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CIDD-0166596

Development stage: Preclinical
Lead developer: Center for Innovative Drug Discovery
Modality: Small Molecules

Overview

CIDD-0166596 is a potent and selective small molecule agonist of the estrogen receptor beta (ERβ). Developed by the Center for Innovative Drug Discovery (CIDD) at the University of Texas at San Antonio (UTSA) and UT Health San Antonio, it is a next-generation indanone/tetralone-keto/hydroxyloxime derivative optimized for high blood-brain barrier permeability. In preclinical studies for glioblastoma (GBM), CIDD-0166596 demonstrated significant brain exposure (brain/plasma ratio of 3.12) and tumor-suppressive activity. It reduces the viability of glioblastoma stem cells and synergizes with temozolomide (TMZ) to increase DNA damage and prolong survival in orthotopic xenograft models.

Targets

ESR2 (ERβ)

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