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Zamicastat is a peripherally selective dopamine beta-hydroxylase (DBH) inhibitor developed as an orally administered small molecule for the treatment of pulmonary arterial hypertension and heart failure. By inhibiting DBH, zamicastat decreases noradrenaline (norepinephrine) and increases dopamine levels in peripheral sympathetically innervated tissues, thereby reducing sympathetic tone—a mechanism considered beneficial in cardiovascular diseases characterized by sympathetic overactivity. It is structurally related to etamicastat but designed as an improved version. As of July 2022, zamicastat has reached phase II clinical trials for pulmonary arterial hypertension and completed phase I trials for heart failure; however, no recent development has been reported for heart failure[3][5][7][6].
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