Valbenazine

The mechanism of action of valbenazine for the treatment of tardive dyskinesia and chorea in patients with Huntington’s disease is unclear, but is thought to be mediated through the reversible inhibition of vesicular monoamine transporter 2 (VMAT2), a transporter that regulates monoamine uptake from the cytoplasm to the synaptic vesicle for storage and release.

• INGREZZA and INGREZZA SPRINKLE are indicated for the treatment of adults with: - tardive dyskinesia [see Clinical Studies ( 14.1 )] . - chorea associated with Huntington’s disease [see Clinical Studies ( 14.2 )] .

• INGREZZA and INGREZZA SPRINKLE are contraindicated in patients with a history of hypersensitivity to valbenazine or any components of INGREZZA or INGREZZA SPRINKLE. Rash, urticaria, and reactions consistent with angioedema (e.g., swelling of the face, lips, and mouth) have been reported with use of INGREZZA [see Warnings and Precautions ( 5.2 ) and Adverse Reactions ( 6.2 )].contraindicated

Tardive dyskinesia: The initial dosage is 40 mg once daily. After one week, increase the dose to the recommended dosage of 80 mg once daily. ( 2.1 ) Chorea associated with Huntington’s disease: The initial dosage is 40 mg once daily. Increase the dose in 20 mg increments every two weeks to the recommended dosage of 80 mg once daily. ( 2.1 ) 40 mg or 60 mg once daily may be considered depending on response and tolerability. ( 2.1 ) Can be taken with or without food. ( 2.2 ) INGREZZA SPRINKLE may be opened and sprinkled over soft food (do not use milk or drinking water). INGREZZA SPRINKLE may be swallowed whole with water. Do not crush or chew. ( 2.2 ) The recommended dosage for patients with moderate or severe hepatic impairment is 40 mg once daily. ( 2.3 ) The recommended dosage for known CYP2D6 poor metabolizers is 40 mg once daily. ( 2.4 ) 2.1 Recommended Dosage Tardive Dyskinesia The initial dosage for INGREZZA and INGREZZA SPRINKLE is 40 mg once daily. After one week, increase the dose to the recommended dosage of 80 mg once daily. A dosage of 40 mg or 60 mg once daily may be considered depending on response and tolerability. Chorea Associated with Huntington ’s Disease The initial dosage for INGREZZA and INGREZZA SPRINKLE is 40 mg once daily. Increase the dose in 20 mg increments every two weeks to the recommended dosage of 80 mg once daily. A dosage of 40 mg or 60 mg once daily may be considered depending on response and tolerability.

Depression and suicidal ideation and behavior in patients with Huntington’s disease. ( 5.1 ) Hypersensitivity, including angioedema may occur. Discontinue if this occurs. ( 5.2 ) Somnolence/sedation: May impair patient’s ability to drive or operate hazardous machinery. ( 5.3 ) QT Prolongation: May cause an increase in QT interval. Avoid use in patients with congenital long QT syndrome or with arrhythmias associated with a prolonged QT interval. ( 5.4 ) Neuroleptic Malignant Syndrome (NMS): Discontinue if this occurs. ( 5.5 ) Parkinsonism: Cases of parkinson-like symptoms, some of which were severe, have been reported in the postmarketing period. Reduce the dose or discontinue INGREZZA or INGREZZA SPRINKLE treatment in patients who develop clinically significant parkinson-like signs or symptoms. ( 5.6 ) 5.1 Depression and Suicidal Ideation and Behavior in Patients with Huntington’s Disease Patients with Huntington’s disease are at increased risk for depression, and suicidal ideation or behaviors. VMAT2 inhibitors, including INGREZZA and INGREZZA SPRINKLE, can increase the risk for suicidal ideation and behaviors in patients with Huntington’s disease. In a 14-week, double-blind, placebo-controlled trial [see Clinical Studies ( 14.2 )] , depression or depressed mood was reported in 4.7% of patients taking INGREZZA compared to 1.6% of patients who received placebo, and no patients taking INGREZZA reported suicidal ideation or behavior compared to 1 patient (1.6%) who received placebo.

The following clinically significant adverse reactions are discussed in more detail in other sections of the labeling: Depression and Suicidal Ideation and Behavior in Patients with Huntington’s Disease [see Boxed Warning and Warnings and Precautions ( 5.1 )] Hypersensitivity Reactions [see Contraindications ( 4 ) and Warnings and Precautions ( 5.2 ) ] Somnolence and Sedation [see Warnings and Precautions ( 5.3 )] QT Prolongation [see Warnings and Precautions ( 5.4 )] Neuroleptic Malignant Syndrome (NMS) [see Warnings and Precautions ( 5.5 )] Parkinsonism [see Warnings and Precautions ( 5.6 )] Most common adverse reaction (≥5% and twice the rate of placebo): - Tardive dyskinesia: somnolence. ( 6.1 ) - Chorea associated with Huntington’s disease: somnolence/lethargy/sedation, urticaria, rash, insomnia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Neurocrine Biosciences, Inc. at 877-641-3461 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of INGREZZA SPRINKLE has been established from adequate and well-controlled studies of INGREZZA [see Clinical Studies ( 14 )] . Below is a display of the adverse reactions of INGREZZA in these adequate and well-controlled studies.

Pregnancy: May cause fetal harm. ( 8.1 ) Lactation: Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary The limited available data on INGREZZA or INGREZZA SPRINKLE use in pregnant women are insufficient to inform a drug-associated risk. In animal reproductive studies, no malformations were observed when valbenazine was administered orally to rats and rabbits during the period of organogenesis at doses up to 1.8 or 24 times, respectively, the maximum recommended human dose (MRHD) of 80 mg/day based on mg/m 2 body surface area. However, administration of valbenazine to pregnant rats during organogenesis through lactation produced an increase in the number of stillborn pups and postnatal pup mortalities at doses <1 times the MRHD based on mg/m 2 [see Data ]. Advise a pregnant woman of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. The background risk of major birth defects and miscarriage in the U.S. general population is 2 to 4% and 15 to 20% of clinically recognized pregnancies, respectively.

Metabolism

Valbenazine and its active metabolite ([+]-α-HTBZ) demonstrate approximate proportional increases for the area under the plasma concentration versus time curve (AUC) and maximum plasma concentration (C max ) after single oral doses from 40 mg to 300 mg (i.e., 50% to 375% of the recommended treatment dose). Absorption INGREZZA Following oral administration of INGREZZA, the time to reach maximum valbenazine plasma concentration (t max ) ranges from 0.5 to 1.0 hours.

Human Experience The pre-marketing clinical trials involving INGREZZA in approximately 850 subjects do not provide information regarding symptoms with overdose. Management of Overdosage No specific antidotes for INGREZZA or INGREZZA SPRINKLE are known. In managing overdose, provide supportive care, including close medical supervision and monitoring, and consider the possibility of multiple drug involvement. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.

• Apr 11, 2017NDANDA209241Neurocrine
• Apr 30, 2024NDANDA218390Neurocrine

1. 1Drug Ineffective2,73711%
2. 2Somnolence2,4309.9%
3. 3Fatigue1,6566.7%
4. 4Tremor1,5596.3%
5. 5Tardive Dyskinesia1,4966.1%
6. 6Fall1,1174.5%
7. 7Dizziness9423.8%
8. 8Death9213.7%
9. 9Drooling8893.6%
10. 10Therapeutic Product Effect Decreased8603.5%
11. 11Dyskinesia8443.4%
12. 12Off Label Use6762.7%
13. 13Anxiety6662.7%
14. 14Hospitalisation6572.7%
15. 15Nausea6192.5%

The 10 most recently updated of 33 ClinicalTrials.gov registrations naming Valbenazine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Evaluate the Effectiveness of Valbenazine in Adult Participants With Tardive Dyskinesia (TD) Who Remain Symptomatic While Receiving or After Stopping a Vesicular Monoamine Transporter 2 (VMAT2) Inhibitor
  Recruiting · Phase 4 · Interventional · 50 enrolled · Neurocrine Biosciences
  NCT07105111updated 2026-06-11
• Valbenazine in Obsessive Compulsive Disorder
  Not yet recruiting · Phase 2 · Interventional · 30 enrolled · University of Chicago
  NCT07111988updated 2026-06-10
• Safety and Effectiveness of Valbenazine as Adjunct Therapy to Botulinum Toxin Injections in Cervical Dystonia
  Recruiting · Phase 2 · Interventional · 20 enrolled · Virginia Commonwealth University
  NCT06771323updated 2026-06-04
• Study to Assess the Efficacy, Safety, and Tolerability of Valbenazine for the Treatment of Dyskinesia Due to Cerebral Palsy
  Completed · Phase 3 · Interventional · 86 enrolled · Neurocrine Biosciences
  NCT05206513updated 2026-04-29
• Long-term Study to Evaluate Safety and Tolerability of Valbenazine in Participants With Chorea Associated With Huntington Disease in Canada
  Enrolling by invitation · Phase 3 · Interventional · 7 enrolled · Neurocrine Biosciences
  NCT06312189updated 2026-04-09
• Journey Study: Evaluate the Efficacy, Safety, and Tolerability of Valbenazine as Adjunctive Treatment for Schizophrenia
  Completed · Phase 3 · Interventional · 442 enrolled · Neurocrine Biosciences
  NCT05110157updated 2026-02-10
• Efficacy of Valbenazine for the Treatment of Trichotillomania in Adults
  Recruiting · Phase 2 · Interventional · 20 enrolled · Yale University
  NCT05207085updated 2026-02-03
• Study of the Effectiveness of Valbenazine on Patient- and Clinician-Reported Outcomes in Participants With Tardive Dyskinesia
  Completed · Phase 4 · Interventional · 59 enrolled · Neurocrine Biosciences
  NCT05859698updated 2026-01-16
• Reduction of Demoralization in Patients With Tardive Dyskinesia After Treatment With Valbenazine
  Withdrawn · Phase 1 · Interventional · 0 enrolled · Yale University
  NCT05053321updated 2025-07-11
• Open-Label Rollover Study for Continuing Valbenazine Administration for the Treatment of Chorea Associated With Huntington Disease
  Active not recruiting · Phase 3 · Interventional · 154 enrolled · Neurocrine Biosciences
  NCT04400331updated 2024-12-24

CPIC-curated drug–gene pairs for Valbenazine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC B/C (provisional)FDA label: Actionable PGx

Frequently asked questions

How does Valbenazine work?

The mechanism of action of valbenazine for the treatment of tardive dyskinesia and chorea in patients with Huntington’s disease is unclear, but is thought to be mediated through the reversible inhibition of vesicular monoamine transporter 2 (VMAT2), a transporter that regulates monoamine uptake from the cytoplasm to the synaptic vesicle for storage and release.

What is Valbenazine used for?

According to FDA labeling, Valbenazine carries indications including: INGREZZA and INGREZZA SPRINKLE are indicated for the treatment of adults with: - tardive dyskinesia [see Clinical Studies ( 14.1 )] . - chorea associated with Huntington’s disease [see Clinical Studies ( 14.2 )] .. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Valbenazine?

Valbenazine is classified as Other nervous system drugs, Vesicular Monoamine Transporter 2 Inhibitor, Vesicular Monoamine Transporter 2 Inhibitors, Decreased Dopamine Activity, Decreased Histamine Activity, Decreased Norepinephrine Activity, Decreased Serotonin Activity.

What are the brand names for Valbenazine?

Valbenazine is marketed under brand names including Ingrezza.

What are the contraindications for Valbenazine?

Valbenazine labeling lists contraindications including: INGREZZA and INGREZZA SPRINKLE are contraindicated in patients with a history of hypersensitivity to valbenazine or any components of INGREZZA or INGREZZA SPRINKLE. Rash, urticaria, and reactions consistent with angioedema (e.g., swelling of the face, lips, and mouth) have been reported with use of INGREZZA [see Warnings and Precautions ( 5.2 ) and Adverse Reactions ( 6.2 )].. Always consult the full prescribing information and a clinician.