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TAK‐906, a Dopamine D2/D3 Receptor Antagonist with Minimal Brain Penetration for Gastrointestinal Disorders

Metoclopramide and domperidone are dopamine receptor antagonists utilized for the symptomatic treatment of gastrointestinal disorders such as gastroparesis. Metoclopramide is labeled only for acute use due to the potential for extrapyramidal side‐effects elicited through the blockade of central dopamine D2 receptors, while domperidone is a peripherally selective antagonist but therapy is limited due to the potential for cardiac arrhythmias. TAK‐906 is a dopamine receptor antagonist with minimal CNS penetration and minimal potential for cardiac QTc prolongation/arrhythmia.