valbenazine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5227 1025504-45-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • valbenazine
  • valbenazine tosylate
  • ingrezza
  • NBI-98854
  • NBI 98854
  • valbenazine ditosylate
  • dysval
The mechanism of action of valbenazine in the treatment of tardive dyskinesia is unknown, 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.
  • Molecular weight: 418.58
  • Formula: C24H38N2O4
  • CLOGP: 3.77
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 74.02
  • ALOGS: -4.04
  • ROTB: 8

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.31 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.71 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 18 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 11, 2017 FDA NEUROCRINE BIOSCIENCES INC
March 28, 2022 PMDA Mitsubishi Tanabe Pharma Corporation

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Tardive dyskinesia 847.77 38.22 187 5107 7844 56278929
Somnolence 467.95 38.22 250 5044 163163 56123610
Drooling 382.67 38.22 84 5210 3410 56283363
Tremor 281.67 38.22 162 5132 120927 56165846
Parkinsonism 276.18 38.22 79 5215 9467 56277306
Sedation 222.17 38.22 93 5201 34761 56252012
Dyskinesia 186.55 38.22 78 5216 29030 56257743
Hospitalisation 139.24 38.22 87 5207 74913 56211860
Death 110.00 38.22 147 5147 341279 55945494
Therapeutic product effect decreased 92.94 38.22 96 5198 169356 56117417
Balance disorder 92.27 38.22 68 5226 76452 56210321
Adverse drug reaction 90.27 38.22 63 5231 65069 56221704
Akathisia 86.41 38.22 32 5262 8620 56278153
Restlessness 84.85 38.22 44 5250 26542 56260231
Therapeutic product effect incomplete 84.68 38.22 74 5220 105957 56180816
Drug ineffective 83.55 38.22 230 5064 918759 55368014
Fall 61.93 38.22 116 5178 357394 55929379
Urticaria 58.57 38.22 70 5224 144606 56142167
Anxiety 54.16 38.22 78 5216 193094 56093679
Feeling abnormal 53.01 38.22 64 5230 133538 56153235
Dizziness 51.85 38.22 111 5183 376029 55910744
Nightmare 48.42 38.22 26 5268 16800 56269973
Bradykinesia 44.98 38.22 17 5277 4837 56281936
Gait disturbance 44.37 38.22 65 5229 163256 56123517
Depression 40.93 38.22 66 5228 180051 56106722
Lethargy 39.19 38.22 35 5259 51406 56235367
Fatigue 38.69 38.22 161 5133 788391 55498382

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drooling 412.21 50.59 86 2650 3009 31691599
Tardive dyskinesia 336.11 50.59 81 2655 5478 31689130
Somnolence 274.08 50.59 144 2592 99301 31595307
Parkinsonism 171.91 50.59 51 2685 7585 31687023
Tremor 163.75 50.59 94 2642 76326 31618282
Sedation 144.00 50.59 56 2680 18909 31675699
Hospitalisation 100.38 50.59 59 2677 49748 31644860
Drug ineffective 81.04 50.59 131 2605 395442 31299166
Therapeutic product effect decreased 78.58 50.59 43 2693 31579 31663029
Dyskinesia 70.78 50.59 35 2701 20875 31673733
Anxiety 64.25 50.59 57 2679 90976 31603632
Adverse drug reaction 61.83 50.59 34 2702 25167 31669441
Death 59.88 50.59 109 2627 360460 31334148
Fall 58.85 50.59 76 2660 186013 31508595
Restlessness 53.16 50.59 30 2706 23331 31671277

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Tardive dyskinesia 687.99 37.07 158 5282 9771 70913233
Somnolence 442.35 37.07 247 5193 215359 70707645
Drooling 432.89 37.07 97 5343 5339 70917665
Tremor 293.14 37.07 169 5271 155455 70767549
Parkinsonism 230.06 37.07 73 5367 15252 70907752
Sedation 181.98 37.07 83 5357 46648 70876356
Dyskinesia 153.75 37.07 71 5369 41003 70882001
Death 146.72 37.07 187 5253 509874 70413130
Hospitalisation 145.26 37.07 86 5354 82482 70840522
Anxiety 102.59 37.07 104 5336 220226 70702778
Restlessness 95.93 37.07 52 5388 42076 70880928
Fall 85.92 37.07 135 5305 443961 70479043
Balance disorder 81.21 37.07 62 5378 90066 70832938
Therapeutic product effect decreased 72.90 37.07 71 5369 142947 70780057
Therapeutic product effect incomplete 67.71 37.07 63 5377 119819 70803185
Feeling abnormal 67.61 37.07 68 5372 142251 70780753
Dizziness 60.86 37.07 119 5321 464022 70458982
Fatigue 60.44 37.07 168 5272 824151 70098853
Urticaria 58.24 37.07 67 5373 162982 70760022
Lethargy 57.50 37.07 47 5393 75203 70847801
Drug ineffective 56.98 37.07 179 5261 939573 69983431
Akathisia 54.68 37.07 24 5416 12269 70910735
Adverse drug reaction 50.89 37.07 38 5402 53306 70869698
Depression 44.68 37.07 65 5375 198909 70724095
Gait disturbance 43.80 37.07 62 5378 185044 70737960
Salivary hypersecretion 41.11 37.07 20 5420 12905 70910099
Insomnia 38.88 37.07 64 5376 217742 70705262
Bradykinesia 37.80 37.07 16 5424 7486 70915518

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07XX13 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
OTHER NERVOUS SYSTEM DRUGS
Other nervous system drugs
FDA MoA N0000190855 Vesicular Monoamine Transporter 2 Inhibitors
FDA EPC N0000190856 Vesicular Monoamine Transporter 2 Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Tardive dyskinesia indication 102449007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.25 Basic
pKa2 7.56 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 8357697 Nov. 8, 2027 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 8357697 Nov. 8, 2027 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 8357697 Nov. 8, 2027 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10065952 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10844058 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10851103 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10851104 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10065952 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10844058 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10851103 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10851104 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10065952 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10844058 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10851103 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10851104 Oct. 28, 2036 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10857137 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10857148 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10874648 Oct. 10, 2037 METHOD OF ADMINISTERING VALBENAZINE WHILE AVOIDING CONCOMITANT USE OF A STRONG CYP3A4 INDUCER
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10874648 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10912771 Oct. 10, 2037 METHOD OF TREATING TARDIVE DYSKINESIA WHILE AVOIDING CONCOMITANT USE OF A STRONG CYP3A4 INDUCER
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10912771 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10952997 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10993941 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 11040029 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10857137 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10857148 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10874648 Oct. 10, 2037 METHOD OF ADMINISTERING VALBENAZINE WHILE AVOIDING CONCOMITANT USE OF A STRONG CYP3A4 INDUCER
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10874648 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10912771 Oct. 10, 2037 METHOD OF TREATING TARDIVE DYSKINESIA WHILE AVOIDING CONCOMITANT USE OF A STRONG CYP3A4 INDUCER
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10912771 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10952997 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10993941 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 11040029 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10857137 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10857148 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10874648 Oct. 10, 2037 METHOD OF ADMINISTERING VALBENAZINE WHILE AVOIDING CONCOMITANT USE OF A STRONG CYP3A4 INDUCER
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10874648 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10912771 Oct. 10, 2037 METHOD OF TREATING TARDIVE DYSKINESIA WHILE AVOIDING CONCOMITANT USE OF A STRONG CYP3A4 INDUCER
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10912771 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10952997 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10993941 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 11040029 Oct. 10, 2037 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 11026939 Sept. 18, 2038 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 11311532 Sept. 18, 2038 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 11026939 Sept. 18, 2038 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 11311532 Sept. 18, 2038 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 11026939 Sept. 18, 2038 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 11311532 Sept. 18, 2038 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 11026931 Aug. 14, 2039 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 11026931 Aug. 14, 2039 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 11026931 Aug. 14, 2039 TREATMENT OF TARDIVE DYSKINESIA
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL 10940141 Aug. 10, 2040 TREATMENT OF TARDIVE DYSKINESIA
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL 10940141 Aug. 10, 2040 TREATMENT OF TARDIVE DYSKINESIA
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL 10940141 Aug. 10, 2040 TREATMENT OF TARDIVE DYSKINESIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 40MG BASE INGREZZA NEUROCRINE N209241 April 11, 2017 RX CAPSULE ORAL April 11, 2022 NEW CHEMICAL ENTITY
EQ 60MG BASE INGREZZA NEUROCRINE N209241 April 23, 2021 RX CAPSULE ORAL April 11, 2022 NEW CHEMICAL ENTITY
EQ 80MG BASE INGREZZA NEUROCRINE N209241 Oct. 4, 2017 RX CAPSULE ORAL April 11, 2022 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Synaptic vesicular amine transporter Transporter INHIBITOR Ki 8.52 DRUG LABEL DRUG LABEL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.77 CHEMBL
Synaptic vesicular amine transporter Transporter INHIBITOR Ki 6.73 IUPHAR

External reference:

IDSource
54K37P50KH UNII
1639208-54-0 SECONDARY_CAS_RN
C4078701 UMLSCUI
CHEMBL2364639 ChEMBL_ID
24795069 PUBCHEM_CID
DB11915 DRUGBANK_ID
D10675 KEGG_DRUG
CHEMBL3707248 ChEMBL_ID
9744 INN_ID
8694 IUPHAR_LIGAND_ID
255701 MMSL
32624 MMSL
d08559 MMSL
017167 NDDF
017168 NDDF
733727001 SNOMEDCT_US
763512007 SNOMEDCT_US
4036639 VANDF
C000603978 MESH_SUPPLEMENTAL_RECORD_UI
14580381 PUBCHEM_CID
1918219 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-1060 CAPSULE 60 mg ORAL NDA 29 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-1060 CAPSULE 60 mg ORAL NDA 29 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-1080 CAPSULE 80 mg ORAL NDA 29 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-1080 CAPSULE 80 mg ORAL NDA 29 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-2040 CAPSULE 40 mg ORAL NDA 29 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-2040 CAPSULE 40 mg ORAL NDA 29 sections