FDA approves vepdegestrant for ESR1-mutated ER-positive advanced breast cancer

On May 1, 2026 the FDA gave its first approval to vepdegestrant, an oral selective estrogen receptor degrader, for adult patients with estrogen receptor-positive, HER2-negative breast cancer that carries ESR1 mutations and has progressed after at least one endocrine therapy line. The approval requires detection of the ESR1 mutation with an FDA-authorized test.

Vepdegestrant works by linking the estrogen receptor to an E3 ubiquitin ligase, prompting the receptor’s degradation. This mode of action sets it apart from other oral SERDs that are currently in development.

According to Dr. Kelly Elizabeth McCann of UC San Diego, the drug’s value will likely be realized in combination regimens, and ongoing trials will explore its use with other targeted agents.