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ACT-777991 is a highly potent, orally available small molecule antagonist of the C-X-C chemokine receptor 3 (CXCR3), developed by Idorsia Pharmaceuticals. It acts as an insurmountable and selective CXCR3 antagonist, blocking the migration of activated T cells to sites of inflammation by inhibiting the binding of its ligands (CXCL9, CXCL10, and CXCL11) to the receptor. This mechanism is relevant in autoimmune diseases where CXCR3-expressing T cells contribute to tissue damage. Preclinical studies have shown that ACT-777991 inhibits chemotaxis of CXCR3+ T cells and demonstrates efficacy in models of type 1 diabetes. The drug has advanced into Phase I clinical trials for type 1 diabetes mellitus and vitiligo.
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