Valbenazine

Valbenazine is an inhibitor of vesicular monoamine transporter 2 (VMAT2). VMAT2 plays an important role in the packaging of monoamines into presynaptic vesicles. Valbenazine shows Ki values of 110 and 150 nM in rat striatum homogenates and human platelets, respectively. It is selective for VMAT2 over serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2B and dopamine D1 and D2 receptors. It is used for the treatment of tardive dyskinesia.