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Vepdegestrant is the first PROTAC ever approved (2026): a pill that tags the oestrogen receptor for destruction, for breast cancers with ESR1 mutations.
Vepdegestrant is a PROTAC: a heterobifunctional molecule with one end binding oestrogen receptor alpha and the other recruiting the cereblon E3 ligase, tagging the receptor for proteasomal destruction rather than simply blocking it. Taken as 200 mg once daily, it was approved in Q2 2026 for ESR1-mutated ER-positive, HER2-negative advanced breast cancer after endocrine therapy, the first PROTAC ever approved (Arvinas/Pfizer). In VERITAC-2 it improved progression-free survival versus fulvestrant to 5.0 versus 2.1 months (HR 0.57) in ESR1-mutant disease after CDK4/6 and endocrine therapy, but showed no benefit in the overall population, so the label is restricted to ESR1-mutant tumours. The absolute gain is modest, and combinations with CDK4/6 inhibitors are the next test. For a newcomer: a pill that dismantles the oestrogen receptor instead of just blocking it.
Ball-and-stick model from PubChem 2D record (no 3D conformer available). PubChem record
Heterobifunctional molecule recruiting cereblon E3 ligase to ERα for proteasomal degradation. Connects to Estrogen receptor (ERα).
1.Oral heterobifunctional molecule enters the tumour cell
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
Source: www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications. Doses are for orientation; the current label governs.
Sources: NICE search: vepdegestrant. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
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Fast Track designation source
NDA submitted (VERITAC-2) source
ESR1-mutated ER+/HER2- advanced breast cancer after endocrine therapy: first PROTAC approved source
| Region | Year | Indication |
|---|---|---|
| US | 2026 | ESR1-mutated ER+/HER2- advanced or metastatic breast cancer after endocrine therapy |
| Adverse event |
|---|
| Fatigue |
| Nausea |
| Arthralgia |
| Hot flush |
| Transaminase increase |
Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.
| Country | Reimbursement | List price | Assistance |
|---|---|---|---|
| United States | Medicare Part D (oral); commercial plans per formulary, often with prior authorisation | not disclosed | pfizeroncologytogether.com |
List prices are manufacturer or Medicare figures where publicly disclosed; net prices after rebates are usually lower. Reimbursement changes; check the payer.
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Query for this drug: (TITLE:"Vepdegestrant" OR ABSTRACT:"Vepdegestrant" OR TITLE:"Veppanu" OR ABSTRACT:"Veppanu" OR TITLE:"ARV-471" OR ABSTRACT:"ARV-471") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Vepdegestrant, not a curated reading list.
Shares Oral SERDs, ESR1 mutation, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Estrogen receptor (ERα).
Shares Oral SERDs, ESR1 mutation, Oestrogen receptor signalling, Hormone therapy.
Shares A Study to Learn About Vepdegestrant When Given With PF-07220060 to People With Advanced or Metastatic Breast Cancer., Study of PF-07248144 in Advanced or Metastatic Solid Tumors, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test.
Shares ESR1 mutation, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Estrogen receptor (ERα), Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test.
Shares ESR1 mutation, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Estrogen receptor (ERα), Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test.
Shares 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), HR-positive metastatic breast cancer after CDK4/6 inhibitors, Pfizer (incl. Seagen), HR-positive / HER2-negative breast cancer.
Shares HR-positive metastatic breast cancer after CDK4/6 inhibitors, Estrogen receptor (ERα), Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test, Endocrine therapy (SERMs, AIs, SERDs).
Shares Oral SERDs, ESR1 mutation, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Estrogen receptor (ERα).