Novel Class of Anti-estrogen Drugs for the Treatment of Breast Cancer

Many estrogen receptor α (ERα)-positive breast cancers often develop resistance to endocrine therapy due to mutations in ERs. These mutations are associated with shorter patient survival and, therefore, there is a need for novel anti-estrogen therapy against these mutant ERs. A team of scientists from the University of Illinois at Urbana-Champaign, led by Dr. John Katzenellenbogen, have developed a novel class of anti-estrogen compounds with the potential to act as breast cancer therapeutics. They have shown that the novel compounds have potent anti-proliferation effects and result in downregulation of ERα. Importantly, these compounds demonstrate enhanced bioavailability and oral potency as compared to currently prescribed therapeutics. These novel compounds, due to their potency, have the potential for low-dose administration, which minimizes deleterious side effects. Studies in female mouse models have shown suppressed tumor volumes, reduced breast cancer metastases and prolonged survival.