alisertib + fulvestrant

Alisertib + fulvestrant is a combination therapy that has been investigated for the treatment of endocrine-resistant, HER2-negative metastatic breast cancer, particularly in patients who had progressed on prior CDK4/6 inhibitor therapy. Alisertib is a highly selective, reversible, ATP-competitive, orally administered small-molecule inhibitor of Aurora kinase A (AURKA). Fulvestrant is an estrogen receptor antagonist that works by blocking the use of estrogen by tumor cells or reducing the amount of estrogen made by the body. The combination was studied based on the hypothesis that alisertib might restore sensitivity to fulvestrant in endocrine-resistant breast cancer, as AURKA has been implicated in endocrine and CDK4/6 inhibitor resistance.