Camizestrant

DB19218ApprovedInvestigationalSmall molecule

Camizestrant is an oral selective estrogen receptor degrader used with a CDK4/6 inhibitor for hormone receptor-positive, HER2-negative advanced breast cancer upon emergence of an *ESR1* mutation during first-line endocrine therapy. It binds the ligand binding domain of ERα, antagonizing ERα encoded by both wild-type and mutated ESR1 and inducing proteasome-dependent degradation of the receptor without agonizing it.

Mechanism: Camizestrant is an oral selective estrogen receptor degrader (SERD) and estrogen receptor antagonist. It binds to the ligand binding domain of ERα, antagonizing the activity of ERα encoded by both wild-type ESR1 and mutated ESR1, and induces proteasome-dependent degradation of ERα without agonizing ERα. Camizestrant has demonstrated anti-tumor activity in ER-positive cell lines and patient-derived xenograft models, including those with wild-type or mutated ESR1, and the combination of camizestrant with a CDK4/6 inhibitor showed greater anti-tumor activity than either agent alone in these models.
Curator reviewed · 4 references
Primary indication: United States Camizestrant, in combination with a CDK4/6 inhibitor (abemaciclib, palbociclib, or ribociclib), is indicated for the treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or...Curator reviewed · 9 structured indications
Formula / weight: C₂₄H₂₈F₄N₆ · 476.524 g/mol (avg)
First approval: Canada, 2026 · United States, 2026
Also known as: 3-pyridinamine, n-(1-(3-fluoropropyl)-3-azetidinyl)-6-((6s,8r)-6,7,8,9-tetrahydro-8-methyl-7-(2,2,2-trifluoroethyl)-3h-pyrazolo(4,3-f)isoquinolin-6-yl)- · N-(1-(3-fluoropropyl)-3-azetidinyl)-6-((6s,8r)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3h-pyrazolo(4,3-f)isoquinolin-6-yl)-3-pyridinamine
Code names: AZ-14066724 · AZD-9833