Drugs / H3B-6545
last change Oct 2025 re-read 9 days ago

H3B-6545

Small molecule targets ESR1 via inhibition

Developed for
estrogen-receptor positive breast cancer · breast adenocarcinoma · breast cancer · female breast carcinoma · Her2-receptor negative breast cancer
Investigated by
Eisai Inc.

Trials 3

2018201920202021202220232024202520262027
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 12 trials
Phase 1 NCT04568902 Sep 2020 → Oct 2025 breast cancer Eisai Inc. Completed No outcome recorded
Phase 1 NCT04288089 Apr 2020 → Sep 2022 overdue Her2-receptor negative breast cancer, estrogen-receptor positive breast cancer Eisai Inc. Active not recruiting No outcome recorded
Phase 1/21 trial
Phase 1/2 NCT03250676 Aug 2017 → Oct 2023 breast adenocarcinoma, estrogen-receptor positive breast cancer, female breast carcinoma Eisai Inc. Completed No outcome recorded

Evidence & citations 5 cited values

Every value below carries the sentence it was read from. 6 sources stand behind the page.

FieldValueCited text
Known as H3B-6545 ClinicalTrials.gov intervention name — accepted as the source's own label NCT04568902 ↗
2

NCT03250676 ↗

NCT04288089 ↗

Action Inhibit “H3B-6545 (a novel selective ER covalent antagonist that inactivates wild-type and mutant ERα)” PMID 40830892 ↗ Aug 2025
Modality Small molecule — CHEMBL5425361 ↗
Route Oral “Oral capsules by mouth once daily” NCT03250676 ↗
Target ESR1 “H3B-6545 is an ERα covalent antagonist that exhibits encouraging preclinical activity against CDK4/6i naïve and resistant ERαWT and ERαMUT tumors.” PMID 35642432 ↗ Jun 2022