NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

selective estrogen receptor covalent antagonist H3B-6545
An orally available, selective and covalent antagonist of estrogen receptor alpha (ERalpha; ERa; ESR1; nuclear receptor subfamily 3, group A, member 1; NR3A1), with potential antineoplastic activity. Upon oral administration, selective estrogen receptor covalent antagonist (SERCA) H3B-6545 selectively and covalently binds to a cysteine that is unique to ERalpha and is not present in other nuclear hormone receptors, thereby inhibiting the activity of ERalpha. This inhibits the growth and survival of ERalpha-expressing cancer cells. ERalpha, a nuclear hormone receptor, is often overexpressed and/or mutated in a variety of cancer cell types. It plays a key role in tumor cell proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

Synonym:SERCA H3B-6545
Code name:H3B 6545