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
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

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 470.52 38.72 250 4721 154735 50445418
Drooling 370.67 38.72 82 4889 3302 50596851
Tremor 261.81 38.72 154 4817 114749 50485404
Parkinsonism 256.30 38.72 74 4897 8773 50591380
Sedation 229.98 38.72 93 4878 30517 50569636
Dyskinesia 166.65 38.72 72 4899 27789 50572364
Hospitalisation 143.72 38.72 87 4884 67850 50532303
Death 107.53 38.72 145 4826 325234 50274919
Therapeutic product effect decreased 107.35 38.72 96 4875 135954 50464199
Adverse drug reaction 94.79 38.72 62 4909 55160 50544993
Balance disorder 92.27 38.72 67 4904 70523 50529630
Therapeutic product effect incomplete 91.41 38.72 74 4897 91441 50508712
Drug ineffective 90.01 38.72 226 4745 819107 49781046
Restlessness 85.32 38.72 44 4927 25129 50575024
Akathisia 79.31 38.72 30 4941 8199 50591954
Urticaria 62.39 38.72 70 4901 129491 50470662
Fall 61.24 38.72 114 4857 334818 50265335
Anxiety 56.63 38.72 78 4893 177528 50422625
Dizziness 52.50 38.72 109 4862 346260 50253893
Feeling abnormal 50.73 38.72 62 4909 125430 50474723
Bradykinesia 47.70 38.72 17 4954 3926 50596227
Gait disturbance 44.97 38.72 64 4907 149941 50450212
Fatigue 44.60 38.72 161 4810 707440 49892713
Depression 41.60 38.72 65 4906 165358 50434795
Nightmare 40.22 38.72 23 4948 16063 50584090
Lethargy 39.08 38.72 35 4936 49397 50550756

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 411.92 48.12 86 2540 2935 29568966
Somnolence 269.43 48.12 141 2485 93814 29478087
Parkinsonism 168.54 48.12 50 2576 7228 29564673
Tremor 159.32 48.12 92 2534 73446 29498455
Sedation 147.16 48.12 56 2570 17349 29554552
Hospitalisation 100.55 48.12 58 2568 45930 29525971
Drug ineffective 86.78 48.12 131 2495 363039 29208862
Therapeutic product effect decreased 80.32 48.12 43 2583 29408 29542493
Adverse drug reaction 62.47 48.12 34 2592 23986 29547915
Anxiety 62.01 48.12 55 2571 85310 29486591
Death 61.85 48.12 109 2517 341975 29229926
Fall 58.54 48.12 75 2551 177103 29394798
Dyskinesia 56.65 48.12 30 2596 20031 29551870
Restlessness 53.87 48.12 30 2596 22115 29549786
Dizziness 50.03 48.12 72 2554 189612 29382289
Therapeutic product effect incomplete 49.37 48.12 35 2591 39270 29532631

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 439.84 35.97 244 4871 203401 64290216
Drooling 420.92 35.97 95 5020 5224 64488393
Tremor 271.67 35.97 160 4955 148070 64345547
Parkinsonism 219.84 35.97 70 5045 14303 64479314
Sedation 188.88 35.97 83 5032 41379 64452238
Hospitalisation 147.41 35.97 85 5030 75122 64418495
Death 146.87 35.97 185 4930 482520 64011097
Dyskinesia 126.73 35.97 62 5053 39326 64454291
Anxiety 105.16 35.97 103 5012 202546 64291071
Restlessness 97.11 35.97 52 5063 39733 64453884
Fall 84.79 35.97 132 4983 416694 64076923
Therapeutic product effect decreased 84.02 35.97 71 5044 115280 64378337
Balance disorder 81.09 35.97 61 5054 83865 64409752
Therapeutic product effect incomplete 73.91 35.97 63 5052 103419 64390198
Fatigue 67.28 35.97 168 4947 748562 63745055
Urticaria 62.00 35.97 67 5048 147250 64346367
Dizziness 61.99 35.97 117 4998 430046 64063571
Feeling abnormal 61.98 35.97 64 5051 133538 64360079
Drug ineffective 61.78 35.97 175 4940 840072 63653545
Lethargy 55.51 35.97 46 5069 72548 64421069
Adverse drug reaction 52.87 35.97 37 5078 45427 64448190
Akathisia 48.97 35.97 22 5093 11488 64482129
Depression 45.64 35.97 64 5051 183227 64310390
Gait disturbance 44.19 35.97 61 5054 172094 64321523
Salivary hypersecretion 41.72 35.97 20 5095 12093 64481524
Bradykinesia 39.36 35.97 16 5099 6544 64487073
Insomnia 37.72 35.97 61 5054 197775 64295842

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
Synaptic vesicular amine transporter Transporter INHIBITOR Ki 6.73 IUPHAR

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-1060 CAPSULE 60 mg ORAL NDA 28 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-1080 CAPSULE 80 mg ORAL NDA 28 sections
INGREZZA HUMAN PRESCRIPTION DRUG LABEL 1 70370-2040 CAPSULE 40 mg ORAL NDA 28 sections