Reparixin is a CXC chemokine receptor type 1 (CXCR1) and type 2 (CXCR2) inhibitor. This compound has potential antineoplastic activity. It can be administered orally, binds to CXCR1 (overexpressed on cancer stem cells) and prevents its activation by its ligand interleukin 8. This might result in the death of cancer cells and inhibition of cell progression and metastasis. Reparixin also inhibits CXCR2 activation, possibly reducing both neutrophil recruitment and vascular permeability during inflammation or injury. A phase II clinical trial evaluating the effects of orally administered reparixin on cancer stem cells in the primary tumor and the tumoral microenvironment in an early breast cancer population was terminated. Reparixin has also been suggested as a novel potential therapeutic strategy for aggressive forms of thyroid cancer, based on results of a xenotransplantation study in mice.