Drug intelligence / Profile preview

LXY18

Development stage
Preclinical
Lead developer
Anticancer Bioscience
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

LXY18 is a potent, orally available small molecule based on a 4-phenoxy-quinoline scaffold that acts as an Aurora kinase B (AURKB) relocation blocker. Unlike traditional AURKB inhibitors that target the enzyme's catalytic activity, LXY18 prevents the proper localization of AURKB during late mitosis, thereby disrupting cytokinesis and inducing prolonged mitotic arrest in cancer cells. This leads to apoptosis selectively in malignant cells while sparing non-transformed cells. The compound demonstrates broad-spectrum antimitotic and apoptosis-inducing activity at low nanomolar concentrations, with effective tissue distribution including blood-brain barrier penetration and tumor accumulation. Preclinical studies show marked suppression of tumor growth in vivo. Its novel mechanism may help overcome resistance mechanisms associated with direct kinase inhibition and offers promise as a new anticancer therapeutic candidate[1][2][3][4][6].

02

Targets

AURKB (Aurora kinase B)

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