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	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

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

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
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 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	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 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
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:

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])	Mechanism action	Bioact source	MoA source
Synaptic vesicular amine transporter	Transporter	Q05940	VMAT2_HUMAN	INHIBITOR	Ki	8.52		DRUG LABEL	DRUG LABEL
Synaptic vesicular amine transporter	Transporter		VMAT2_RAT	INHIBITOR	Ki	6.73		IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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