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Cintirorgon is an orally bioavailable, small molecule agonist of the retinoic acid-related orphan receptor gamma (RORγ). It selectively binds to RORγ, a nuclear receptor transcription factor involved in the differentiation and function of type 17 T-cells (Th17 and Tc17). By activating RORγ, cintirorgon enhances the proliferation and survival of these T-cells, increases expression of co-stimulatory molecules, decreases expression of co-inhibitory molecules on T-cells, boosts cytokine and chemokine production by T-cells, reduces regulatory T-cell proliferation, and counteracts tumor-induced immunosuppression. This results in a heightened T-cell-mediated immune response against cancer cells with potential antineoplastic effects. Cintirorgon is being developed primarily for solid tumors[1][2][6].
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