MOA

Tardive dyskinesia (TD)—an often persistent movement disorder induced by prolonged DRBA exposure1

VMAT2 plays a key role in dopamine signaling.2

  • VMAT2 is a transporter protein found in presynaptic neurons of the CNS
  • VMAT2 packages monoamines (eg, dopamine) for release into the synaptic cleft

TD is associated with prolonged exposure to
DRBAs, including antipsychotics1

Prolonged exposure to DRBAs is believed to cause hypersensitivity in postsynaptic dopamine D2 receptors in one of the areas of the brain that controls motor function4

Vesicle
Vesicle
VMAT2
VMAT2
Dopamine
Dopamine
D2 Receptor
D2 receptor

CNS, central nervous system; DRBA, dopamine receptor blocking agent; VMAT2,
vesicular monoamine transporter 2.

INGREZZA is a selective VMAT2 inhibitor with once-daily dosing2,3

While the MOA of INGREZZA® (valbenazine) capsules is not fully understood, it is believed that it may be mediated through selective inhibition of VMAT2 in the presynaptic neurons, with no appreciable binding affinity to VMAT1, dopaminergic receptors, or serotonergic receptors.3

INGREZZA® (valbenazine) capsules is believed to provide reversible reductions of dopamine release into the synaptic cleft3

INGREZZA® (valbenazine) capsules is believed to reduce the amount of dopamine available to hypersensitive postsynaptic dopamine D2 receptors2,3

Vesicle
Vesicle
VMAT2
VMAT2
Dopamine
Dopamine
D2 Receptor
D2 receptor
Ingrezza
INGREZZA

VMAT1, vesicular monoamine transporter 1; VMAT2, vesicular monoamine transporter 2.

Watch the INGREZZA mechanism of action video

How INGREZZA®
(valbenazine) capsules is
thought to work

REFERENCES: 1. Hauser RA, Factor SA, Marder SR, et al. KINECT 3: a phase 3 randomized, double-blind, placebo-controlled trial of valbenazine for tardive dyskinesia. Am J Psychiatry. 2017;174(5):476-484. 2. Harriott ND, Williams JP, Smith EB, Bozigian HP, Grigoriadis DE. VMAT2 inhibitors and the path to INGREZZA (valbenazine). Prog Med Chem. 2018;57(1):87-111. 3. INGREZZA [package insert]. San Diego, CA: Neurocrine Biosciences, Inc; 2019. 4. Stahl SM. Antipsychotic agents. Stahl Online website. http://stahlonline.cambridge.org/essential_4th_chapter.jsf?page=chapter5_introduction.htm&name=Chapter%205&title=Conventional%20antipsychotics#c02598-5-1. Published 2013. Accessed August 22, 2018.