South San Francisco, California, August 13, 2026
Rigel Pharmaceuticals, Inc. announced the U.S. commercial availability of VEPPANU™ (vepdegestrant) for adults with estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-), ESR1-mutated advanced or metastatic breast cancer whose disease has progressed following at least one line of endocrine therapy. The therapy is indicated when the ESR1 mutation is identified using an FDA-authorized test. VEPPANU is the first and only FDA-approved PROTAC, introducing a targeted protein-degradation approach into the treatment of this breast cancer population.
VEPPANU Introduces a New PROTAC Treatment Approach
VEPPANU is a proteolysis-targeting chimera (PROTAC), a class of heterobifunctional protein degraders designed to harness the body’s natural cellular machinery to selectively remove disease-associated proteins rather than simply inhibit their activity. The treatment is administered as an oral 200 mg dose once daily, providing a convenient oral treatment option for eligible patients. Rigel announced that VEPPANU is immediately available through its network of specialty distributors and specialty pharmacies in the United States and Puerto Rico. The commercial launch follows Rigel’s exclusive global licensing agreement with Arvinas and Pfizer, announced in May 2026, under which Rigel obtained rights to develop, manufacture and commercialize VEPPANU. The launch represents an important expansion of Rigel’s oncology portfolio and establishes the company’s commercial presence with a novel targeted therapy for a genetically defined breast cancer population.
Targeting ESR1-Mutated Breast Cancer
ER+/HER2- breast cancer represents approximately 70% of breast cancer cases, making it the largest breast cancer subtype. Endocrine therapy remains a cornerstone of treatment for metastatic ER+/HER2- disease, but resistance can develop during treatment. According to Rigel, up to 50% of patients treated with endocrine therapy and a CDK4/6 inhibitor acquire ESR1 mutations, which can contribute to endocrine resistance and poorer outcomes. VEPPANU is specifically indicated for patients whose tumors harbor ESR1 mutations and whose disease has progressed after at least one line of endocrine therapy. The development of therapies targeting this molecularly defined population reflects the increasing role of biomarker-driven treatment strategies in breast cancer. In this setting, treatment selection relies on identifying the relevant ESR1 mutation through an FDA-authorized diagnostic test. Rigel reported that VEPPANU demonstrated a statistically significant and clinically meaningful improvement in progression-free survival compared with fulvestrant in its pivotal clinical trial. The company described the therapy as generally well tolerated and highlighted its novel mechanism as an important addition to treatment options for patients with ESR1-mutated advanced or metastatic breast cancer.
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Safety and Commercial Availability
The launch also brings important safety considerations for physicians and patients. VEPPANU can cause QTc interval prolongation, and the prescribing information recommends correcting electrolyte abnormalities before and during treatment, performing an ECG before initiation, and avoiding treatment initiation in patients with QTc greater than 470 milliseconds. The drug should also be used carefully with certain medications that affect QTc or CYP3A pathways. Rigel reported that serious adverse reactions occurred in 9% of patients, while permanent treatment discontinuation due to an adverse reaction occurred in 2.9%. Common adverse reactions and laboratory abnormalities included decreases in white blood cells, neutrophils, hemoglobin and platelets, as well as increased liver enzymes, musculoskeletal pain, fatigue, nausea, decreased appetite, constipation and QT prolongation.
VEPPANU is available at a listed price of $29,400 per 30-day supply, with Rigel’s patient support program providing assistance with insurance coverage and financial support for eligible patients. The commercial launch marks a significant milestone for Rigel Pharmaceuticals and the emerging PROTAC therapeutic class. By bringing an FDA-approved targeted protein degrader to patients with ESR1-mutated breast cancer, Rigel is expanding the treatment landscape while advancing the application of protein degradation technology in oncology.
Source: Rigel Pharmaceuticals press release
