Burixafor (hydrobromide)

Burixafor (TG-0054) hydrobromide is a selective, orally active CXCR4 antagonist that effectively blocks the interaction between CXCR4 and its ligand, stromal cell-derived factor SDF-1. Burixafor hydrobromide interferes with the SDF-1/CXCR4 signaling pathway, prompting the release of bone marrow stem cells into the peripheral circulation, exerting immunomodulatory and anti-inflammatory activities. Burixafor hydrobromide can be used in the study of cancer, Intraocular neovascular diseases (such as choroidal neovascularization), myocardial infarction and other diseases, with the potential to mobilize stem cells, improve cardiac function and reduce inflammatory responses^[1][2][3]. In Vitro:Burixafor hydrobromide (1 μM; 2 h) inhibits microenvironment-induced phosphorylation of Pyk2 (Y579/Y580) and FAK (Y925) in human glioblastoma (GBM) cell lines and suppresses cell migration and invasion^[1].
In Vivo:Burixafor hydrobromide (2.85 mg/kg; intravenous injection; 2 times) mobilizes CD34⁺CXCR4⁺, CD133⁺CXCR4⁺, and CD271⁺CXCR4⁺ cells into the peripheral circulation in the Taiwan Blue Island miniature pig myocardial infarction model, reduces the levels of TNF-α, IL-1β, and IL-6 in the myocardium and plasma, and improves left ventricular ejection fraction (LVEF)^[2].
Burixafor hydrobromide (1.5 mg/50 μL; intravitreal injection; single dose) achieves sustained delivery to the retina and choroid via polylactic acid (PLA) microparticles in the New Zealand white rabbit choroidal neovascular disease model, exerting anti-angiogenic activity^[3].