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TRV120027 is an investigational peptide drug that acts as a β-arrestin–biased ligand at the angiotensin II type 1 receptor (AT1R). Unlike conventional angiotensin receptor blockers, which block both G-protein and β-arrestin signaling, TRV120027 selectively antagonizes G-protein-mediated coupling while engaging β-arrestin-mediated signaling. This unique mechanism allows it to inhibit angiotensin II–mediated vasoconstriction and simultaneously enhance cardiac contractility via β-arrestin pathways. Preclinical studies have shown that TRV120027 produces vasodilation, increases cardiac output, preserves renal function, and has a short half-life requiring parenteral administration. It has been evaluated in phase II clinical trials for acute heart failure (AHF) and kidney disease[1][2][3][4][5][6].
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