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
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

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
Somnolence 479.52 35.01 250 4951 178435 63305386
Drooling 391.32 35.01 85 5116 3783 63480038
Tremor 292.00 35.01 163 5038 132076 63351745
Parkinsonism 275.46 35.01 78 5123 10361 63473460
Sedation 224.92 35.01 93 5108 38716 63445105
Dyskinesia 183.03 35.01 76 5125 31926 63451895
Hospitalisation 140.21 35.01 87 5114 84994 63398827
Death 115.36 35.01 147 5054 374234 63109587
Balance disorder 97.01 35.01 69 5132 84353 63399468
Therapeutic product effect decreased 93.51 35.01 96 5105 193091 63290730
Akathisia 88.99 35.01 32 5169 9114 63474707
Adverse drug reaction 86.64 35.01 63 5138 79651 63404170
Restlessness 86.33 35.01 44 5157 29409 63454412
Drug ineffective 85.01 35.01 230 4971 1044535 62439286
Therapeutic product effect incomplete 82.96 35.01 74 5127 124982 63358839
Fall 67.01 35.01 117 5084 392217 63091604
Urticaria 60.33 35.01 71 5130 165731 63318090
Anxiety 55.33 35.01 78 5123 217463 63266358
Feeling abnormal 54.72 35.01 64 5137 148328 63335493
Dizziness 52.20 35.01 111 5090 429814 63054007
Lethargy 51.33 35.01 40 5161 55967 63427854
Nightmare 48.57 35.01 26 5175 19168 63464653
Tardive dyskinesia 47.88 35.01 20 5181 8482 63475339
Bradykinesia 46.16 35.01 17 5184 5171 63478650
Gait disturbance 45.53 35.01 65 5136 183113 63300708
Depression 43.47 35.01 66 5135 196426 63287395
Fatigue 40.41 35.01 161 5040 887867 62595954
Insomnia 36.34 35.01 64 5137 215188 63268633

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 414.64 45.50 86 2599 3296 34950950
Somnolence 274.92 45.50 144 2541 110972 34843274
Parkinsonism 170.18 45.50 50 2635 8088 34946158
Tremor 164.48 45.50 93 2592 82494 34871752
Sedation 151.97 45.50 58 2627 20948 34933298
Hospitalisation 99.49 45.50 59 2626 56843 34897403
Therapeutic product effect decreased 79.50 45.50 43 2642 34700 34919546
Drug ineffective 78.43 45.50 131 2554 456620 34497626
Fall 67.23 45.50 80 2605 202805 34751441
Anxiety 65.67 45.50 57 2628 99371 34854875
Dyskinesia 63.41 45.50 32 2653 22381 34931865
Death 61.31 45.50 109 2576 397940 34556306
Adverse drug reaction 60.71 45.50 34 2651 29308 34924938
Restlessness 53.99 45.50 30 2655 25452 34928794
Dizziness 50.21 45.50 72 2613 218449 34735797
Therapeutic product effect incomplete 46.03 45.50 35 2650 50506 34903740

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
Somnolence 447.82 36.45 247 5143 238734 79500264
Drooling 442.15 36.45 98 5292 5836 79733162
Tremor 301.80 36.45 170 5220 169913 79569085
Parkinsonism 233.47 36.45 73 5317 16511 79722487
Sedation 190.08 36.45 85 5305 51810 79687188
Death 149.94 36.45 187 5203 566327 79172671
Hospitalisation 147.43 36.45 87 5303 94149 79644849
Dyskinesia 143.93 36.45 67 5323 44706 79694292
Anxiety 103.12 36.45 104 5286 248408 79490590
Restlessness 97.29 36.45 52 5338 46440 79692558
Fall 96.53 36.45 140 5250 487489 79251509
Balance disorder 85.33 36.45 63 5327 98794 79640204
Lethargy 72.83 36.45 53 5337 81239 79657759
Therapeutic product effect decreased 72.32 36.45 71 5319 163792 79575206
Feeling abnormal 68.43 36.45 68 5322 159131 79579867
Therapeutic product effect incomplete 65.54 36.45 63 5327 141582 79597416
Fatigue 61.09 36.45 168 5222 929559 78809439
Dizziness 60.90 36.45 119 5271 526322 79212676
Urticaria 59.89 36.45 68 5322 185133 79553865
Akathisia 55.85 36.45 24 5366 13235 79725763
Drug ineffective 55.53 36.45 179 5211 1080734 78658264
Adverse drug reaction 47.77 36.45 38 5352 66354 79672644
Depression 46.72 36.45 65 5325 216725 79522273
Gait disturbance 44.39 36.45 62 5328 207444 79531554
Salivary hypersecretion 41.70 36.45 20 5370 14204 79724794
Insomnia 40.63 36.45 65 5325 245105 79493893
Bradykinesia 38.68 36.45 16 5374 8027 79730971

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)

None

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
4036639 VANDF
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
14580381 PUBCHEM_CID
1918219 RXNORM
C000603978 MESH_SUPPLEMENTAL_RECORD_UI

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