Ladarixin (DF 2156A free base) is an orally active, non-competitive CXCR1/CXCR2 allosteric inhibitor that suppresses AKT, NF-κB, and angiogenesis, thereby slowing the progression of experimental human melanoma. It may be employed in research concerning COPD, asthma, and melanoma.

Ladarixin inhibits the migration of Homo sapiens polymorphonuclear leukocytes (PMNs) toward CXCL8, with a half-maximal inhibitory concentration (IC₅₀) of 0.7 nM [2].

Ladarixin (10 mg/kg) administered orally demonstrated rapid onset of action (inhibiting early neutrophil infiltration 2 hours after a single dose), broad-spectrum anti-inflammatory effects (suppressing Th2/Th17 inflammation, fibrosis, and oxidative stress), and reversal of steroid resistance across various pulmonary disease models, with particularly notable potential in severe asthma and COPD exacerbation models [1].
When different Homo sapiens-derived melanoma cell lines were inoculated into NCrNU-M nude mice, Ladarixin (15 mg/kg) administered via intraperitoneal injection once daily significantly inhibited the growth of WM164, UM001, and UM004 melanomas, though it showed weaker inhibitory effects on C8161 melanoma growth. Ladarixin treatment markedly increased apoptotic areas and leukocyte infiltration in tumor tissues, particularly elevating the proportion of M1-type macrophages [2].