H3B-6545

selective estrogen receptor (ER)alpha covalent antagonist

Also Known As:

((2E)-N,N-dimethyl-4-((2-((5-((1Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide) hydrochloride salt

Networked: 3 relevant articles (1 outcomes, 1 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Pyrazoles: 61
      - Indazoles: 179
        H3B-6545: 3
  - Pyridines: 88
    - H3B-6545: 3
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Indazoles: 179
      - H3B-6545: 3

Experts

1.	Korpal, Manav: 2 articles (01/2022 - 01/2019)
2.	Prajapati, Sudeep: 2 articles (01/2022 - 01/2019)
3.	Zheng, Guo Zhu: 2 articles (01/2022 - 01/2019)
4.	Aithal, Kiran B: 1 article (01/2022)
5.	Albacker, Lee A: 1 article (01/2022)
6.	Banka, Deepti: 1 article (01/2022)
7.	Bolduc, David M: 1 article (01/2022)
8.	Furman, Craig: 1 article (01/2022)
9.	Hao, Ming-Hong: 1 article (01/2022)
10.	Irwin, Sean: 1 article (01/2022)

Related Diseases

1.	Neoplasms (Cancer) 02/01/2020 - "H3B-6545 is a selective ERα covalent antagonist, which has been demonstrated to be effective in anti-tumor. " 01/01/2022 - "H3B-6545 is an ERα covalent antagonist that exhibits encouraging preclinical activity against CDK4/6i naïve and resistant ERαWT and ERαMUT tumors."
2.	Breast Neoplasms (Breast Cancer) 01/01/2022 - "In summary, the compelling preclinical activity of H3B-6545 supports its further development for the potential treatment of endocrine therapy-resistant ERα+ breast cancer harboring wild-type or mutant ESR1, as demonstrated by the ongoing clinical trials (NCT03250676, NCT04568902, NCT04288089). " 01/01/2022 - "Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer." 01/01/2019 - "H3B-6545, a novel selective estrogen receptor (ER)α covalent antagonist (SERCA) which inactivates both wild-type and mutant ERα, is in clinical development for the treatment of metastatic breast cancer. "

Related Drugs and Biologics

1.	Estrogen Receptors

Related Therapies and Procedures

1.	Therapeutics