Drug intelligence / Profile preview

gac0003a4

Development stage
Preclinical
Lead developer
University of Houston
Modality
Small Molecules
Administration
Unknown
01

Overview

GAC0003A4 is a **small molecule LXR inverse agonist and degrader** that targets and inhibits the transcriptional activity of Liver X Receptor beta (LXRβ), a nuclear receptor involved in the regulation of cholesterol transport, lipid and glucose metabolism, and inflammatory and immune processes. GAC0003A4 selectively disrupts LXRβ signaling, leading to reduced LXRβ protein levels in pancreatic ductal adenocarcinoma (PDAC) cells, thereby suppressing cancer cell proliferation and inducing cell death pathways such as apoptosis and necroptosis. This compound was developed for potential application in advanced pancreatic cancer and other difficult-to-treat malignancies, especially those with KRAS mutations, as an alternative to direct KRAS targeting[1][2][3][4][6].

Brand names
GAC0003A4GAC-0003A4GAC 0003A4
Other names
GAC0003A4GAC-0003A4GAC 0003A4EVT-1260261EVT1260261EVT 1260261
02

Targets

LXRB (Liver X receptor beta)

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