Veppanu vepdegestrant 100 mg Tablet, 30-count — NDC 84043-100-30 (Billing 84043-0100-30)
This is a package of 30 tablets of Veppanu vepdegestrant 100 mg Tablet from Arvinas Operations, Inc., marketed since May 2026 and currently FDA-listed. It is this product's only package size.
NDC database record
One package, one record: these facts belong to NDC 84043-100-30 alone.
- Record
- FDA NDC Directory package listing · Human prescription drug
- Code segments
- 84043 labeler · 100 product · 30 package
- Package marketed since
- May 1, 2026
- Sample package
- No — commercial package
- Listing certified through
- Dec 31, 2027
- Barcode (UPC-A, from the NDC)
- 3 8404310030 0
- FDA record last changed
- Jul 24, 2026
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
- RxCUI (RxNorm): 2743355
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 6, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
Clinical
Vepdegestrant is used to treat a certain type of breast cancer. Vepdegestrant is in a class of medications called selective estrogen receptor degraders (SERDs). It works by blocking estrogen from attaching to cancer cells to help stop the growth of cancer cells.
Read the full MedlinePlus article ↗Patient education
Supplement & herbal interactions
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 6, 2026
Ask a licensed pharmacist directly — free, answered by our team.
Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
Where does this data come from?
- CMS NADAC weekly file
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · refreshed Oct 6, 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Marketing end | Status |
|---|---|---|---|---|
| 84043-0100-30 You're viewing this Main listing | 30 TABLET in 1 BOTTLE | 2026-05-01 | — | Active |
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Veppanu 100 mg 71332-0007-30 | Rigel | 30 tablets | — | — | FDA listed | — |
| Veppanu 100 mgthis 84043-0100-30 | Arvinas | 30 tablets | — | — | FDA listed | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Oct 3, 2026
- CMS NADAC weekly file
Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 11597720 ↗ | Drug substance | U-4278 | Dec 1, 2037 |
| US 11597720 ↗ | Drug substance | U-4278 | Dec 1, 2037 |
| US 10899742 ↗ | Method of use | U-4278 | Dec 1, 2037 |
| US 10899742 ↗ | Method of use | U-4278 | Dec 1, 2037 |
| US 10647698 ↗ | Drug substance | — | Jan 30, 2038 |
| US 10647698 ↗ | Drug substance | — | Jan 30, 2038 |
| Code | What it grants | Expires |
|---|---|---|
| NCE | New Chemical Entity (5-year) | May 1, 2031 |
| NCE | New Chemical Entity (5-year) | May 1, 2031 |
Is there a generic version of this drug?
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Can a generic come out before the last patent expires?
Can a generic come out after the listed dates?
What is the difference between patents and exclusivity?
Why are there multiple patent dates?
Where does this data come from?
- FDA Orange Book · refreshed Oct 3, 2026
What it looks like
Where does this data come from?
- FDA label on DailyMed · label index refreshed Oct 6, 2026
Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII M28OL1HH48
Croscarmellose sodium is a plant-based substance derived from cellulose. It acts as a disintegrant, helping tablets and capsules break down quickly in the digestive system so the medicine can be absorbed.
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UNII L06K8R7DQK
A synthetic blue dye approved by the FDA for use in medications and foods. It serves as a colorant to make pills and liquids visually distinct and easier to identify.
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UNII EX438O2MRT
Ferric oxide yellow is a naturally occurring iron compound used as a colorant in medications. It gives tablets, capsules, and other forms a yellow or golden hue for identification and appearance.
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UNII XM0M87F357
A dark iron oxide compound that gives medicines their black or dark color. It's used as a colorant in tablets and capsules to help identify the product and make it visually distinctive.
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UNII U72Q2I8C85
A mixture of fats derived from coconut oil that acts as an emulsifier and solubilizer. It helps blend oil and water-based ingredients together and improves how the body absorbs certain drugs.
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UNII 3NXW29V3WO
Hypromellose is a plant-based thickener made from cellulose. It's used in medicines as a binder to hold ingredients together, a coating for tablets, and a thickener for liquids.
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UNII EWQ57Q8I5X
Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII 532B59J990
Polyvinyl alcohol is a synthetic polymer made from plant-derived materials. It's used as a binder to hold ingredients together, a film-former in coatings, and a thickener in liquid formulations.
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UNII 23ZQ42JZZH
A synthetic polymer made by chemically linking polyvinyl alcohol to polyethylene glycol. It acts as a binder and film-former to hold tablet ingredients together and create smooth coatings on capsules or tablets.
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UNII ETJ7Z6XBU4
Silicon dioxide is a naturally occurring mineral used as a glidant and anti-caking agent. It helps powder ingredients flow smoothly and prevents clumping during manufacturing and storage.
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UNII 7CV7WJK4UI
Sodium stearyl fumarate is a synthetic compound made from stearyl alcohol and fumaric acid. It acts as a lubricant and glidant in tablets and capsules, helping ingredients flow smoothly during manufacturing and preventing sticking.
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UNII 7SEV7J4R1U
A powder made from a naturally occurring mineral. In medicines, talc works as a glidant and anti-caking agent, helping tablets and capsules flow smoothly during manufacturing and preventing clumping.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
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UNII O03S90U1F2
A synthetic compound combining vitamin E with polyethylene glycol and succinic acid. It acts as a solubilizer and antioxidant in medicines, helping dissolve poorly water-soluble drugs and prevent degradation of active ingredients.
15 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.- FDA label on DailyMed · label index refreshed Oct 6, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
Inactive ingredient FAQ
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Manufacturer & labeler
More NDCs from Arvinas Operations, Inc. labeler code 84043
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE 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.
( 1 )
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION 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)
2.1Patient 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.
2.2Recommended 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.
2.3Dosage 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.
Table 1: Dosage Modifications for Adverse Reactions (Except QTc Prolongation) CTCAE Severity Grade Dosage Modification Grade1 No dose modification is required. Grade 2 Consider interruption of VEPPANU until recovery to Grade ≤1 or baseline. Then resume VEPPANU at the same dose.
Grade 3 First occurrence: Interrupt VEPPANU until recovery to Grade ≤1 or baseline. Then resume VEPPANU at the same dose or at the reduced dose at the discretion of the physician. If the Grade 3 toxicity recurs, interrupt VEPPANU until recovery to Grade ≤1 or baseline.
Then resume VEPPANU at the reduced dose or discontinue VEPPANU at the discretion of the physician. Grade 4 First occurrence: Interrupt VEPPANU until recovery to Grade ≤1 or baseline. Then resume VEPPANU at the reduced dose.
If a Grade 4 or intolerable adverse reaction recurs, permanently discontinue VEPPANU. Abbreviations: CTCAE=National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events Table 2: Dosage Modification and Management for QTc Prolongation QTc Prolongation1 [see Warnings and Precautions (5.1)] Dosage Modification and Management QTc >480 ms or >60 ms increase from baseline (and QTc ≤500 ms) Withhold until QTc resolves to ≤480 ms and ≤60 ms above baseline, then resume VEPPANU at the same dose. Identify and treat reversible causes (e.g., hypokalemia and hypomagnesemia).
Initiate more frequent ECG monitoring. QTc >500 ms Withhold until QTc resolves to ≤480 ms and ≤60 ms above baseline, then: resume VEPPANU at the same dose if reversible cause is identified and corrected (e.g., hypokalemia and hypomagnesemia). resume VEPPANU at the reduced dose if no reversible cause is identified. Initiate more frequent ECG monitoring.
Permanently discontinue if QTc >500 ms recurs. Torsade de Pointes, polymorphic ventricular tachycardia, or signs/symptoms of serious arrhythmia Permanently discontinue VEPPANU. 1 Heart-rate corrected QTc using Fridericia's method.
2.4Dosage Modifications for Drug Interactions Strong CYP3A Inhibitors Avoid concomitant use with strong CYP3A inhibitors in patients receiving VEPPANU 200 mg once daily. If concomitant use cannot be avoided, reduce VEPPANU from 200 mg once daily to 100 mg once daily [see Drug Interactions ( 7.1 )] . After a CYP3A inhibitor has been discontinued for 3 to 5 elimination half-lives, resume VEPPANU 200 mg once daily.
Avoid concomitant use with strong CYP3A inhibitors in patients receiving VEPPANU 100 mg… [Excerpted — this section continues on DailyMed.]
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tablets: 100 mg blue film-coated, immediate release, round tablet debossed with “VEP” on one side and “100” on the other side. 200 mg blue film-coated, immediate release, oval tablet debossed with “VEP” on one side and “200” on the other side. Tablets: 100 mg and 200 mg ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS 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)
5.1QTc 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. Avoid concomitant use of VEPPANU with strong CYP3A inhibitors or drugs known to prolong the QTc interval.
Reduce VEPPANU dose when concomitant use with strong CYP3A inhibitors cannot be avoided [see Dosage and Administration ( 2.4 ), Drug Interactions ( 7.1 , 7.3 ), and Clinical Pharmacology ( 12.2 )] . If concomitant use with other QTc-prolonging agents cannot be avoided, increase the frequency of ECG monitoring. Withhold, reduce dose, or permanently discontinue based on severity [see Dosage and Administration ( 2.3 )] .
5.2Embryo-Fetal Toxicity Based on findings from animal studies and its mechanism of action, VEPPANU can cause fetal harm when administered to a pregnant woman. In an animal reproduction study, oral administration of vepdegestrant to pregnant rats during the period of organogenesis resulted in adverse developmental outcomes, including embryo-fetal mortality and structural abnormalities, at maternal exposures below the recommended dose based on area under the curve (AUC). Advise pregnant women and females of reproductive potential of the potential risk to a fetus.
Advise females of reproductive potential to use effective contraception during treatment with VEPPANU and for 2 weeks after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with VEPPANU and for 2 weeks after the last dose [see Use in Specific Populations ( 8.1 , 8.3 ) and Clinical Pharmacology ( 12.1 )] .
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS 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.
6.1Clinical 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. The serious adverse reactions included any fracture (1.3%), fall, hypercalcemia, hepatic injury, pneumonia, musculoskeletal pain (0.6% each), and QTc prolonged (0.3%).
Fatal adverse reactions occurred in 1.0% of patients who received VEPPANU, including dyspnea, cerebral ischemia, and unknown cause (one patient each). Permanent discontinuation of VEPPANU due to an adverse reaction occurred in 2.9% of patients. Adverse reactions that resulted in permanent discontinuation of VEPPANU included increased alanine aminotransferase (ALT) and dyspnea (0.6% each).
Dosage interruptions of VEPPANU due to an adverse reaction occurred in 14% of patients. Adverse reactions which required dosage interruption in >1% of patients included neutropenia (1.9%), anemia, hepatic injury, nausea, fatigue, and musculoskeletal pain (1.3% each). Dosage reductions of VEPPANU due to an adverse reaction occurred in 1.9% of patients.
Adverse reactions which required dosage reductions of VEPPANU included electrocardiogram QT prolonged, fatigue and musculoskeletal pain (0.3% each). The most common (≥10%) adverse reactions, 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.
Table 3 and Table 4 summarize adverse reactions and laboratory abnormalities in VERITAC-2, respectively. Table 3: Adverse Reactions (≥10%) in Patients with ER+, HER2-, Advanced or Metastatic Breast Cancer Who Received VEPPANU in VERITAC-2a Adverse Reaction VEPPANU N=312 Fulvestrant N=307 All Grades % Grade 3b % All Grades % Grade 3b % Musculoskeletal and Connective Tissue Disorders Musculoskeletal pain c 30 2.6 23 1 General Disorders and Administration Site Conditions Fatigue c 29 1 16
1.3Gastrointestinal Disorders Nausea 14 0 9 1 Constipation 10 0 3.3 0 Metabolism and Nutrition Disorders Decreased appetite 11 0.3 5 0 Investigations Electrocardiogram QT prolonged 10 1.6 1.3 0.3 a Adverse reactions were graded using NCI CTCAE version 5.0 b No Grade 4 events were reported. c Includes multiple related terms. Clinically relevant adverse reactions in <10% of patients who received VEPPANU included headache, hot flush, diarrhea, vomiting, bradyc… [Excerpted — this section continues on DailyMed.]
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Strong CYP3A Inhibitors : Avoid concomitant use with strong CYP3A inhibitors. If concomitant use cannot be avoided, reduce VEPPANU dosage. ( 2.4 , 7.1 ) Strong CYP3A Inducers : Avoid concomitant use with strong CYP3A inducers.
If concomitant use cannot be avoided, increase VEPPANU dosage. ( 2.4 , 7.1 ) Certain P-gp Substrates : Avoid concomitant use with certain P-gp substrates where minimal increases in concentration may lead to serious adverse reactions. ( 7.2 ) Certain UGT1A9 Substrates : Refer to the Prescribing Information for UGT1A9 substrates where minimal increases in concentration may lead to serious adverse reactions.
( 7.2 )
7.1Effect of Other Drugs on VEPPANU Table 5 describes drug interactions where concomitant use of another drug affects VEPPANU. Table 5: Drug Interactions that Affect VEPPANU Strong CYP3A Inhibitors Prevention or Management Strong CYP3A Inhibitors: Avoid concomitant use of VEPPANU with strong CYP3A inhibitors in patients receiving VEPPANU 200 mg once daily. If concomitant use cannot be avoided, reduce VEPPANU dosage [see Dosage and Administration (2.4)] .
Avoid concomitant use with strong CYP3A inhibitors in patients receiving VEPPANU 100 mg once daily. Mechanism and Clinical Effect(s) Vepdegestrant is a CYP3A substrate. Concomitant use with a strong CYP3A inhibitor may increase vepdegestrant plasma concentration [see Clinical Pharmacology (12.3)] , which may increase the risk of VEPPANU-associated adverse reactions.
Strong CYP3A Inducers Prevention or Management Avoid concomitant use with strong CYP3A inducers in patients receiving VEPPANU 200 mg once daily. If concomitant use cannot be avoided, increase VEPPANU dosage [see Dosage and Administration (2.4)] . Avoid concomitant use with strong CYP3A inducers in patients receiving VEPPANU 100 mg once daily.
Mechanism and Clinical Effect(s) Vepdegestrant is a CYP3A substrate. Concomitant use with a strong CYP3A inducer may decrease vepdegestrant plasma concentration [see Clinical Pharmacology (12.3)] , which may reduce the effectiveness of VEPPANU.
7.2Effect of VEPPANU on Other Drugs Table 6 describes drug interactions where concomitant use of VEPPANU affects another drug. Table 6: VEPPANU Drug Interactions that Affect Other Drugs Certain P-gp Substrates Prevention or Management Avoid concomitant use with certain P-gp substrates where minimal increases in concentration may lead to serious adverse reactions. Mechanism and Clinical Effect(s) Vepdegestrant is a P-gp inhibitor.
Vepdegestrant increases exposure of P-gp substrates [see Clinical Pharmacology (12.3)] , which may increase the risk of adverse reactions related to these substrates. Certain UGT1A9 Substrates Prevention or Management Refer to the Prescribing Information for UGT1A9 substrates where minimal increases in the concentration may lead to serious adverse reactions. Mechanism and Clinical Effect(s) Vepdegestrant is a UGT1A9 inhibitor.
Vepdegestrant increases exposure of UGT1A9 substrates [see Clinical Pharmacology (12.3)] , which may increase the risk of adverse reactions related to these substrates.
7.3Drugs that Prolong QTc Interval Avoid concomitant use of VEPPANU with other drugs with a known potential to prolong the QTc interval. If concomitant use cannot be avoided: Obtain ECGs when initiating and during concomitant use, and as clinically indicated [see Warnings and Precautions ( 5.1 )] . Withhold VEPPANU if the QTc interval is >480 ms or the change from baseline is >60 ms [see Dosage and Administration ( 2.3 )] .
Vepdegestrant causes QTc interval prolongation [see Clinical Pharmacology ( 12.2 )] . Concomitant use of VEPPANU with other drugs that prolong the QTc interval may result in a greater increase in the QTc interval and adverse reactions associated with QTc interval prolongation, including Torsade de Pointes, other serious arrythmias, and sudden death [see Warnings and Precautions ( 5.1 )] .
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS Lactation : Advise not to breastfeed. (8.2)
8.1Pregnancy 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).
Additional adverse effects at ≥30 mg/kg/day included reduced fetal weight and skeletal abnormalities including delays in skeletal ossification (reduced number of ossification sites, incompletely ossified cervical arches or thoracic centra), skeletal malformations (fusion of sacral centra, hemivertebrae of the sacrum), and/or increased incidence of fetal variations (short cervical ribs, misaligned caudal vertebrae, misshapen cervical arches, and misaligned sacral vertebrae).
8.2Lactation Risk Summary There are no data on the presence of vepdegestrant or its metabolites in human milk, or its effects on milk production or the breastfed child. Because of the potential for serious adverse reactions in the breastfed child, advise lactating women not to breastfeed during treatment with VEPPANU and for 2 weeks after the last dose.
8.3Females and Males of Reproductive Potential VEPPANU can cause fetal harm when administered to a pregnant woman [see Use in Specific Populations ( 8.1 )] . Pregnancy Testing Verify the pregnancy status in females of reproductive potential prior to initiating VEPPANU treatment. Contraception Females Advise females of reproductive potential to use effective contraception during treatment with VEPPANU and for 2 weeks after the last dose.
Males Advise male patients with female partners of reproductive potential to use effective contraception during treatment with VEPPANU and for 2 weeks after the last dose. Infertility Based on findings from animal studies, VEPPANU may impair fertility in females and males of reproductive potential. The effects of vepdegestrant on fertility were reversible in female animals [see Nonclinical Toxicology ( 13.1 )] .
8.4Pediatric Use The safety and effectiveness of VEPPANU in pediatric patients have not been established.
8.5Geriatric Use Of 313 patients who received VEPPANU in the VERITAC-2 study, 39% were 65 years of age or older and 13% were 75 years of age or older. No overall differences in safety or effectiveness of VEPPANU were observed between patients 65 years of age or older compared to younger patients. There is an insufficient number of patients 75 years of age or older to assess whether there are differences in safety or effectiveness.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Vepdegestrant is a heterobifunctional protein degrader that binds to estrogen receptor (ER) and the E3 ligase cereblon (CRBN). This interaction results in the degradation cascade through CRBN-mediated polyubiquitination and degradation of ER by the proteasome, leading to reduction of ER protein levels in breast cancer cells. Vepdegestrant induced degradation of wild-type (WT) and mutant ER, inhibited ER-dependent breast cancer cell line proliferation in vitro and demonstrated antitumor activity in vivo in both WT and mutant ESR1 breast cancer models.
12.2Pharmacodynamics The exposure-response relationship and time-course of pharmacodynamic response of vepdegestrant have not been fully characterized. Cardiac Electrophysiology The largest mean increase in QTc interval was 12 ms (upper confidence interval = 15 ms) after administration of vepdegestrant at the recommended dosage of 200 mg once daily in patients with ESR1 mutation-positive breast cancer.
12.3Pharmacokinetics Vepdegestrant pharmacokinetics were observed at steady state in patients with ER+/HER2- breast cancer at the approved recommended dosage of 200 mg once daily and are presented as mean (coefficient of variation (CV%)) unless otherwise specified. Vepdegestrant maximum concentration (C max ) is 926 ng/mL (39%), and the total systemic exposure (AUC) is 17155 ng•hr/mL (36%). Vepdegestrant AUC and C max increase in an approximately dose proportional manner over the dose range of 100 mg (0.5 times the approved recommended dose) to 500 mg (2.5 times the approved recommended dose).
Vepdegestrant accumulation is approximately 1.4-fold for AUC and 1.3-fold for C max . Vepdegestrant steady state is reached in approximately 7 days. Absorption Vepdegestrant median (min, max) time to maximum plasma concentration (T max ) is approximately 6 (4, 8) hours.
Effect of Food Vepdegestrant AUC increased 2.9-fold and C max 3.2-fold following administration with a high-fat meal (approximately 800 to 1,000 calories; ≥50% fat). Distribution Vepdegestrant plasma protein binding is >99%. The apparent (oral) volume of distribution is 764 L (26%) following a single 200 mg dose.
Elimination Vepdegestrant effective elimination half-life is 19 hours (50%) with an apparent (oral) clearance of 12 L/h (36%). Metabolism Vepdegestrant is primarily metabolized through direct sulfation via multiple SULT isoforms and oxidation via CYP3A4 and to a lesser extent by CYP2C8, CYP2C9 and CYP3A5. Unchanged total vepdegestrant represented 92% of total radioactivity in plasma.
Excretion Following a single oral dose of radiolabeled vepdegestrant 200 mg to healthy subjects, approximately 68% of the dose was recovered in feces (18% unchanged) and 1.5% in urine (<0.02% unchanged). Specific Populations No clinically significant differences in the pharmacokinetics of vepdegestrant were observed based on age (26 to 89 years), sex, body weight (37 to 181 kg), race (60% White, 27% Asian, 2.2% Black or African American, and 10% other), CLcr 30 mL/min to 90 mL/min (estimated by Cockcroft Gault equation) or mild hepatic impairment (total bilirubin ≤ULN and AST>ULN or total bilirubin >1 to 1.5 × ULN and any AST).
The effect of moderate hepatic impairment (total bilirubin >1.5 to 3 × ULN and any AST), severe hepatic impairment (total bilirubin > 3 x ULN and any AST), CLcr 15 to < 30 mL/min, and end-stage renal disease (CLcr < 15 mL/min) on the pharmacokinetics of vepdegestrant is unknown. Drug Interaction Studies Clinical Studies and Model-Informed Approaches Strong CYP3A Inhibitors : Vepdegestrant AUC increased 1.7-fold and C max 1.5-fold following concomitant use of itraconazole (strong CYP3A inhibitor) 200 mg once daily. Strong CYP3A Inducers: Vepdegestrant AUC decreased to 64% and C max to 80% following concomitant use of carbamazepine (strong CYP3A inducer) 200 mg three times daily.
Acid Reducing Agents: Vepdegestrant AUC decreased to 84% and C max to 74% following conc… [Excerpted — this section continues on DailyMed.]
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied VEPPANU (vepdegestrant) film-coated tablets for oral use are supplied in bottles of 30 tablets with child‑resistant closures as follows: Strength Description NDC Number 100 mg Blue round tablet “VEP” debossed on one side and “100” on the other side. 84043-100-30 200 mg Blue oval tablet “VEP” debossed on one side and “200” on the other side. 84043-200-30 Storage Store at 20°C to 25°C (68°F to 77°F).
Excursions permitted between 15°C and 30°C (between 59°F and 86°F) [see USP controlled room temperature].
📋 Description ▾
11 DESCRIPTION Vepdegestrant is a heterobifunctional protein degrader. It is a small molecule comprised of an estrogen receptor binding domain joined by a linker to an E3 ligase binding domain. The chemical name of vepdegestrant is 2,6-piperidinedione, 3-[1,3-dihydro-1-oxo-5-[4-[[1-[4-[(1 R ,2 S )-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl]phenyl]-4-piperidinyl]methyl]-1-piperazinyl]-2 H -isoindol-2-yl]-, (3 S )-.
The chemical structure of vepdegestrant is: Vepdegestrant is white to off-white to pale yellow solid with the molecular formula of C 45 H 49 N 5 O 4 and a molecular weight of 723.90 Daltons. Vepdegestrant solubility is pH dependent. The solubility ranges from freely soluble under gastric pH conditions to slightly soluble under intestinal pH conditions.
VEPPANU is supplied as blue film-coated, immediate release tablets containing either 100 mg or 200 mg vepdegestrant together with: colloidal silicon dioxide, croscarmellose sodium, hypromellose, lactose monohydrate, microcrystalline cellulose, sodium stearyl fumarate, vitamin E-polyethylene glycol succinate, and Opadry ® QX Blue as inactive ingredients. Opadry ® QX Blue film-coating contains: FD&C Blue No. 2 (indigo carmine) aluminum lake, ferric oxide yellow (yellow iron oxide), ferrosoferric oxide (black iron oxide), glyceryl mono and dicaprylocaprate (glycerol monocaprylocaprate), polyvinyl alcohol, polyvinyl alcohol polyethylene glycol graft copolymer [macrogol poly (vinyl alcohol) grafted copolymer], talc, and titanium dioxide. chemstructure
🔬 Clinical Studies ▾
14 CLINICAL STUDIES The efficacy of VEPPANU was evaluated in VERITAC-2 (NCT05654623), a randomized, open-label, active-controlled, multicenter trial that enrolled 624 adult patients with ER-positive, HER2-negative, advanced or metastatic breast cancer, of whom 270 patients had tumors carrying ESR1 mutations. Patients were required to have disease progression on 1 to 2 prior lines of endocrine therapy, including 1 line with a CDK4/6 inhibitor. Progression during or within 12 months from the end of adjuvant therapy was counted as 1 line of endocrine therapy for advanced/metastatic setting.
Pre-menopausal and peri-menopausal women and men received a gonadotropin-releasing hormone (GnRH) agonist. Patients were excluded if they had received chemotherapy for advanced or metastatic disease or fulvestrant in any line of therapy, or if progression on the most recent line of endocrine therapy occurred within the first 6 months. Patients were randomized 1:1 to receive VEPPANU 200 mg orally once daily (N=313), or fulvestrant 500 mg intramuscularly on Days 1 and 15 of Cycle 1 and then once monthly thereafter (N=311).
Randomization was stratified by ESR1 mutation status (detected vs. not detected) and visceral metastasis (yes vs. no). ESR1 mutational status was determined by blood circulating tumor deoxyribonucleic acid (ctDNA) using central or local testing. Patients were treated until disease progression or unacceptable toxicity.
Among the patients whose tumors had ESR1 mutations (N=270), the median age was 60 (range: 26 to 87) years; all but 1 were female; 47% were White; 41% Asian; 3.3% Black; 8% unknown/not reported; 7% were Hispanic/ Latino, 83% were Not Hispanic or Latino and 10% not reported. Of the 269 women, 20% were pre/perimenopausal. Baseline Eastern Cooperative Oncology Group (ECOG) performance status was 0 (57%) or 1 (43%).
Most patients (68%) had visceral disease; 81% had received 1 line of endocrine therapy and 19% had received 2 lines of endocrine therapy in the advanced or metastatic setting. All patients had received prior treatment with a CDK4/6 inhibitor. The major efficacy outcome was progression-free survival (PFS) as assessed by blinded independent central review (BICR) in the population of patients whose tumors had an ESR1 mutation and in the overall population evaluated according to Response Evaluation Criteria in Solid Tumors (RECIST), version 1.1.
Additional efficacy outcomes were overall survival (OS) and objective response rate (ORR) as assessed by BICR. A statistically significant difference in PFS by BICR was observed for the patients whose tumors had ESR1 mutations for VEPPANU compared with fulvestrant. Overall survival was immature with 16% of deaths in this population at the time of the PFS analysis.
Efficacy results are provided in Table 7 and Figure 1. Table 7: Efficacy Results for VERITAC-2 (Patients with ESR1-Mutated Tumors) VEPPANU N=136 Fulvestrant N=134 Progression-free Survival* Number of events (%) 79 (58) 95 (71) Median in months (95% CI) 5.0 (3.7, 7.4) 2.1 (1.9, 3.5) Hazard ratio (95% CI)a 0.57 (0.42, 0.77) p-value (1-sided)b 0.0001 Confirmed Objective Response Rate* Patients with measurable disease 97 100 ORR (95% CI) 19% (12, 27) 4% (1.6, 10) Complete response rate 0% 0% Partial response rate 19% 4% Abbreviations: CI=Confidence interval; n=number of events; N=number of participants * By blinded independent central review (BICR). a Hazard ratio based on stratified Cox proportional hazards model. b p-value based on stratified log-rank test (compared to a significance level of 0.01875). figure1
🧪 Nonclinical Toxicology ▾
13 NONCLINICAL TOXICOLOGY
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenesis Vepdegestrant was not carcinogenic in a 6-month carcinogenicity study in rasH2 transgenic mice with daily oral administration of vepdegestrant up to 800 mg/kg/day. Mutagenesis Vepdegestrant was not mutagenic in an in vitro bacterial reverse mutation assay (Ames) or clastogenic in an in vitro human lymphocyte micronucleus assay or an in vivo rat micronucleus assay. Impairment of Fertility Fertility studies with vepdegestrant in animals have not been conducted.
In repeat-dose toxicity studies up to 26 weeks duration in rats and 39 weeks duration in dogs, oral administration of vepdegestrant resulted in adverse female reproductive effects including atrophy of the uterus, oviduct, cervix and vagina and follicular cysts in rats at doses > 30 mg/kg/day (0.3 times the human AUC at the recommended dose) and in dogs at doses > 10 mg/kg/day (0.4 times the human AUC at the recommended dose). Additional findings in the ovary in rats included decreased corpora lutea and follicle hemorrhage at > 30 mg/kg/day.
Oral administration of vepdegestrant resulted in adverse male reproductive effects including decreased epididymis and prostate weights with decreased secretion and decreased secretion in the seminal vesicle in rats at doses > 30 mg/kg/day, and seminiferous tubular degeneration, hypoplasia of seminiferous tubules, and epididymal epithelial cell necrosis in dogs at 90 mg/kg/day (approximately 2 times the human AUC at the recommended dose). The effects of vepdegestrant on female reproductive organs were reversible following a 4-week recovery period.
The effects on male reproductive organs were not reversible following a 4-week recovery period.
13.2Animal Toxicology and/or Pharmacology In a 6-month repeat-dose toxicity study, oral administration of vepdegestrant to rats resulted in granulosa cell hyperplasia in the ovary at 300 mg/kg/day (5 times the human AUC at the recommended dose). In a 9-month repeat-dose toxicity study, oral administration of vepdegestrant to dogs resulted in interstitial cell hypertrophy/hyperplasia in the testis at doses ≥10 mg/kg/day (0.4 times the human AUC at the recommended dose). Reversibility was not assessed.
📄 Patient Package Insert ▾
PATIENT INFORMATION PATIENT INFORMATION VEPPANU (VEP-uh-new) (vepdegestrant) tablets, for oral use What is VEPPANU? VEPPANU is a prescription medicine to treat people with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, estrogen receptor-1 (ESR1) -mutated advanced breast cancer or breast cancer that has spread to other parts of the body (metastatic), and whose disease has progressed after at least one line of endocrine-based therapy. Your healthcare provider will perform a test to make sure that VEPPANU is right for you.
It is not known if VEPPANU is safe and effective in children. Before taking VEPPANU, tell your healthcare provider about all of your medical conditions, including if you: have heart failure or heart rhythm problems, including QTc prolongation, and long QTc syndrome have low blood levels of potassium or magnesium are pregnant or plan to become pregnant. VEPPANU can harm your unborn baby.
Females who are able to become pregnant: o Your healthcare provider may do a pregnancy test before you start treatment with VEPPANU. o Use effective birth control (contraception) during treatment with VEPPANU and for 2 weeks after the last dose. o Tell your healthcare provider right away if you become pregnant or think you may be pregnant during treatment with VEPPANU. Males with female partners who are able to become pregnant: o Use effective birth control (contraception) during treatment with VEPPANU and for 2 weeks after the last dose. are breastfeeding or plan to breastfeed.
It is not known if VEPPANU passes into your breast milk. Do not breastfeed during treatment with VEPPANU and for 2 weeks after the last dose. Tell your healthcare provider about all the medicines you take, including prescription and over-the counter medicines, vitamins, and herbal supplements.
VEPPANU and other medicines may affect the way each other works and may cause serious side effects. Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine.
How should I take VEPPANU? • Take VEPPANU exactly as your healthcare provider tells you. • Do not change your dose or stop taking VEPPANU unless your healthcare provider tells you. • Take VEPPANU 1 time each day. • Take VEPPANU with food. • Swallow VEPPANU tablets whole. Do not chew, crush, dissolve, or split the tablets before swallowing. • Do not take VEPPANU tablets that are broken, cracked, or look damaged. • If you miss a dose or vomit after taking VEPPANU, do not take another dose of VEPPANU on that day. Take your next dose the following day at your regularly scheduled time.
Do not take 2 doses on the next treatment day. What should I avoid while taking VEPPANU? Avoid taking St.
John's wort, eating grapefruit, or drinking grapefruit juice during treatment with VEPPANU. What are the possible side effects of VEPPANU? VEPPANU can cause serious side effects, including: • Heart rhythm problems (QTc interval prolongation).
VEPPANU can cause changes in the electrical activity of your heart and may increase your risk of abnormal heart rhythm problems, and sudden death. Your healthcare provider will check your heart with a test called an electrocardiogram (ECG) and check your blood potassium and magnesium levels before and as needed during treatment with VEPPANU. Get emergency medical help right away if you get any signs and symptoms of abnormal heart rhythm, including: o feeling lightheaded or faint o dizziness o feeling that your heart is pounding or beating fast (heart palpitations) o shortness of breath o chest pain The most common side effects of VEPPANU include: decreased white blood cell counts increased liver function tests muscle and bone pain tiredness decreased red blood cell counts nausea decreased potassium levels in your blood decreased appetite abnormal electrocardiogram (QT prolonged) decreased platelet counts constipation Your healthcare provider may decrease your dose, temporarily stop… [Excerpted — this section continues on DailyMed.]
📄 Package Label / Principal Display Panel ▾
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL NDC 84043-100-30 VEPPANU TM (vepdegestrant) tablets 100 mg ARVINAS Pfizer 30 Tablets Rx only vep100
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL NDC 84043-200-30 VEPPANU TM (vepdegestrant) tablets 200 mg ARVINAS Pfizer 30 Tablets Rx only vepp200
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