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XT-0528 is an oral small molecule inverse agonist of the retinoic acid receptor-related orphan receptor gamma T (RORγT), developed by Xenthera for the treatment of advanced and metastatic solid tumors. RORγT is a ligand-dependent transcription factor that regulates pro-inflammatory genes and drives the differentiation of T helper cells into Th17 cells. By inhibiting RORγT, XT-0528 reduces the production of the key inflammatory cytokine IL-17 and alters inflammatory signaling within the tumor microenvironment. This modulation may enhance the effectiveness of immunotherapy while potentially lowering toxicity. The drug has demonstrated a favorable safety profile in early clinical trials and is currently undergoing Phase 1 dose-escalation studies to determine the recommended Phase 2 dose for patients with various solid tumor malignancies.
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