Drug intelligence / Profile preview

XK469

Development stage
Phase 1
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous
01

Overview

XK469 (NSC 697887) is a synthetic quinoxaline phenoxypropionic acid derivative developed as an antineoplastic agent. It is structurally distinguished by its ability to selectively target and inhibit **DNA topoisomerase II beta (TOP2B)**, whereas most traditional topoisomerase inhibitors target both alpha and beta isoforms or are selective for the alpha isoform. The drug's mechanism involves inducing G2/M phase cell cycle arrest, inhibiting cytokinesis, and promoting polyploidy, eventually leading to cell death through mechanisms such as autophagy or senescence rather than traditional apoptosis in certain cell types. XK469 has been investigated in Phase I clinical trials for the treatment of advanced solid tumors, neuroblastoma, and various refractory hematologic malignancies. Its pharmacokinetic profile is characterized by a long half-life and elimination primarily via the enzyme aldehyde oxidase 1 (AOX1).

Other names
2-{4-[(7-chloro-2-quinoxalinyl)oxy]phenoxy}propionic acidR(+)-2-[4-(7-chloroquinoxalin-2-yloxy)phenoxy]propionic acid
02

Targets

TOP2B (DNA topoisomerase II beta)TOP2A (DNA topoisomerase II)

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