Drug intelligence / Profile preview

BHPI

Development stage
Preclinical
Lead developer
University of Illinois, Urbana-Champaign
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

BHPI is a first-generation small molecule anticancer agent that induces immunogenic necrosis in estrogen receptor (ER)-positive cancer cells, including breast, ovarian, and endometrial cancers. Developed by researchers at the University of Illinois at Urbana-Champaign, BHPI functions by hyperactivating the anticipatory unfolded protein response (a-UPR). This hyperactivation leads to a massive, sustained increase in intracellular calcium levels and rapid depletion of ATP, ultimately resulting in necrotic cell death rather than apoptosis. The necrotic process is mediated by the Transient Receptor Potential Melastatin Member 4 (TRPM4) channel. BHPI served as the lead compound for the development of the more potent second-generation analog, ErSO.

Other names
3,3-bis(4-hydroxyphenyl)-7-methylindolin-2-one
02

Targets

ESR1 (ERα)

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