XY003

XY003 (also known as HXG-001) is a first-in-class, orally bioavailable small molecule G-quadruplex (G4) stabilizer developed by Hexin Biotech. It targets G4 DNA structures, which are four-stranded DNA motifs often found in regulatory regions of the genome. By stabilizing these structures, XY003 induces DNA damage at G4-rich loci, leading to synthetic lethality in cancer cells with deficiencies in DNA damage repair pathways, specifically homologous recombination deficiency (HRD) or non-homologous end joining (NHEJ) defects. Preclinical data indicate that XY003 can cross the blood-brain barrier, showing efficacy in primary and metastatic brain tumor models. It is currently being evaluated in Phase I clinical trials for advanced solid tumors, including pancreatic cancer and triple-negative breast cancer.