Alpelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potent antitumor activity. It works by selectively inhibiting class I PI3K p110? [A179203], which is the catalytic subunit of PI3K, a lipid kinase that plays a role in various biological proce…

Hormone receptor (HR) positive, especially estrogen receptor-positive, HER2-negative breast cancer is the most common subtype of metastatic breast cancer, resulting in more than 400,000 deaths annually. Although endocrine-based therapy is the first line of tr…

Elacestrant is a non-steroidal small molecule and an estrogen receptor (ER) antagonist.[A256838,L44918] In January 2023, it was approved by the FDA for the treatment of ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer.[L44918,L449…

Fulvestrant is a drug treatment of hormone receptor (HR)-positive metastatic breast cancer in post-menopausal women with disease progression following anti-estrogen therapy. It is an estrogen receptor antagonist with no agonist effects, which works both by do…

Giredestrant is under investigation in clinical trial NCT06065748 (A Study to Evaluate Efficacy and Safety of Giredestrant Compared With Fulvestrant (Plus a CDK4/6 Inhibitor), in Participants With Er-positive, Her2-negative Advanced Breast Cancer Resistant to…

Lerociclib is under investigation in clinical trial NCT02983071 (G1T38, a CDK 4/6 Inhibitor, in Combination With Fulvestrant in Hormone Receptor-positive, Her2-negative Locally Advanced or Metastatic Breast Cancer).

Luvixasertib is under investigation in clinical trial NCT05251714 (CFI-402257, a Potent and Selective TTK Inhibitor, in Solid Tumors and With Fulvestrant in Breast Cancer).