04-15
• A Study to Learn How the Body Processes the Study Medicine Called Vepdegestrant in People With Loss of Liver Function
  Recruiting · Phase 1 · Interventional · 24 enrolled · Pfizer
  NCT07231991updated 2026-04-03
• A Study to Learn About a New Medicine Called Vepdegestrant (ARV-471, PF-07850327) in People Who Have Advanced Metastatic Breast Cancer
  Active not recruiting · Phase 3 · Interventional · 624 enrolled · Pfizer
  NCT05654623updated 2026-03-18
• TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer (Sub-Study B)
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 20 enrolled · Pfizer
  NCT05573555updated 2026-03-09
• A Study to Learn About Vepdegestrant When Given With PF-07220060 to People With Advanced or Metastatic Breast Cancer.
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 71 enrolled · Pfizer
  NCT06206837updated 2026-02-27
• TACTIVE-U: A Study to Learn About the Study Medicine (Vepdegestrant) When Given With Other Medicines in People With Advanced or Metastatic Breast Cancer (Sub-Study A)
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 37 enrolled · Pfizer
  NCT05548127updated 2026-02-10
• Vepdegestrant (ARV-471/PF-07850327) + Palbociclib vs Letrozole + Palbociclib in ER(+)/HER2(-) Advanced Breast Cancer
  Active not recruiting · Phase 3 · Interventional · 59 enrolled · Pfizer
  NCT05909397updated 2026-02-10
• ARV-471 in Combination With Everolimus for the Treatment of Advanced or Metastatic ER+, HER2- Breast Cancer
  Completed · Phase 1 · Interventional · 32 enrolled · Arvinas Estrogen Receptor, Inc.
  NCT05501769updated 2025-09-26

Frequently asked questions

What is Vepdegestrant used for?

According to FDA labeling, Vepdegestrant carries indications including: VEPPANU is indicated for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1) -mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy. VEPPANU is a heterobifunctional protein degrader indicated for the treatment of adults with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 ( ESR1) -mutated advanced or metastatic breast cancer, as detected by an FDA-authorized test, with disease progression following at least one line of endocrine therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What are the brand names for Vepdegestrant?

Vepdegestrant is marketed under brand names including Veppanu.

What are the contraindications for Vepdegestrant?

Vepdegestrant labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.