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valbenazine
- Development stage
- Approved
- Lead developer
- Neurocrine Biosciences
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Valbenazine is a small molecule vesicular monoamine transporter 2 (VMAT2) inhibitor used to treat movement disorders, specifically tardive dyskinesia and chorea associated with Huntington's disease. It acts by selectively and reversibly inhibiting VMAT2 in the central nervous system, which reduces the uptake of monoamines—primarily dopamine—into synaptic vesicles for storage and release. This leads to decreased dopamine signaling in the brain, helping control involuntary movements. Valbenazine is a prodrug of (+)-α-dihydrotetrabenazine ([+]-α-HTBZ), an active metabolite with high affinity for VMAT2. The drug was developed as an improvement over tetrabenazine, offering better dosing convenience and safety profile.
- Brand names
- IngrezzaIngrezza Sprinkle
- Other names
- valbenazine tosylate
02
Targets
VMAT2 (Vesicular monoamine transporter 2)
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