Drug intelligence / Profile preview

1,4-dihydroxy quininib

Development stage
Preclinical
Lead developer
University College Dublin
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

1,4-dihydroxy quininib (also known as Q8) is a novel small-molecule antagonist of cysteinyl leukotriene receptor 1 (CysLT1) with potent anti-angiogenic, anti-inflammatory, and anti-cancer properties. Developed by researchers at University College Dublin and Trinity College Dublin, it is a structurally modified analogue of quininib. 1,4-dihydroxy quininib has demonstrated preclinical efficacy in several hard-to-treat cancers, including colorectal cancer, uveal melanoma (including metastatic uveal melanoma), glioblastoma multiforme, and non-small cell lung cancer (NSCLC). It acts by inhibiting CysLT1, which in turn modulates downstream signaling pathways such as NF-κB, calpain-2, and TIE-2/angiopoietin, and can induce ferroptosis in metastatic uveal melanoma cells.

Other names
(E)-2-(2-quinolin-2-yl-vinyl)-benzene-1,4-diol(E)-2-(2-quinolin-2-yl-vinyl)-benzene-1,4-diol HCl1,4-dihydroxyquininib
02

Targets

CYSLTR1 (Cysteinyl-leukotriene type 1 receptor)CYSLTR2 (Cysteinyl leukotriene receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)GPX4 (Glutathione peroxidase 4)VEGFR2 (Vascular endothelial growth factor receptor 2)

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