NCIt definition : An orally available inhibitor of CXC chemokine receptor types 1 (CXCR1) and 2 (CXCR2),
with potential antineoplastic activity. Upon administration, reparixin allosterically
binds to CXCR1 and prevents CXCR1 activation by its ligand interleukin 8 (IL-8 or
CXCL8). This may cause cancer stem cell (CSC) apoptosis and may inhibit tumor cell
progression and metastasis. CXCR1, overexpressed on CSCs, plays a key role in CSC
survival and the ability of CSC to self-renew; it is also linked to tumor resistance
to chemotherapy. Inhibition of the IL-8/CXCR1 interaction also potentiates the cytotoxic
effect of chemotherapeutic agents. In addition, reparixin inhibits CXCR2 activation
and may reduce both neutrophil recruitment and vascular permeability during inflammation
or injury.;