H3B-6545

Cancer Research | Apr. 15, 2019

Estrogen Receptor Covalent Antagonists: The Best Is Yet to Come

The development of tamoxifen and subsequent estrogen receptor alpha (ERα) antagonists represents a tremendous therapeutic breakthrough in the treatment of… Read More

Cancer Chemotherapy and Pharmacology | Jan. 2019

Nonclinical Pharmacokinetics and in Vitro Metabolism of H3B-6545, a Novel Selective ERα Covalent Antagonist (SERCA)

Purpose: H3B-6545, a novel selective estrogen receptor (ER)α covalent antagonist (SERCA) which inactivates both wild-type and mutant ERα, is in… Read More

Cancer Discovery | Sept. 2018

Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERα WT and ERα MUT Breast Cancer

Mutations in estrogen receptor alpha (ERα) that confer resistance to existing classes of endocrine therapies are detected in up to… Read More