Valbenazine
Ingrezza
VMAT2 Inhibitor
Valbenazine is a highly selective inhibitor of vesicular monoamine transporter 2 (VMAT2). By inhibiting VMAT2, it decreases the packaging of monoamines (primarily dopamine) into synaptic vesicles, reducing dopaminergic transmission in the basal ganglia and treating the hyperkinetic movements of tardive dyskinesia. Unlike tetrabenazine, valbenazine has minimal affinity for D2, 5-HT2, and sigma receptors.
Compare Valbenazine →FDA-Approved Indications
- Tardive dyskinesia
What Sets This Drug Apart
- First FDA-approved treatment for tardive dyskinesia (April 2017) — filled a major unmet need with no prior approved therapies
- Highly selective VMAT2 inhibitor — minimal D2/5-HT2/sigma binding distinguishes it from tetrabenazine with potentially fewer psychiatric side effects
- Once-daily dosing — advantage over deutetrabenazine (BID) and tetrabenazine (TID)
- Somnolence in ~11% — the most common treatment-limiting side effect
- Brand-only (Ingrezza) — high cost limits access for some patients