Rigel Announces Availability of VEPPANU™ (vepdegestrant) for Patients with ER+/HER2-, ESR1-Mutated Advanced or Metastatic Breast Cancer

Rhea-AI Summary

Rigel (Nasdaq: RIGL) announced that VEPPANU™ (vepdegestrant), an oral PROteolysis TArgeting Chimera (PROTAC), is now commercially available by prescription in the United States and Puerto Rico. The drug is indicated for adults with ER+/HER2-, ESR1‑mutated advanced or metastatic breast cancer whose disease has progressed after at least one line of endocrine therapy, based on an FDA‑authorized test.

According to Rigel, VEPPANU is the first and only FDA‑approved PROTAC and showed statistically significant, clinically meaningful progression‑free survival improvement versus fulvestrant in a pivotal trial. The recommended dose is 200 mg once daily, priced at $29,400 per 30‑day supply, distributed through specialty distributors and pharmacies. Rigel supports access via its RIGEL ONECARE® patient assistance and reimbursement services and holds an exclusive global license to develop, manufacture and commercialize VEPPANU from Arvinas and Pfizer. The label includes warnings for QTc interval prolongation, embryo‑fetal toxicity, and details on adverse reactions, drug interactions and contraception and lactation guidance.

Positive

• First FDA‑approved PROTAC for ER+/HER2-, ESR1‑mutated advanced or metastatic breast cancer
• Commercial launch with $29,400 list price per 30‑day VEPPANU supply in US and Puerto Rico
• Exclusive global license agreement with Arvinas and Pfizer to develop, manufacture and commercialize VEPPANU
• Pivotal trial showed statistically significant, clinically meaningful progression‑free survival improvement versus fulvestrant

Negative

• Serious adverse reactions in VEPPANU recipients reported in 9% of patients; fatal events in 1.0%
• Permanent treatment discontinuation due to adverse reactions in 2.9%; dose interruptions in 14%; dose reductions in 1.9%
• VEPPANU can cause QTc prolongation; initiation not recommended if QTc >470 msec and requires ECG monitoring
• Label carries embryo‑fetal toxicity warning, requiring effective contraception during treatment and for 2 weeks after last dose for patients and partners

Market Context

Rigel’s August 4 earnings event had a 4.6% 24-hour reaction, providing a recent positive comparison ...

Analysis

Rigel’s August 4 earnings event had a 4.6% 24-hour reaction, providing a recent positive comparison for this commercial launch. The platform record also flags moderate short positioning and recent insider net selling as risks to monitor.

Key Figures

Treatment setting: 2L+ Recommended dosage: 200 mg 30-day supply price: $29,400 +5 more

8 metrics

Treatment setting 2L+ ER+/HER2-, ESR1-mutated advanced or metastatic breast cancer

Recommended dosage 200 mg Taken orally once daily

30-day supply price $29,400 United States and Puerto Rico

Breast cancer population 70% ER+/HER2- represents the majority of breast cancer

ESR1 mutation acquisition up to 50% Patients treated with endocrine therapy and a CDK4/6 inhibitor

Serious adverse reactions 9% Patients who received VEPPANU

Fatal adverse reactions 1.0% Patients who received VEPPANU

Permanent discontinuation 2.9% Due to an adverse reaction

Historical Context

5 past events · Latest: Aug 04 (Positive)

Pattern 5 events

Date	Event	Sentiment	24h Move	Catalyst
Aug 04	Second-quarter earnings	Positive	+4.6%	Revenue, net income, and 2026 revenue outlook increased alongside VEPPANU launch preparation.
Jul 28	Earnings call scheduling	Neutral	+3.0%	Conference call scheduled to discuss second-quarter 2026 financial results.
Jul 07	Inducement grants	Neutral	+5.7%	Restricted stock units granted to six new non-executive employees.
Jul 01	Leadership change	Neutral	-2.1%	Alison L. Hannah became executive vice president and chief medical officer.
Jun 16	License agreement	Positive	+2.8%	Exclusive VEPPANU license closed with Arvinas and Pfizer ahead of August availability.

24h Move is the share-price change in the day after each event; other market factors may also have contributed.

Pattern Detected

The four latest listed events had positive 24-hour reactions, while the July 1 leadership announcement had a -2.12% reaction.

Key Terms

protac, qtc interval prolongation, cyp3a inhibitors, p-gp substrates, +1 more

5 terms

protac medical

"VEPPANU is the first and only FDA-approved PROTAC."

A PROTAC (proteolysis targeting chimera) is a small engineered molecule that tags a specific protein inside cells and brings it to the cell’s disposal machinery so the protein is destroyed rather than just blocked. Think of it as a targeted cleanup crew that removes a problematic part instead of temporarily turning it off. Investors care because PROTACs can tackle disease targets that traditional drugs cannot, creating potential for breakthrough therapies, larger markets, and binary clinical readouts that can sharply affect company value.

qtc interval prolongation medical

"VEPPANU can cause QT (QTc) interval prolongation."

QTc interval prolongation is a lengthening of the heart’s electrical “reset” time measured on an electrocardiogram after adjusting for heart rate; think of it like a loading bar that takes longer than normal to return to zero. It matters to investors because pronounced prolongation can signal a risk of dangerous irregular heartbeats, trigger regulatory review, clinical-trial changes, safety warnings or market setbacks for drugs and medical devices, and therefore can affect a company’s valuation and timelines.

cyp3a inhibitors medical

"Avoid concomitant use of VEPPANU with strong CYP3A inhibitors"

CYP3A inhibitors are drugs or substances that block a key liver and gut protein (CYP3A) responsible for breaking down many medicines; think of the protein as a traffic officer that clears drugs through the body, and an inhibitor as something that slows that traffic. They matter to investors because they can change how other drugs behave—raising safety risks, altering dosing, complicating regulatory approval, and affecting sales or liability for companies with drugs metabolized by CYP3A.

p-gp substrates medical

"Certain P-gp Substrates: Avoid concomitant use with certain P-gp substrates"

P‑gp substrates are drugs that are recognized and pumped out of cells by P‑glycoprotein, a protein that acts like a cellular “bouncer” controlling how much of a medicine gets into tissues such as the gut, liver, kidneys and brain. For investors, whether a drug is a P‑gp substrate matters because it can change how well the drug reaches its target, how it is dosed, and whether it will interact with other medicines—factors that affect safety, efficacy, regulatory review and commercial success.

ugt1a9 substrates medical

"Certain UGT1A9 Substrates: Refer to the Prescribing Information"

UGT1A9 substrates are drugs or chemical compounds that are broken down by the liver enzyme UGT1A9; think of the enzyme as a specific conveyor belt in the body’s recycling plant that tags certain molecules for removal. For investors, knowing whether a medicine is a UGT1A9 substrate matters because this pathway affects how long a drug stays in the body, its safety, dosing, and the risk of interactions with other medicines—factors that influence approval, marketability, and commercial value.

AI-generated analysis. How Rhea-AI works. Not financial advice.

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VEPPANU is the first and only FDA-approved PROTAC and has the potential to become an important new treatment option for adult patients with 2L+ ER+/HER2-, ESR1-mutated mBC

SOUTH SAN FRANCISCO, Calif., Aug. 11, 2026 /PRNewswire/ -- Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL), a commercial stage biotechnology company focused on hematologic disorders and cancer, today announced VEPPANU^TM (vepdegestrant) is now available by prescription in the United States for the treatment of adults with estrogen receptor-positive (ER+)/human epidermal growth factor receptor 2-negative (HER2-), estrogen receptor 1 (ESR1)-mutated advanced or metastatic breast cancer (mBC), as detected by a U.S. Food and Drug Administration (FDA)-authorized test, with disease progression following at least one line of endocrine therapy. 

"The commercial launch of VEPPANU marks an important milestone for Rigel and, more importantly, for patients living with ER+/HER2-, ESR1-mutated advanced or metastatic breast cancer. In a pivotal trial, VEPPANU was generally well tolerated and demonstrated statistically significant and clinically meaningful improvement in progression-free survival versus fulvestrant in this patient population. As the first and only FDA-approved PROTAC, VEPPANU introduces a novel mechanism of action and represents an important new treatment option for healthcare providers to consider with their patients," said Raul Rodriguez, Rigel's president and CEO. "Supported by our established oncology infrastructure, experienced commercial and medical affairs teams and comprehensive patient support programs, we are well positioned to execute a successful commercial launch of VEPPANU, allowing Rigel to deliver for patients while advancing our long-term growth strategy."

VEPPANU is the first and only FDA-approved PROteolysis TArgeting Chimera (PROTAC). PROTACs are a new class of heterobifunctional protein degraders designed to harness the body's natural machinery to selectively degrade, rather than inhibit, disease-causing proteins. The recommended dosage of VEPPANU is 200 mg taken orally once daily. VEPPANU is immediately available through Rigel's network of specialty distributors and specialty pharmacies in the United States and Puerto Rico at $29,400 per 30-day supply.

More information on how to order VEPPANU can be found at www.RIGELONECARE.com.  For those who qualify, Rigel offers patient assistance programs for patients prescribed VEPPANU by their doctor. RIGEL ONECARE^®, the company's comprehensive patient support center, can help patients and physicians as they navigate insurance coverage requirements and provide financial assistance when needed and if eligible, along with other support programs. To learn more, visit www.RIGELONECARE.com or contact RIGEL ONECARE at 833-RIGELOC (833-744-3562).

In May 2026, Rigel announced it entered into an exclusive, global license agreement with Arvinas, Inc. and Pfizer Inc. to develop, manufacture and commercialize VEPPANU.

About ER+/HER2-, ESR1-mutated Metastatic Breast Cancer
Breast cancer is the most common cancer in women in the United States, except for skin cancers.¹ The estrogen receptor-positive/human epidermal growth factor receptor 2-negative (ER+/HER2-) patient population represents the majority (70%) of breast cancer, where treatment with endocrine therapies (aromatase inhibitors) is the standard of care. While endocrine therapy remains a cornerstone of metastatic ER+/HER2- breast cancer treatment, up to 50% of patients treated with endocrine therapy and a CDK4/6 inhibitor acquire estrogen receptor 1 gene (ESR1) mutations, resulting in endocrine resistance and poor prognosis. Treatment options in second-line and later ER+/HER2-, ESR1-mutated advanced or metastatic breast cancer setting include chemotherapy, selective estrogen receptor degraders (SERDs), and as of May 2026, vepdegestrant, the first and only FDA-approved oral PROteolysis TArgeting Chimera (PROTAC).

About VEPPANU^TM (vepdegestrant)

INDICATION
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.

IMPORTANT SAFETY INFORMATION

WARNINGS AND PRECAUTIONS
QTc Interval Prolongation
VEPPANU can cause QT (QTc) interval prolongation. 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. Avoid concomitant use of VEPPANU with strong CYP3A inhibitors or drugs known to prolong the QTc interval.

Embryo-Fetal Toxicity
Based on findings from animal studies and its mechanism of action, VEPPANU can cause fetal harm when administered to a pregnant woman. 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.

ADVERSE REACTIONS
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, dosage interruptions of VEPPANU due to an adverse reaction occurred in 14% of patients, and dosage reductions of VEPPANU due to an adverse reaction occurred in 1.9% of patients.

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.

Clinically relevant adverse reactions in <10% of patients who received VEPPANU included headache, hot flush, diarrhea, vomiting, bradycardia, and urinary tract infection.

DRUG INTERACTIONS

• Strong CYP3A Inhibitors: Avoid concomitant use of VEPPANU with strong CYP3A inhibitors. If concomitant use cannot be avoided, reduce VEPPANU dosage.
• Strong CYP3A Inducers: Avoid concomitant use with strong CYP3A inducers in patients receiving VEPPANU. If concomitant use cannot be avoided, increase VEPPANU dosage.
• Certain P-gp Substrates: Avoid concomitant use with certain P-gp substrates where minimal increases in concentration may lead to serious adverse reactions.
• Certain UGT1A9 Substrates: Refer to the Prescribing Information for UGT1A9 substrates where minimal increases in the concentration may lead to serious adverse reactions.

Avoid concomitant use of VEPPANU with other drugs with a known potential to prolong the QTc interval.

LACTATION
Advise lactating women not to breastfeed during treatment with VEPPANU and for 2 weeks after the last dose.

Click here for Important Safety Information and Full Prescribing Information. 

To report side effects of prescription drugs to the FDA, visit www.fda.gov/medwatch or call 1-800-FDA-1088 (800-332-1088).

VEPPANU is a trademark and RIGEL ONECARE is a registered trademark of Rigel Pharmaceuticals, Inc.

About Rigel
Rigel Pharmaceuticals, Inc. (Nasdaq: RIGL) is a biotechnology company dedicated to discovering, developing and providing novel therapies that significantly improve the lives of patients with hematologic disorders and cancer. Founded in 1996, Rigel is based in South San Francisco, California. For more information on Rigel, the Company's marketed products and pipeline of potential products, visit www.rigel.com.

1. The American Cancer Society. Key Statistics for Breast Cancer. Revised June 24, 2026. Accessed July 30, 2026: https://www.cancer.org/cancer/types/breast-cancer/about/how-common-is-breast-cancer.html

Forward-Looking Statements
This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995 ("PSLRA") relating to, among other things, the potential of VEPPANU (vepdegestrant); Rigel's expectations regarding the commercialization of VEPPANU; the contributions of VEPPANU to Rigel's long-term growth strategy; and the anticipated timing of commercial availability of VEPPANU. Any statements contained in this press release that are not statements of historical fact may be deemed to be forward-looking statements and as such are intended to be covered by the safe harbor for "forward-looking statements" provided by the PSLRA. Forward-looking statements can be identified by words such as "plan", "potential", "may", "anticipates", "expects", "will" and similar expressions in reference to future periods. Forward-looking statements are neither historical facts nor assurances of future performance. Instead, they are based on Rigel's current beliefs, expectations and assumptions and therefore inherently involve significant risks and uncertainties that are difficult to predict and many of which are outside of Rigel's control. Actual results and the timing of events could differ materially from those anticipated in such forward-looking statements as a result of these risks and uncertainties, which include, without limitation, risks related to the successful transfer of development, manufacturing and commercialization responsibilities to Rigel; risks associated with integrating newly acquired or licensed assets; risks related to Rigel's dependence on third parties, including Arvinas and Pfizer, for development, manufacturing and supply activities; risks related to Rigel's ability to successfully launch and commercialize VEPPANU, including uncertainties related to physician adoption, patient demand, market acceptance, reimbursement and pricing; competition from other therapies; regulatory risks, including the risk that regulatory approvals may be subject to limitations or may be withdrawn; risks that clinical trial results may not be predictive of real-world results; risks that VEPPANU may have unintended side effects or adverse reactions; and risks related to Rigel's ability to successfully execute its strategic and commercial plans. There can be no assurance that VEPPANU will achieve the commercial potential anticipated by Rigel or that the license agreement will result in the expected benefits. Additional risks and uncertainties are described in the "Risk Factors" section of Rigel's Quarterly Report on Form 10-Q for the quarter ended June 30, 2026 and in other filings Rigel makes with the Securities and Exchange Commission. Any forward-looking statement made by Rigel in this press release speaks only as of the date on which it is made. Rigel undertakes no obligation to update or revise any forward-looking statements, whether as a result of new information, future developments or otherwise, except as required by law.

Contact for Investors & Media:

Investors:
Rigel Pharmaceuticals, Inc.
650.624.1232
ir@rigel.com 

Media:
David Rosen
Argot Partners
646.461.6387
david.rosen@argotpartners.com

 

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SOURCE Rigel Pharmaceuticals, Inc.

FAQ

What is VEPPANU (vepdegestrant) and which breast cancer patients can receive it?

VEPPANU is an oral PROTAC approved for adults with ER+/HER2-, ESR1‑mutated advanced or metastatic breast cancer after at least one endocrine therapy. According to Rigel, treatment requires an FDA‑authorized ESR1 mutation test to confirm eligibility before prescribing the recommended 200 mg once‑daily dose.

What does the VEPPANU launch mean for Rigel (NASDAQ: RIGL) and its oncology portfolio?

VEPPANU’s launch adds an FDA‑approved oral PROTAC to Rigel’s commercial oncology portfolio. According to Rigel, the product is supported by its existing oncology infrastructure, medical affairs team and RIGEL ONECARE programs, aligning with the company’s stated long‑term growth strategy in hematologic disorders and cancer therapeutics.

How much does VEPPANU cost and how is it supplied in the United States?

VEPPANU is priced at $29,400 per 30‑day supply and taken as 200 mg orally once daily. According to Rigel, it is immediately available through specialty distributors and specialty pharmacies in the United States and Puerto Rico, with ordering details and support via the RIGEL ONECARE program.

What key clinical benefit did VEPPANU show versus fulvestrant in ER+/HER2-, ESR1‑mutated metastatic breast cancer?

According to Rigel, VEPPANU demonstrated statistically significant and clinically meaningful improvement in progression‑free survival versus fulvestrant in a pivotal trial. The company notes the treatment was generally well tolerated in the studied population, supporting its role as a second‑line or later option after endocrine therapy failure.

What are the main safety risks and adverse reactions of VEPPANU reported by Rigel?

VEPPANU can cause QTc interval prolongation and embryo‑fetal toxicity and is associated with serious adverse reactions in 9% of patients. According to Rigel, fatal events occurred in 1.0%, with common laboratory and clinical adverse reactions including cytopenias, liver enzyme elevations, musculoskeletal pain, fatigue and QT prolongation.

Are there important drug interactions and monitoring requirements for VEPPANU treatment?

VEPPANU should be used cautiously with strong CYP3A inhibitors or inducers, certain P‑gp and UGT1A9 substrates, and other QT‑prolonging drugs. According to Rigel, patients require ECG before therapy, repeat ECG around week four, electrolyte correction, contraception counseling, and breastfeeding avoidance for two weeks after the last dose.

What support and patient assistance programs are available for VEPPANU from Rigel (RIGL)?

Rigel offers RIGEL ONECARE, a comprehensive support center that assists with insurance coverage, financial assistance and access to VEPPANU. According to Rigel, eligible patients may receive help with affordability and logistical support, with information available at RIGELONECARE.com or by calling 833‑744‑3562.