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

Stem definition	Drug id	CAS RN
	5227	1025504-45-3

Description:

Molecule	Description
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

Molecule

Description

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:

Property	Value	Reference
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:

Date	Agency	Company	Orphan
April 11, 2017	FDA	NEUROCRINE BIOSCIENCES INC
March 28, 2022	PMDA	Mitsubishi Tanabe Pharma Corporation

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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|

Disease	Relation	SNOMED_ID	DOID
Tardive dyskinesia	indication	102449007

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.25	Basic
pKa2	7.56	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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 strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Synaptic vesicular amine transporter	Transporter	Q05940	VMAT2_HUMAN	INHIBITOR	Ki	8.52	DRUG LABEL	DRUG LABEL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.77	CHEMBL
Synaptic vesicular amine transporter	Transporter		VMAT2_RAT	INHIBITOR	Ki	6.73	IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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