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RCT001 is a small molecule inverse agonist of the C-X-C motif chemokine receptor 2 (CXCR2) developed by the French biotechnology company Rocartab. It is primarily being investigated for the treatment of clear cell renal cell carcinoma (ccRCC). RCT001 functions by inhibiting CXCR2-mediated signaling, which leads to the suppression of tumor cell proliferation and angiogenesis. Additionally, it acts as an immunomodulator within the tumor microenvironment by redirecting M2-like (pro-tumor) macrophages toward an M1-like (anti-tumor) phenotype and reducing the infiltration of tumor-associated neutrophils. Preclinical studies have demonstrated that RCT001 can potentiate the efficacy of immune checkpoint inhibitors, such as anti-PD-1 and anti-CTLA-4 therapies, by increasing the activation of natural killer (NK) cells and dendritic cells while reducing immune-tolerant lymphocytes.
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