Valbenazine (NBI-98854) – VMAT2 Inhibitor

Valbenazine (NBI-98854)

To address the unmet medical needs of patients suffering from tardive dyskinesia (TD), Neurocrine is developing valbenazine (NBI-98854).  Valbenazine causes reversible reduction of dopamine release at the nerve terminal by selectively inhibiting the pre-synaptic human vesicular monoamine transporter type 2 (VMAT2).  In vitro, valbenazine is a highly selective inhibitor of human VMAT2 showing little or no affinity for VMAT1, other receptors (eg, dopamine D2 receptors), transporters, and ion channels.  We have designed this novel compound to provide sustained, plasma, and brain concentrations of the active drug to allow for once daily dosing.