Page last updated: 2024-12-05

tetrabenazine

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Description

9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

(3S,11bS)-9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one : A 9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one in which both stereocentres have S configuration. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID6018
CHEMBL ID117785
CHEBI ID64028
CHEBI ID9467
SCHEMBL ID62026
MeSH IDM0021208
PubMed CID11634155
CHEMBL ID519344
CHEBI ID64030
SCHEMBL ID12394431
MeSH IDM0021208

Synonyms (199)

Synonym
ro-19569
ro-1-9569
chebi:64028 ,
ro 1-9569/12
nsc172187
2-oxo-3-isobutyl-9,2,3,4,6,7-hexahydro-11bh-benzo[a]quinolizine
1,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2h-benzo[a]quinolizin-2-one
rubigen
wln: t b666 dv gntt&j e1y1&1 lo1 mo1
nsc-172187
tetrabenzine
nsc-169886
nitoman
tetrabenzaine
mls003106727 ,
2h-benzo[a]quinolizin-2-one,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-
2h-benzo[a]quinolizin-2-one,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-
nsc169886
2-oxo-3-isobutyl-9,3,4,6,7,11.beta.-hexahydro-2h-benzoquinolizine
tetra benazin
1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2h-benzo[a]quinolizin-2-one
nsc 169886
2h-benzo(a)quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-
tetrabenazinum [inn-latin]
2h-benzo(a)quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-
tetrabenazina [inn-spanish]
TIMTEC1_002217
58-46-8
tetrabenazine ,
1,2,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2h-benzo[a]quinolizin-2-one
DB04844
2-oxo-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-benzoquinolizine
2-oxo-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bh-benzo[a]quinolizine
OPREA1_264344
MLS001249426
smr000718664
9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one
HMS1540E17
NCGC00160421-02
MLS001249497
BRD-A47564106-001-01-8
nitoman (tn)
xenazine (tn)
tetrabenazine (jan/inn)
D08575
9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one
3-isobutyl-9,10-dimethoxy-3,4,6,7-tetrahydro-1h-pyrido[2,1-a]isoquinolin-2(11bh)-one ,
bdbm50017701
chembl117785 ,
3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-pyrido[2,1-a]isoquinolin-2-one
AKOS001681311
STK678061
HMS3263I14
HMS2966E06
CCG-118217
FT-0674921
tetrabenazinum
9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one
LP01086
PB38735
PB25061
PB21652
S1789
AKOS016347602
revocon
gtpl4834
9,10-dimethoxy-3-(2-methylpropyl)-1h,2h,3h,4h,6h,7h,11bh-pyrido[2,1-a]isoquinolin-2-one
3-isobutyl-9-,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-benzo[a]quinolizin-2-one
tetrabenazine racemate
718635-93-9
SCHEMBL62026
tox21_501086
NCGC00261771-01
tetrabenazin
2-oxo-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7,11b-hexahydro-2h-benzo(a)quinolizine
3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one #
2h-benzo[a]quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-
2h-benzo[a]quinolizin-2-one, 1,3,4,6,7, 11b-hexahydro-3-isobutyl-9,10-dimethoxy-,
HMS3430F03
mfcd00042740
CS-5700
HY-B0590A
tetrabenazine (racemate)
sr-01000833864
SR-01000833864-4
FT-0771873
BCP24156
Q413050
mfcd11519951
SY055407
Z1544404943
FT-0772314
tetrabenazine (nitoman, xenazine)
FT-0700948
EX-A2361
AS-35785
ro 1-9569 racemate
SDCCGSBI-0633786.P001
HMS3884E10
NCGC00160421-06
nitoman;ro 1-9569
BCP15831
A917912
tetrabenazine (3r,11br)-rel-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2h-benzo[a]quinolizin-2-one
A856325
SB49797
EN300-122639
tetrabenazine- bio-x
BT164463
SY333387
DTXSID501127442
9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2h-pyrido(2,1-a)isoquinolin-2-one
tetrabenazine (mart.)
2-oxo-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11-beta-hexahydro-
9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydro-2h-pyrido(2,1-a)isoquinolin-2-one
chebi:9467
n07xx06
tetrabenazina (inn-spanish)
tetrabenazine (usp-rs)
1,2,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2h-benzo(a)quinolizin-2-one
rac-(3s,11bs)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydro-2h-pyrido(2,1-a)isoquinolin-2-one
(3rs,11brs)-9,10-dimethoxy-3-(2-methylpropyl)-3,4,6,7-tetrahydro-1h-pyrido(2,1-a)isoquinolin-2(11bh)-one
tetrabenazinum (latin)
tetrabenazinum (inn-latin)
2-oxo-3-isobutyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bh-benzo(a)quinolizine
HMS3268P05
BRD-K95739795-001-01-1
ro 1-9569
2-oxo-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11-beta-hexahydro-2h-benzoquinolizine
1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy-2h-benzo(a)quinolizin-2-one
einecs 200-383-6
ai3-52046
c19h27no3
brn 0040090
tetrabenazine [inn:ban]
NCGC00160421-01
NCGC00092321-01
(3s,11bs)-tetrabenazine
CHEMBL519344 ,
chebi:64030 ,
xenazine
1026016-84-1
2h-benzo[a]quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-, (3s,11bs)-
dtxsid0042614 ,
cas-58-46-8
tox21_111803
dtxcid001476353
bdbm50342818
T2839
3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-benzo[a]quinolizin-2-one
tetrabenazina
z9o08yrn8o ,
5-21-13-00178 (beilstein handbook reference)
unii-z9o08yrn8o
hsdb 8412
(s,s)-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2h-benzo[a]quinolizin-2-one
(3s,11bs)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one
(3s,11bs)-9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one
(-)-ro 1-9569
MKJIEFSOBYUXJB-HOCLYGCPSA-N
8a3np33e5m ,
tetrabenazine [vandf]
tetrabenazine, (-)-
tetrabenazine [usp-rs]
tetrabenazine [mi]
unii-8a3np33e5m
tetrabenazine [mart.]
tetrabenazine [who-dd]
(-)-tbz
tetrabenazine [orange book]
(3s,11bs)-tbz
tetrabenazine [jan]
tetrabenazine [inn]
2h-benzo(a)quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-, (3r,11br)-rel-
2h-benzo(a)quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-, (3s,11bs)
AKOS022177259
NCGC00160421-03
tox21_111803_1
(3r,11br)-rel-1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-2h-benzo[a]quinolizin-2-one
SCHEMBL12394431
Q-101507
3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one
(3s,11bs)-3-isobutyl-9,10-dimethoxy-3,4,6,7-tetrahydro-1h-pyrido[2,1-a]isoquinolin-2(11bh)-one
(3r,11br)-rel-1,3,4,6,7,11b-hexahyd ro-9,10-dimethoxy-3-(2-methylpropyl)-2h-benzo[a]qu inolizin-2-one
HB1711
Q27132978
(3s,11bs)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one ,
HMS3677K03
HMS3413K03
SB13207
(3s,11bs)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydrobenzo[a]quinolizin-2-one
NCGC00092321-03
2h-benzo[a]quinolizin-2-one, 1,3,4,6,7,11b-hexahydro-9,10-dimethoxy-3-(2-methylpropyl)-, (3r,11br)-rel-
A896751
BRB01684
(-)-tetrabenazine-d3
(3s,11bs)-9,10-dimethoxy-3-(2-methylpropyl)-1h,2h,3h,4h,6h,7h,11bh-pyrido[2,1-a]isoquinolin-2-one
EN300-7429993
(3s,5r,11bs)-9,10-dimethoxy-3-(2-methylpropyl)-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-one

Research Excerpts

Overview

Tetrabenazine (TBZ) is a non-competitive inhibitor of VMAT2 that is used in the treatment of hyperkinetic disorders associated with Huntington disease and Tourette syndrome. DeutetrAbenazine is a deuterated form of tetrabinazine with a confirmed lower rate of CYP2D6 metabolism of the active metabolites.

ExcerptReferenceRelevance
"Tetrabenazine (TBZ) is a non-competitive inhibitor of VMAT2 that is used in the treatment of hyperkinetic disorders associated with Huntington disease and Tourette syndrome."( Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine.
Gros, Y; Schuldiner, S; Segal, T; Ugolev, Y; Yaffe, D, 2013
)
1.31
"Deutetrabenazine is a deuterated form of tetrabenazine with a confirmed lower rate of CYP2D6 metabolism of the active metabolites, α- and β-HTBZ. "( The effect of potent CYP2D6 inhibition on the pharmacokinetics and safety of deutetrabenazine in healthy volunteers.
Bradbury, MJ; Gordon, MF; Loupe, PS; Rabinovich-Guilatt, L; Schneider, F; Stamler, D, 2022
)
1.57
"Deutetrabenazine is a selective vesicular monoamine transporter 2 inhibitor approved for the treatment of chorea associated with Huntington disease and tardive dyskinesia in adults."( Safety and Efficacy of Flexible-Dose Deutetrabenazine in Children and Adolescents With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, J; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
1.4
"Deutetrabenazine is a vesicular monoamine transporter 2 inhibitor approved in the US for the treatment of chorea associated with Huntington disease and tardive dyskinesia."( Efficacy and Safety of Fixed-Dose Deutetrabenazine in Children and Adolescents for Tics Associated With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, JK; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
1.41
"Tetrabenazine is a US Food and Drug Administration (FDA)-approved drug that exhibits a dopamine depleting effect and is used for the treatment of chorea in Huntington's disease. "( Synthesis of Tetrabenazine and Its Derivatives, Pursuing Efficiency and Selectivity.
Paek, SM, 2020
)
2.37
"Tetrabenazine (TBZ) is a vesicular monoamine transport type-2 inhibitor that blocks DA storage and depletes DA."( The dopamine depleting agent tetrabenazine alters effort-related decision making as assessed by mouse touchscreen procedures.
Correa, M; Fitch, RH; Okifo, K; Presby, RE; Quiles, T; Rotolo, RA; Salamone, JD; Yang, JH; Zorda, E, 2020
)
1.57
"Deutetrabenazine is a derivative of tetrabenazine in which two trideuteromethoxy groups substitute two methoxy groups. "( Deutetrabenazine: Treatment of hyperkinetic aspects of Huntington's disease, tardive dyskinesia and Tourette syndrome.
Paton, DM, 2017
)
1.7
"Deutetrabenazine is a deuterated formulation of tetrabenazine. "( Deutetrabenazine for tardive dyskinesia: A systematic review of the efficacy and safety profile for this newly approved novel medication-What is the number needed to treat, number needed to harm and likelihood to be helped or harmed?
Citrome, L, 2017
)
1.7
"Deutetrabenazine is a deuterated form of tetrabenazine and is a vesicular monoamine transporter 2 (VMAT2) inhibitor."( Review of deutetrabenazine: a novel treatment for chorea associated with Huntington's disease.
Dean, M; Sung, VW, 2018
)
1.36
"Deutetrabenazine (DTBZ) is a US FDA-approved treatment for chorea in Huntington's disease. "( Deutetrabenazine in the treatment of Huntington's disease.
Frank, S; Richard, A, 2019
)
1.76
"Tetrabenazine (TBZ) is a reversible inhibitor of vesicular monoamine storage that is used to treat Huntington's disease. "( The vesicular monoamine transporter (VMAT-2) inhibitor tetrabenazine induces tremulous jaw movements in rodents: implications for pharmacological models of parkinsonian tremor.
Baqi, Y; Barber, J; Correa, M; Lee, CA; Lendent, C; López-Cruz, L; Milligan, M; Müller, CE; Nunes, EJ; Pardo, M; Podurgiel, SJ; Salamone, JD; Thompson, A; Valverde, O; Yohn, SE, 2013
)
2.08
"Tetrabenazine is a dopamine-depleting agent that may be one of the more effective agents for reducing chorea, although it has a risk of potentially serious adverse effects."( Treatment of Huntington's disease.
Frank, S, 2014
)
1.12
"Tetrabenazine (TBZ) is a possible option for treating TT.This study aimed to evaluate the efficacy and tolerability of TBZ in elderly patients with TT."( Tetrabenazine for tardive tremor in elderly adults: a prospective follow-up study.
Barak, Y; Kertesz, DP; Plopski, I; Swartz, MV; Tadger, S,
)
2.3
"Deutetrabenazine is a novel molecule containing deuterium, which attenuates CYP2D6 metabolism and increases active metabolite half-lives and may therefore lead to stable systemic exposure while preserving key pharmacological activity."( Effect of Deutetrabenazine on Chorea Among Patients With Huntington Disease: A Randomized Clinical Trial.
Agarwal, P; Anderson, KE; Beck, C; Beland, M; Blindauer, KA; Boyd, JT; Brashers-Krug, T; Carlson, A; Chouinard, S; Christopher, E; Claassen, DO; Clouse, R; Colcher, A; Criswell, S; Davis, C; Dhall, R; Dubinsky, RM; Duker, A; Eberly, SW; Edicola, J; Edmondson, MC; Eglow, M; Esmail, S; Evans, S; Factor, SA; Fafard, L; Farbman, ES; Feigin, A; Frank, S; Fung, WL; Gibbons, C; Goldstein, J; Graffitti, L; Gray, C; Gudesblatt, M; Hackmyer, C; Heller, H; Herzog, M; Hickey, PT; Hohler, A; Houston, E; Hunter, C; James, RC; Janicki, S; Jankovic, J; Jimenez-Shahed, J; Kayson, E; Kerr, J; Kinel, S; Klos, K; Kumar, R; LaFaver, K; Leavitt, B; Margolis, RL; McGarry, A; Mendis, N; Mendis, T; Miller, A; Molho, E; Neefus, E; Nucifora, F; O'Neill, C; Oakes, D; Ong, M; Orme, C; Paulsen, JS; Qi, L; Quesada, M; Racette, BA; Reeves, C; Revilla, FJ; Rizer, K; Rodriguez, R; Roman, OC; Saint-Hilaire, M; Samii, A; Schneider, DP; Scott, BL; Shprecher, D; Singer, C; Smith, J; Snively, V; Sperin, E; Stamler, D; Sung, V; Suter, G; Tariot, PN; Testa, CM; Turpin, D; Vaughan, C; Wall, P; Watts, A; Whaley, J; Wheeler, L; Wilson-Perez, H; Wojcieszek, JM; Wong, C, 2016
)
1.42
"Tetrabenazine is a benzoquinolizine with a high antidopaminergic potential due to a monoamine depletion effect that acts equally on the three main neurotransmitters (dopamine, noradrenalin and serotonin). "( [Therapeutic use of tetrabenazine].
López Del Val, LJ; López-García, E; Martínez-Martínez, L; Santos-Lasaosa, S,
)
1.9
"Tetrabenazine appears to be an excellent pharmacological agent for use in a number of pathologies that are accompanied by hyperkinesias; it is well tolerated and has few complications or side effects deriving from its administration."( [Therapeutic use of tetrabenazine].
López Del Val, LJ; López-García, E; Martínez-Martínez, L; Santos-Lasaosa, S,
)
1.9
"Tetrabenazine (TBZ) is a monoamine-depleting agent initially studied in the 1950s and currently approved by the US Food and Drug Administration for the treatment of chorea in Huntington's disease."( Tetrabenazine, a monoamine-depleting drug used in the treatment of hyperkinetic movement disorders.
Guay, DR, 2010
)
2.52
"Tetrabenazine is a central monoamine-depleting agent approved by the Food and Drug Administration for chorea associated with Huntington's disease."( Tetrabenazine for the treatment of tardive dyskinesia.
Breden, EL; Leung, JG, 2011
)
2.53
"Tetrabenazine (TBZ) is a monoamine storage inhibitor that was first introduced in the 1970s for the management of hyperkinetic movement disorders. "( Tetrabenazine for the treatment of hyperkinetic movement disorders: a review of the literature.
Chen, JJ; Dashtipour, K; Ondo, WG; Swope, DM, 2012
)
3.26
"Tetrabenazine (TBZ) is a catecholamine depletor used for the treatment of a variety of movement disorders. "( Tetrabenazine treatment in movement disorders.
Badarny, S; Giladi, N; Honigman, S; Moore, O; Paleacu, D; Stern, A,
)
3.02
"Tetrabenazine is a useful and safe therapeutic agent in some patients with hyperkinetic movement disorders."( Treatment of hyperkinetic movement disorders with tetrabenazine: a double-blind crossover study.
Jankovic, J, 1982
)
1.24
"Tetrabenazine is considered to be a reserpine-like drug because of its ability to block dopamine storage in presynaptic vesicles. "( Neuroendocrine evidence that tetrabenazine is a dopamine antagonist.
Cronin, MJ; Harcus, CT; Login, IS; MacLeod, RM, 1983
)
2
"[11C]Tetrabenazine is a promising new radioligand for the in vivo study of monoaminergic neurons using PET."( Synthesis of [11C]tetrabenazine, a vesicular monoamine uptake inhibitor, for PET imaging studies.
DaSilva, JN; Kilbourn, MR; Mangner, TJ, 1993
)
1.07
"Tetrabenazine is a high-affinity inhibitor of the vesicular monoamine transporter in mammalian brain. "( In vitro and in vivo studies of benzisoquinoline ligands for the brain synaptic vesicle monoamine transporter.
Frey, KA; Kilbourn, MR; Lee, LC; Sherman, PS; Vander Borght, T, 1996
)
1.74
"[11C]Tetrabenazine ([11C]TBZ) is a new in vivo radioligand for positron emission tomographic (PET) imaging of vesicular monoamine transporters. "( Characterization of [11C]tetrabenazine as an in vivo radioligand for the vesicular monoamine transporter.
Carey, JE; DaSilva, JN; Kilbourn, MR; Pisani, TJ; Sherman, PS, 1994
)
1.11
"Tetrabenazine has proved to be a safe and frequently useful drug in the long-term treatment of approximately 400 dyskinetic patients."( Neuroleptic malignant syndrome related to tetrabenazine introduction and haloperidol discontinuation in Huntington's disease.
Giménez-Roldán, S; Mateo, D; Muñoz-Blanco, JL, 1992
)
1.27
"Tetrabenazine is an effective and relatively safe drug for a variety of hyperkinetic movement disorders."( Tetrabenazine therapy of dystonia, chorea, tics, and other dyskinesias.
Jankovic, J; Orman, J, 1988
)
2.44
"Tetrabenazine is an effective agent for the suppression of choreiform and ballistic involuntary movements."( Treatment of involuntary movement disorders with tetrabenazine.
Heathfield, KW; Roberts, AH; Swash, M; Zakko, H, 1972
)
1.23

Effects

Tetrabenazine has been used for treatment of tardive dyskinesia sporadically over the past twenty years. It also has a black box warning for increasing the risk of depression and suicidality.

ExcerptReferenceRelevance
"Tetrabenazine also has a black box warning for increasing the risk of depression and suicidality."( Role of tetrabenazine for Huntington's disease-associated chorea.
Kang, GA; Lee, AJ; Poon, LH, 2010
)
1.52
"Tetrabenazine also has a black box warning for increasing the risk of depression and suicidality."( Role of tetrabenazine for Huntington's disease-associated chorea.
Kang, GA; Lee, AJ; Poon, LH, 2010
)
1.52
"Tetrabenazine has proved to be a safe and frequently useful drug in the long-term treatment of approximately 400 dyskinetic patients."( Neuroleptic malignant syndrome related to tetrabenazine introduction and haloperidol discontinuation in Huntington's disease.
Giménez-Roldán, S; Mateo, D; Muñoz-Blanco, JL, 1992
)
1.27
"Tetrabenazine has been used for treatment of tardive dyskinesia sporadically over the past twenty years. "( Treatment of tardive dyskinesia: preliminary report on use of tetrabenazine.
Jamali, F; Skelton, D; Watson, MW, 1988
)
1.96

Actions

ExcerptReferenceRelevance
"Tetrabenazine dosing was lower than predicted, and many patients experienced adverse symptoms of intolerability at high doses."( Tetrabenazine Treatment Patterns and Outcomes for Chorea Associated with Huntington Disease: A Retrospective Chart Review.
Abler, V; Claassen, DO; DiBonaventura, M; Iyer, RG; Shah-Manek, B; Sung, VW, 2018
)
2.64

Treatment

Tetrabenazine (1mg/kg sc) depletes the transmitters from their stores in the nerve terminals of the catecholaminergic neurons and blocks the acquisition of a CAR. The greatest reduction was dopamine in the caudate.

ExcerptReferenceRelevance
"Deutetrabenazine treatment was associated with sustained improvements in total motor AIMS score, treatment success, and improved quality of life, and was well tolerated in younger and older adults with TD in this 3-year OLE study."( Long-Term Safety and Efficacy of Deutetrabenazine in Younger and Older Patients With Tardive Dyskinesia.
Barkay, H; Chaijale, N; Finkbeiner, S; Gordon, MF; Gross, N; Sajatovic, M; Wilhelm, A, 2022
)
1.62
"Tetrabenazine-treatment (1mg/kg sc) depletes the transmitters from their stores in the nerve terminals of the catecholaminergic neurons and blocks the acquisition of a CAR."( Essential difference between the pharmacological spectrum of (-)-deprenyl and rasagiline.
Miklya, I, 2014
)
1.12
"Tetrabenazine, a treatment for chorea in Huntington disease, carries a boxed warning due to safety, especially related to suicidality."( Depressed mood and suicidality in individuals exposed to tetrabenazine in a large Huntington disease observational study.
Anderson, KE; Beck, CA; Biglan, KM; Brocht, AF; Darwin, KC; Dorsey, ER; Nichols, PE; Shoulson, I; Singh, S, 2013
)
2.08
"Tetrabenazine treatment (1 mg/kg, s.c.) depletes from their stores the transmitters of the catecholaminergic neurons of the brain stem."( [A comparison of the pharmacology of (-)-deprenyl to N-methylpropargylamine-1-aminoindane (J-508) and rasagiline, the desmethyl-analogue of J-508].
Miklya, I, 2008
)
1.07
"The tetrabenazine-treated group showed a general description of monoamines in all regions studied, the greatest reduction being dopamine in the caudate."( Depletion of monoamine transmitters by tetrabenazine in brain tissue in Huntington's disease.
Pearson, SJ; Reynolds, GP, 1988
)
1.03
"Tetrabenazine pretreatment prevented the antidiuretic response to histamine.5."( Mechanism of histamine-induced antidiuretic response.
Bhargava, KP; Kulshrestha, VK; Santhakumari, G; Srivastava, YP, 1973
)
0.97
"Treatment with tetrabenazine did not significantly alter the metabolite levels in patients in whom it produced either improvement, or side effects."( CSF studies on the relationship between dopamine and 5-hydroxytryptamine in Parkinsonism and other movement disorders.
Davidson, DL; Mawdsley, C; Pullar, IA; Wilson, H; Yates, CM, 1977
)
0.6

Toxicity

Deutetrabenazine was initiated at 12 mg/day and titrated once weekly by 6mg/day using a response-driven dosing regimen. Treatment-emergent adverse events were reported for 38 patients (66%) and 33 patients (56%) receiving deutetrabsenazine and placebo. No clinical improvements were observed with carbidopa/levodopa, tetrabasine, or clonazepam.

ExcerptReferenceRelevance
" As an extension of this hypothesis, the relative resistance of some brain monoaminergic neurons to the toxic actions of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine may result from the subcellular sequestration of MPP+ in the storage vesicle."( Subcellular compartmentalization of 1-methyl-4-phenylpyridinium with catecholamines in adrenal medullary chromaffin vesicles may explain the lack of toxicity to adrenal chromaffin cells.
Daniels, AJ; Diliberto, EJ; Reinhard, JF; Viveros, OH, 1987
)
0.27
" To verify this hypothesis, we investigated the influence of hypothermia on the toxic activity of both neurotoxins."( Apparent opposite effects of tetrabenazine and reserpine on the toxic effects of 1-methyl-4-phenylpyridinium or 6-hydroxydopamine on nigro-striatal dopaminergic neurons.
Cleren, C; Costentin, J; Naudin, B, 2003
)
0.61
"5mg/kg PM treatments antagonized the toxic effect of MPTP on TH and DAT expression (p<0."( Neurotoxicity in murine striatal dopaminergic pathways following long-term application of low doses of permethrin and MPTP.
Bloomquist, JR; Kou, J, 2007
)
0.34
" Valbenazine is about 15 times more likely to result in a response than in a discontinuation because of an adverse event."( Valbenazine for tardive dyskinesia: A systematic review of the efficacy and safety profile for this newly approved novel medication-What is the number needed to treat, number needed to harm and likelihood to be helped or harmed?
Citrome, L, 2017
)
0.46
"Safety measures included adverse events (AEs), clinical laboratory tests, vital signs, electrocardiograms, and validated scales."( Safety of Converting From Tetrabenazine to Deutetrabenazine for the Treatment of Chorea.
Claassen, DO; Colcher, A; Davis, C; Duker, A; Eberly, S; Elmer, L; Frank, S; Furr-Stimming, E; Goldstein, J; Gudesblatt, M; Hunter, C; Jankovic, J; Kayson, E; Kostyk, SK; Kumar, R; Loy, C; Mallonee, W; Oakes, D; Scott, BL; Stamler, D; Sung, V; Testa, CM; Vaughan, C, 2017
)
0.76
" Safety assessments included adverse events (AEs), laboratory tests, vital signs, electrocardiograms (ECGs), and extrapyramidal symptom (EPS) scales."( Long-Term Safety and Tolerability of Valbenazine (NBI-98854) in Subjects with Tardive Dyskinesia and a Diagnosis of Schizophrenia or Mood Disorder.
Burke, J; Josiassen, RC; Kane, JM; Liang, GS; O'Brien, CF, 2017
)
0.46
" Safety measures included incidence of adverse events (AEs) and scales used to monitor parkinsonism, akathisia/restlessness, anxiety, depression, suicidality and somnolence/sedation."( Long-term safety and efficacy of deutetrabenazine for the treatment of tardive dyskinesia.
Anderson, KE; Bega, D; Davis, MD; Factor, SA; Fernandez, HH; Hauser, RA; Jarskog, LF; Jimenez-Shahed, J; LeDoux, MS; Ondo, WG; Shprecher, DR; Stamler, D; Woods, SW, 2019
)
0.79
"Deutetrabenazine was initiated at 12 mg/day and titrated once weekly by 6 mg/day using a response-driven dosing regimen until adequate dyskinesia control was reached or a clinically significant adverse event occurred."( Long-Term Safety and Efficacy of Deutetrabenazine in Younger and Older Patients With Tardive Dyskinesia.
Barkay, H; Chaijale, N; Finkbeiner, S; Gordon, MF; Gross, N; Sajatovic, M; Wilhelm, A, 2022
)
1.62
"To examine whether deutetrabenazine is effective and safe for the treatment of Tourette syndrome in children and adolescents."( Safety and Efficacy of Flexible-Dose Deutetrabenazine in Children and Adolescents With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, J; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
1.2
" Safety was assessed based on treatment-emergent adverse events, vital signs, questionnaires, and laboratory parameters."( Safety and Efficacy of Flexible-Dose Deutetrabenazine in Children and Adolescents With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, J; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
0.89
" Treatment-emergent adverse events were reported for 38 patients (66%) and 33 patients (56%) receiving deutetrabenazine and placebo, respectively, and were generally mild or moderate."( Safety and Efficacy of Flexible-Dose Deutetrabenazine in Children and Adolescents With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, J; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
1.1
" Safety assessments included incidence of treatment-emergent adverse events, laboratory parameters, vital signs, and questionnaires."( Efficacy and Safety of Fixed-Dose Deutetrabenazine in Children and Adolescents for Tics Associated With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, JK; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
0.89
" Treatment-emergent adverse events were reported for 34 participants (65%) treated with high-dose deutetrabenazine, 24 (44%) treated with low-dose deutetrabenazine, and 25 (49%) treated with placebo and were generally mild or moderate."( Efficacy and Safety of Fixed-Dose Deutetrabenazine in Children and Adolescents for Tics Associated With Tourette Syndrome: A Randomized Clinical Trial.
Alexander, JK; Barkay, H; Claassen, DO; Coffey, B; Garofalo, EA; Gertz, BJ; Gordon, MF; Harary, E; Jankovic, J; Jimenez-Shahed, J; Savola, JM; Stamler, DA; Wieman, M, 2021
)
1.11
" Incidence of adverse events was highest in the 80-mg group; common events included nasopharyngitis, somnolence, schizophrenia worsening, hypersalivation, insomnia, and tremor."( Efficacy and safety of valbenazine in Japanese patients with tardive dyskinesia: A multicenter, randomized, double-blind, placebo-controlled study (J-KINECT).
Horiguchi, J; Iwatake, A; Kondo, K; Masui, H; Sakamoto, H; Susuta, Y; Watanabe, K; Watanabe, Y, 2022
)
0.72
" Safety assessments included treatment-emergent adverse events, vital signs, electrocardiograms, laboratory tests, clinical tests for parkinsonism, and psychiatric assessments."( Safety and efficacy of valbenazine for the treatment of chorea associated with Huntington's disease (KINECT-HD): a phase 3, randomised, double-blind, placebo-controlled trial.
Claassen, DO; Furr Stimming, E; Goldstein, J; Haubenberger, D; Kayson, E; Liang, GS; Mehanna, R; Zhang, H, 2023
)
0.91
" The most commonly reported treatment-emergent adverse event was somnolence (ten [16%] with valbenazine, two [3%] with placebo)."( Safety and efficacy of valbenazine for the treatment of chorea associated with Huntington's disease (KINECT-HD): a phase 3, randomised, double-blind, placebo-controlled trial.
Claassen, DO; Furr Stimming, E; Goldstein, J; Haubenberger, D; Kayson, E; Liang, GS; Mehanna, R; Zhang, H, 2023
)
0.91
" The review included patients diagnosed with chorea and NKX2-1-RD genetic diagnosis, drug therapy as intervention, no comparator, and outcomes of chorea improvement and adverse events."( Systematic review of drug therapy for chorea in NXK2-1-related disorders: Efficacy and safety evidence from case studies and series.
Bachoud-Lévi, AC; Blasco-Amaro, JA; Capuano, A; Isabel-Gómez, R; Martín-Gómez, C; Nou-Fontanet, L; Ortigoza-Escobar, JD; Zorzi, G, 2023
)
0.91
" No clinical improvements were observed with carbidopa/levodopa, tetrabenazine, or clonazepam, and various adverse effects were reported."( Systematic review of drug therapy for chorea in NXK2-1-related disorders: Efficacy and safety evidence from case studies and series.
Bachoud-Lévi, AC; Blasco-Amaro, JA; Capuano, A; Isabel-Gómez, R; Martín-Gómez, C; Nou-Fontanet, L; Ortigoza-Escobar, JD; Zorzi, G, 2023
)
1.15

Pharmacokinetics

ExcerptReferenceRelevance
"A few conclusive experimental models (barbiturate sleep, tetrabenazine reversion, maximum electroshock) were chosen to collect comprehensive data on the pharmacodynamic characteristics of amitriptylinoxide."( Special experiments on central nervous effects of amitriptylinoxide considering pharmacokinetic aspects.
Wenzl, H, 1978
)
0.5
" In both the patients and rats, the plasma profile of TBZ followed characteristics of a multiexponential pharmacokinetic model."( Pharmacokinetics of tetrabenazine and its major metabolite in man and rat. Bioavailability and dose dependency studies.
Jamali, F; Mehvar, R; Skelton, D; Watson, MW,
)
0.45
" The characteristics of high specific binding ratio, reversibility, metabolic stability and longer half-life of the radionuclide make [(18)F]FP-(+)-DTBZ a promising alternative VMAT2 radioligand suitable for widespread use in human positron emission tomography studies of monoaminergic innervation of the brain."( Pharmacokinetics of [(18)F]fluoroalkyl derivatives of dihydrotetrabenazine in rat and monkey brain.
Goswami, R; Hockley, B; Hou, C; Kilbourn, MR; Kung, HF; Kung, MP; Lee, L; Ponde, DE, 2007
)
0.58
" After method validation, an enantioselective in vitro metabolism and in vivo pharmacokinetic prediction was carried out."( In vitro enantioselective human liver microsomal metabolism and prediction of in vivo pharmacokinetic parameters of tetrabenazine by DLLME-CE.
Bocato, MZ; de Albuquerque, NCP; de Gaitani, CM; de Lima Moreira, F; de Oliveira, ARM, 2016
)
0.64
" Terminal elimination half-life for both VBZ and NBI-98782 was ~20 hours."( Single Dose and Repeat Once-Daily Dose Safety, Tolerability and Pharmacokinetics of Valbenazine in Healthy Male Subjects.
Bozigian, H; Jimenez, R; Loewen, G; Luo, R; O'Brien, CF, 2017
)
0.46
" Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs."( Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals.
Bednarczyk, EM; Russak, EM, 2019
)
0.51

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" The second study was an open-label 5-way crossover study in healthy volunteers (n = 32) to evaluate relative bioavailability of 4 dose levels of the commercial formulation of deutetrabenazine (6, 12, 18, and 24 mg) with a standard meal and 18 mg with a high-fat meal."( Pharmacokinetics of Deutetrabenazine and Tetrabenazine: Dose Proportionality and Food Effect.
Bradbury, M; Cox, DS; Gordon, MF; Hellriegel, E; Loupe, PS; Rabinovich-Guilatt, L; Savola, JM; Schneider, F; Stamler, D, 2021
)
1.12
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Two pivotal clinical trials provide evidence that deutetrabenazine dosed 24-48 mg/day effectively controlled involuntary movements. The single high dose of MPTP produced greater losses of [(11)C]dihydrotetrabENazine binding than did the multiple MPTP.

ExcerptRelevanceReference
" In the previously reported case, factors capable of potentiating NMS included a high dosage of tetrabenazine exceeding the accepted therapeutic range, and co-medication with the dopamine-synthesis inhibitor alpha-methylparatyrosine, while in the present case abrupt introduction of the drug and discontinuation of concomitant neuroleptics may have contributed to this important adverse reaction."( Neuroleptic malignant syndrome related to tetrabenazine introduction and haloperidol discontinuation in Huntington's disease.
Giménez-Roldán, S; Mateo, D; Muñoz-Blanco, JL, 1992
)
0.77
"986 for TBZ and HTBZ, respectively, suggesting linear kinetics in the examined dosage range."( Pharmacokinetics of tetrabenazine and its major metabolite in man and rat. Bioavailability and dose dependency studies.
Jamali, F; Mehvar, R; Skelton, D; Watson, MW,
)
0.45
" Cumulative dosing of methamphetamine and morphine increased response rates without marked changes in avoidance rates in the shuttle avoidance response."( [Effects of psychotropic drugs by the cumulative-dosing procedure on lever-press and shuttle discrete avoidance responses in mice].
Furusawa, K; Kuribara, H; Tadokoro, S, 1987
)
0.27
" During the evaluation period, all but 4 patients were treated for three or more weeks at a maximum dosage of 200 mg per day."( Treatment of hyperkinetic movement disorders with tetrabenazine: a double-blind crossover study.
Jankovic, J, 1982
)
0.52
" With respect to both dosage and time, striatal DA was most sensitive to the effects of TBZ while hypothalamic NE was least affected."( Tetrabenazine-induced depletion of brain monoamines: characterization and interaction with selected antidepressants.
Pettibone, DJ; Pflueger, AB; Totaro, JA, 1984
)
1.71
" All active compounds gave inverted U-shaped dose-response curves."( Cognition-activating properties of 3-(Aryloxy)pyridines.
Butler, DE; Marriott, JG; Poschel, BP, 1981
)
0.26
" The ED50 values 4 h after oral dosing were 13."( Topiramate: preclinical evaluation of structurally novel anticonvulsant.
Davis, CB; Dodgson, SJ; Gardocki, JF; Maryanoff, BE; Nortey, SO; Raffa, RB; Schupsky, JJ; Shank, RP; Vaught, JL,
)
0.13
" The single high dose of MPTP produced greater losses of [(11)C]dihydrotetrabenazine binding than did the multiple MPTP dosing regimen."( Rapid and differential losses of in vivo dopamine transporter (DAT) and vesicular monoamine transporter (VMAT2) radioligand binding in MPTP-treated mice.
Kilbourn, MR; Kuszpit, K; Sherman, P, 2000
)
0.54
" TBZ should be dosed individually based on ongoing assessment of possible adverse side effects."( Tetrabenazine as antichorea therapy in Huntington disease: a randomized controlled trial.
, 2006
)
1.78
" Pharmacists managing patients on TBZ need to be well versed in TBZ's potential side effects, drug interactions, and unique dosing considerations."( Treatment of chorea associated with Huntington's disease: focus on tetrabenazine.
Clark, J; Dobbins, EK; DuVall, CA; Neumiller, JJ; Santiago, A; Setter, SM; Wood, L, 2009
)
0.59
" The mean dosage at week 80 was 63."( Tetrabenazine as anti-chorea therapy in Huntington disease: an open-label continuation study. Huntington Study Group/TETRA-HD Investigators.
Frank, S, 2009
)
1.8
"Repeated dosing with alpha-methyl-p-tyrosine (AMPT) at doses that significantly (-75%) depleted brain tissue dopamine levels resulted in increased (+36%) in vivo [(11)C]DTBZ binding to VMAT2 in the striatum."( In vivo [11C]dihydrotetrabenazine binding in rat striatum: sensitivity to dopamine concentrations.
Butch, ER; Desmond, T; Frey, KA; Harris, PE; Kilbourn, MR; Sherman, P, 2010
)
0.68
"This article reviews the chemistry, pharmacology, pharmacokinetics, therapeutic use, tolerability, drug-interaction potential, and dosing and administration of TBZ."( Tetrabenazine, a monoamine-depleting drug used in the treatment of hyperkinetic movement disorders.
Guay, DR, 2010
)
1.8
" It is one of very few drugs whose dosing is based, in part, on the results of genotyping (in its case, genotyping for CYP2D6 metabolizer status)."( Tetrabenazine, a monoamine-depleting drug used in the treatment of hyperkinetic movement disorders.
Guay, DR, 2010
)
1.8
" Dose-limiting adverse events, consisting mainly of sedation, parkinsonism, akathisia and depression, are usually rapidly reversible upon dosage reduction."( Tetrabenazine for the treatment of chorea and other hyperkinetic movement disorders.
Clarence-Smith, K; Jankovic, J, 2011
)
1.81
" In the 12-week trial and 80-week extension study, treatment-emergent adverse events in the tetrabenazine group mainly occurred during the dosage-titration phase, a period during which the dosage was individually optimized."( Tetrabenazine: for chorea associated with Huntington's disease.
Scott, LJ, 2011
)
2.03
"Drug-interaction experiments, supplemented by dose-response data, examined the effects of these compounds on locomotor activity, on striatal levels of dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC), and on levels of activity-regulated cytoskeleton-associated (Arc) gene expression in the striatum and frontal cortex of male Sprague-Dawley rats."( Co-administration of the Dopaminergic Stabilizer Pridopidine and Tetrabenazine in Rats.
Klamer, D; Ponten, H; Waters, N; Waters, S, 2014
)
0.64
"The chronic use and high dosing of typical neuroleptics or centrally acting dopamine receptor blocking antiemetics predispose patients to the onset of tardive syndromes."( Valbenazine granted breakthrough drug status for treating tardive dyskinesia.
Müller, T, 2015
)
0.42
" These findings are consistent with the hypothesis that the inability of memantine, AZD6765 (lanicemine) and MK-0657 to reproduce the rapid and robust antidepressant effects of ketamine in the clinic result from insufficient dosing rather than a difference in mechanism of action among these NMDAR antagonists."( Effect of NMDAR antagonists in the tetrabenazine test for antidepressants: comparison with the tail suspension test.
Czekaj, J; Kos, T; Popik, P; Skolnick, P, 2015
)
0.69
" These findings suggest that dosing regimens could be individualised and tailored for patients on the basis of dyskinesia control and tolerability."( Deutetrabenazine for treatment of involuntary movements in patients with tardive dyskinesia (AIM-TD): a double-blind, randomised, placebo-controlled, phase 3 trial.
Anderson, KE; Davis, MD; Factor, SA; Fernandez, HH; Hauser, RA; Isojärvi, J; Jarskog, LF; Jimenez-Shahed, J; Kumar, R; McEvoy, JP; Ochudlo, S; Ondo, WG; Stamler, D, 2017
)
1.08
"Deutetrabenazine administration at a dosage thought to provide comparable systemic exposure to the active metabolites of the prior, stable tetrabenazine regimen."( Safety of Converting From Tetrabenazine to Deutetrabenazine for the Treatment of Chorea.
Claassen, DO; Colcher, A; Davis, C; Duker, A; Eberly, S; Elmer, L; Frank, S; Furr-Stimming, E; Goldstein, J; Gudesblatt, M; Hunter, C; Jankovic, J; Kayson, E; Kostyk, SK; Kumar, R; Loy, C; Mallonee, W; Oakes, D; Scott, BL; Stamler, D; Sung, V; Testa, CM; Vaughan, C, 2017
)
1.38
" The safety, tolerability and pharmacokinetics of VBZ following single and repeat once-daily (QD) dosing were evaluated in 2 randomized, single-center, double-blind studies in healthy male subjects."( Single Dose and Repeat Once-Daily Dose Safety, Tolerability and Pharmacokinetics of Valbenazine in Healthy Male Subjects.
Bozigian, H; Jimenez, R; Loewen, G; Luo, R; O'Brien, CF, 2017
)
0.46
" However, valbenazine appears to have fewer side effects and a more favorable once-daily dosing regimen for the treatment of TD."( Treatment of tardive dyskinesia with tetrabenazine or valbenazine: a systematic review.
Aggarwal, S; Caroff, SN; Yonan, C, 2018
)
0.75
" The recommended starting dose of deutetrabenazine for TD is 6 mg BID, administered with food, and can be increased at weekly intervals in increments of 6 mg/day to a maximum recommended daily dosage of 24 mg BID."( Deutetrabenazine for tardive dyskinesia: A systematic review of the efficacy and safety profile for this newly approved novel medication-What is the number needed to treat, number needed to harm and likelihood to be helped or harmed?
Citrome, L, 2017
)
1.35
" In the pivotal 12-week phase III FIRST-HD trial (n = 90), deutetrabenazine, at doses titrated for optimal chorea control and tolerability (maintenance dosage range 12-48 mg/day), was significantly more effective for controlling chorea in HD patients than placebo."( Deutetrabenazine: A Review in Chorea Associated with Huntington's Disease.
Heo, YA; Scott, LJ, 2017
)
1.32
" CONCLUSIONS Once-daily dosing of valbenazine (80 mg) was effective and safe over a long period, even in this atypical case of severe and rapid-onset TD."( Successful Treatment of Severe Tardive Dyskinesia with Valbenazine, Including a Patient's Perspective.
Dietterich, TE; Filmyer, DM; Gillean, J; Josiassen, RC; Shah, SS; Shaughnessy, RA, 2017
)
0.46
" Moreover, like the other derivative of tetrabenazine, valbenazine (Ingrezza®), deutetrabenazine offers less frequent dosing and a better short-term adverse effect profile than that of tetrabenazine."( Deuterium Tetrabenazine for Tardive Dyskinesia.
Cummings, MA; Proctor, GJ; Stahl, SM, 2018
)
1.15
" The most common side effects that led to insufficient dosing and disruptions in titration were sedation and somnolence (41%), depression (24%) and anxiety (22%)."( Physician perceptions of pharmacologic treatment options for chorea associated with Huntington disease in the United States.
Abler, V; Claassen, DO; DiBonaventura, M; Gandhi, SK; Iyer, RG; Shah-Manek, B; Sung, VW, 2018
)
0.48
" Compared with tetrabenazine, deutetrabenazine and valbenazine have pharmacokinetic advantages that translate into less frequent dosing and better tolerability."( Treatment of Tardive Dyskinesia: A General Overview with Focus on the Vesicular Monoamine Transporter 2 Inhibitors.
Jankovic, J; Niemann, N, 2018
)
0.83
"Cassette dosing is also known as N-in-One dosing: several compounds are simultaneously administrated to a single animal and then the samples are rapidly detected by LC-MS/MS."( Developing a cassette microdosing approach to enhance the throughput of PET imaging agent screening.
Hong, H; Kung, HF; Liu, F; Liu, Y; Qiao, J; Sun, M; Xiao, H; Zhang, A; Zhang, S; Zhang, Y; Zhao, R; Zhu, L, 2018
)
0.48
"2%), and reaching the maximum recommended dosage despite suboptimal chorea control (11."( Tetrabenazine Treatment Patterns and Outcomes for Chorea Associated with Huntington Disease: A Retrospective Chart Review.
Abler, V; Claassen, DO; DiBonaventura, M; Iyer, RG; Shah-Manek, B; Sung, VW, 2018
)
1.92
" Tetrabenazine dosing was lower than predicted, and many patients experienced adverse symptoms of intolerability at high doses."( Tetrabenazine Treatment Patterns and Outcomes for Chorea Associated with Huntington Disease: A Retrospective Chart Review.
Abler, V; Claassen, DO; DiBonaventura, M; Iyer, RG; Shah-Manek, B; Sung, VW, 2018
)
2.83
" Pharmacokinetics, metabolism, and dosing vary significantly between the three drugs, and likely underlie the more favorable side effect profile of the newer agents (deutetrabenazine and valbenazine)."( VMAT2 Inhibitors in Neuropsychiatric Disorders.
Jimenez-Shahed, J; Tarakad, A, 2018
)
0.68
" Studying treatment of TD can be complex, as the symptoms can be affected by changes in either dosage or type of DRBA, as well as by the variable natural course of the disease."( Current treatment of tardive dyskinesia.
Fernandez, HH; Margolius, A, 2019
)
0.51
" Two pivotal clinical trials, Aim to Reduce Movements in Tardive Dyskinesia (ARM-TD) and Addressing Involuntary Movements in Tardive Dyskinesia (AIM-TD), provide evidence that deutetrabenazine dosed 24-48 mg/day effectively controlled involuntary movements according to rating scales."( Deutetrabenazine in the treatment of tardive dyskinesia.
Jimenez-Shahed, J; Niemann, N, 2019
)
1.33
" The advantages of valbenazine include once-daily dosing and a rapid onset of effect within 2 weeks of treatment initiation."( Valbenazine in the treatment of tardive dyskinesia.
Comella, C; Witek, N, 2019
)
0.51
" Dosing was initiated at 40 mg/d, with escalation to 80 mg/d at week 4 based on efficacy and tolerability."( A Phase 3, 1-Year, Open-Label Trial of Valbenazine in Adults With Tardive Dyskinesia.
Burke, J; Comella, CL; Jimenez, R; Liang, GS; Lindenmayer, JP; Marder, SR; OʼBrien, CF; Singer, C; Tanner, CM; Verghese, C,
)
0.13
" At week 4, dosing was escalated to 80 mg/day based on tolerability and clinical assessment of TD; reduction to 40 mg/day was allowed for tolerability."( A long-term, open-label study of valbenazine for tardive dyskinesia.
Burke, J; Jimenez, R; Liang, GS; Lindenmayer, JP; Marder, SR; O'Brien, CF; Siegert, S; Verghese, C, 2021
)
0.62
" One study was an open-label 2-part study in healthy volunteers; the first part included a crossover single dose of two 15 mg candidate deutetrabenazine formulations in fed and fasted states compared with tetrabenazine 25 mg in the fasted state, and the second part included single and repeated dosing of the commercial formulation of deutetrabenazine (7."( Pharmacokinetics of Deutetrabenazine and Tetrabenazine: Dose Proportionality and Food Effect.
Bradbury, M; Cox, DS; Gordon, MF; Hellriegel, E; Loupe, PS; Rabinovich-Guilatt, L; Savola, JM; Schneider, F; Stamler, D, 2021
)
1.13
"Deutetrabenazine was initiated at 12 mg/day and titrated once weekly by 6 mg/day using a response-driven dosing regimen until adequate dyskinesia control was reached or a clinically significant adverse event occurred."( Long-Term Safety and Efficacy of Deutetrabenazine in Younger and Older Patients With Tardive Dyskinesia.
Barkay, H; Chaijale, N; Finkbeiner, S; Gordon, MF; Gross, N; Sajatovic, M; Wilhelm, A, 2022
)
1.62
" Antipsychotics causing tardive dyskinesia should be reduced in dosage or should be discontinued."( [Late-Onset Dyskinesia Occurring During Antipsychotic Treatment for Schizophrenia: Treatments for Tardive Dyskinesia].
Nomoto, M, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (4)

ClassDescription
benzoquinolizineAny organic heterotricyclic compound with a skeleton consisting of a quinolizine fused to a benzene ring.
cyclic ketone
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-oneA benzoquinolizine that is 1,2,3,4,4a,9,10,10a-octahydrophenanthrene in which the carbon at position 10a is replaced by a nitrogen and which is substituted by an isobutyl group at position 2, an oxo group at position 3, and methoxy groups at positions 6 and 7.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (38)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency2.51190.631035.7641100.0000AID504339
glp-1 receptor, partialHomo sapiens (human)Potency16.90360.01846.806014.1254AID624172; AID624417
ATAD5 protein, partialHomo sapiens (human)Potency24.83440.004110.890331.5287AID493106; AID493107
GLS proteinHomo sapiens (human)Potency27.71700.35487.935539.8107AID624146; AID624170
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
importin subunit beta-1 isoform 1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
DNA polymerase betaHomo sapiens (human)Potency3.98110.022421.010289.1251AID485314
flap endonuclease 1Homo sapiens (human)Potency3.35870.133725.412989.1251AID588795
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency23.28090.00378.618923.2809AID2668
snurportin-1Homo sapiens (human)Potency112.20205.804836.130665.1308AID540263
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency25.57480.005612.367736.1254AID624032
Chain A, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency39.81070.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
TDP1 proteinHomo sapiens (human)Potency28.60660.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency10.06730.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency39.81070.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency23.91450.000221.22318,912.5098AID743035
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency28.18380.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency31.62280.001318.074339.8107AID926; AID938
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency5.95570.001022.650876.6163AID1224838
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency26.60320.001530.607315,848.9004AID1224849
pregnane X nuclear receptorHomo sapiens (human)Potency26.11820.005428.02631,258.9301AID1346982; AID1346985
GVesicular stomatitis virusPotency15.48710.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency9.77170.00108.379861.1304AID1645840
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency25.11890.001815.663839.8107AID894
mitogen-activated protein kinase 1Homo sapiens (human)Potency12.58930.039816.784239.8107AID995
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency39.81070.316212.765731.6228AID881
Interferon betaHomo sapiens (human)Potency15.48710.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.48710.01238.964839.8107AID1645842
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID881
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency17.78280.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.48710.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.48710.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.13710.00100.01460.1000AID1802430
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)Ki0.01030.00101.30096.2600AID459748; AID594597
Synaptic vesicular amine transporterHomo sapiens (human)IC50 (µMol)0.01980.01320.48594.2000AID1794817; AID1912471
Synaptic vesicular amine transporterBos taurus (cattle)Ki0.00400.00103.335010.0000AID321546
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)IC50 (µMol)0.04060.00100.01460.1000AID1770282; AID1770285
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)Ki36.40000.00101.30096.2600AID594597
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)Kd0.05670.00400.02780.0634AID1802430
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (87)

Processvia Protein(s)Taxonomy
response to amphetamineSynaptic vesicular amine transporterHomo sapiens (human)
serotonin secretion by mast cellSynaptic vesicular amine transporterHomo sapiens (human)
histamine secretion by mast cellSynaptic vesicular amine transporterHomo sapiens (human)
neurotransmitter transportSynaptic vesicular amine transporterHomo sapiens (human)
chemical synaptic transmissionSynaptic vesicular amine transporterHomo sapiens (human)
locomotory behaviorSynaptic vesicular amine transporterHomo sapiens (human)
response to toxic substanceSynaptic vesicular amine transporterHomo sapiens (human)
post-embryonic developmentSynaptic vesicular amine transporterHomo sapiens (human)
monoamine transportSynaptic vesicular amine transporterHomo sapiens (human)
dopamine transportSynaptic vesicular amine transporterHomo sapiens (human)
sequestering of neurotransmitterSynaptic vesicular amine transporterHomo sapiens (human)
serotonin uptakeSynaptic vesicular amine transporterHomo sapiens (human)
histamine uptakeSynaptic vesicular amine transporterHomo sapiens (human)
neurotransmitter loading into synaptic vesicleSynaptic vesicular amine transporterHomo sapiens (human)
somato-dendritic dopamine secretionSynaptic vesicular amine transporterHomo sapiens (human)
proton transmembrane transportSynaptic vesicular amine transporterHomo sapiens (human)
negative regulation of reactive oxygen species biosynthetic processSynaptic vesicular amine transporterHomo sapiens (human)
aminergic neurotransmitter loading into synaptic vesicleSynaptic vesicular amine transporterHomo sapiens (human)
response to potassium ionSynaptic vesicular amine transporterBos taurus (cattle)
xenobiotic transportSynaptic vesicular amine transporterBos taurus (cattle)
serotonin uptakeSynaptic vesicular amine transporterBos taurus (cattle)
dopamine uptakeSynaptic vesicular amine transporterBos taurus (cattle)
somato-dendritic dopamine secretionSynaptic vesicular amine transporterBos taurus (cattle)
proton transmembrane transportSynaptic vesicular amine transporterBos taurus (cattle)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

Processvia Protein(s)Taxonomy
protein bindingSynaptic vesicular amine transporterHomo sapiens (human)
monoamine transmembrane transporter activitySynaptic vesicular amine transporterHomo sapiens (human)
monoamine:proton antiporter activitySynaptic vesicular amine transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySynaptic vesicular amine transporterHomo sapiens (human)
monoamine:proton antiporter activitySynaptic vesicular amine transporterBos taurus (cattle)
xenobiotic transmembrane transporter activitySynaptic vesicular amine transporterBos taurus (cattle)
organic cyclic compound bindingSynaptic vesicular amine transporterBos taurus (cattle)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (36)

Processvia Protein(s)Taxonomy
centrosomeSynaptic vesicular amine transporterHomo sapiens (human)
plasma membraneSynaptic vesicular amine transporterHomo sapiens (human)
synaptic vesicleSynaptic vesicular amine transporterHomo sapiens (human)
membraneSynaptic vesicular amine transporterHomo sapiens (human)
axonSynaptic vesicular amine transporterHomo sapiens (human)
dendriteSynaptic vesicular amine transporterHomo sapiens (human)
secretory granule membraneSynaptic vesicular amine transporterHomo sapiens (human)
synaptic vesicle membraneSynaptic vesicular amine transporterHomo sapiens (human)
intracellular membrane-bounded organelleSynaptic vesicular amine transporterHomo sapiens (human)
clathrin-sculpted monoamine transport vesicle membraneSynaptic vesicular amine transporterHomo sapiens (human)
dopaminergic synapseSynaptic vesicular amine transporterHomo sapiens (human)
terminal boutonSynaptic vesicular amine transporterHomo sapiens (human)
synaptic vesicle membraneSynaptic vesicular amine transporterHomo sapiens (human)
axonSynaptic vesicular amine transporterBos taurus (cattle)
dendriteSynaptic vesicular amine transporterBos taurus (cattle)
secretory granule membraneSynaptic vesicular amine transporterBos taurus (cattle)
synaptic vesicle membraneSynaptic vesicular amine transporterBos taurus (cattle)
chromaffin granuleSynaptic vesicular amine transporterBos taurus (cattle)
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (132)

Assay IDTitleYearJournalArticle
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347153Confirmatory screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347168HepG2 cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347167Vero cells viability qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347152Confirmatory screen NINDS AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347149Furin counterscreen qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1802430[3H]TBZOH Binding Assay from Article 10.1074/jbc.M113.502971: \\Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine.\\2013The Journal of biological chemistry, Nov-08, Volume: 288, Issue:45
Identification of conformationally sensitive residues essential for inhibition of vesicular monoamine transport by the noncompetitive inhibitor tetrabenazine.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1345057Human Vesicular monoamine transporter 2 (SLC18 family of vesicular amine transporters)1996Proceedings of the National Academy of Sciences of the United States of America, May-14, Volume: 93, Issue:10
Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter.
AID1345075Human Vesicular monoamine transporter 1 (SLC18 family of vesicular amine transporters)1996Proceedings of the National Academy of Sciences of the United States of America, May-14, Volume: 93, Issue:10
Distinct pharmacological properties and distribution in neurons and endocrine cells of two isoforms of the human vesicular monoamine transporter.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID594597Displacement of [3H]DHTBZ from Sprague-Dawley rat striatum VMAT2 after 1 hr by liquid scintillation counting2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors.
AID440783Inhibition of [3H]dopamine uptake at VMAT2 in rat brain synaptic vesicle by liquid scintillation spectroscopy2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2).
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID459748Displacement of [3H]MTBZ from VMAT2 in rat whole brain vesicles by liquid scintillation spectrophotometry2010Bioorganic & medicinal chemistry, Jan-15, Volume: 18, Issue:2
Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.
AID118793Retention for passive avoidance learning in mice at dose 5 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID440784Ratio of Ki for displacement of [3H]DTBZ from VMAT2 dihydrotetrabenazine binding site in rat brain synaptic vesicle to Ki for inhibition of [3H]dopamine uptake at VMAT2 in rat brain synaptic vesicle2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2).
AID321546Inhibition of dopamine uptake at VMAT in bovine chromaffin granule ghosts2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Vesicular monoamine transporter substrate/inhibitor activity of MPTP/MPP+ derivatives: a structure-activity study.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID205269Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID440782Displacement of [3H]DTBZ from VMAT2 dihydrotetrabenazine binding site in rat brain synaptic vesicle by scintillation counting2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Pyrrolidine analogues of lobelane: relationship of affinity for the dihydrotetrabenazine binding site with function of the vesicular monoamine transporter 2 (VMAT2).
AID387243Toxicity in Lewis rat assessed as tonic seizure at 2 mg/kg2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Novel hypoglycemic dihydropyridones serendipitously discovered from O- versus C-alkylation in the synthesis of VMAT2 antagonists.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID118789Retention for passive avoidance learning in mice at dose 2.5 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID118787Retention for passive avoidance learning in mice at dose 1.25 mg/kg1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Cognition-activating properties of 3-(Aryloxy)pyridines.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1770280Metabolic stability in mouse liver microsomes assessed as intrinsic clearance at 1 uM in the presence of NADPH measured for 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID594597Displacement of [3H]DHTBZ from Sprague-Dawley rat striatum VMAT2 after 1 hr by liquid scintillation counting2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Preparation and evaluation of tetrabenazine enantiomers and all eight stereoisomers of dihydrotetrabenazine as VMAT2 inhibitors.
AID1770279Metabolic stability in monkey liver microsomes assessed as intrinsic clearance at 1 uM in the presence of NADPH measured for 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770276Metabolic stability in monkey liver microsomes assessed as parent compound remaining at 1 uM in the presence of NADPH measured after 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770278Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM in the presence of NADPH measured after 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770286Metabolic stability in human liver microsomes assessed as half life at 1 uM in the presence of NADPH measured for 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770282Inhibition of [3H]DTBZ binding to VMAT2 in rat brain incubated for 30 mins by liquid scintillation spectrometry analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770281Metabolic stability in human liver microsomes assessed as intrinsic clearance at 1 uM in the presence of NADPH measured for 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770285Inhibition of [3H]DA uptake at VMAT2 in rat striatal synaptosome incubated for 10 mins followed by [3H]DA addition and measured after 20 mins by TopCount scintillation counting method2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770288Metabolic stability in monkey liver microsomes assessed as half life at 1 uM in the presence of NADPH measured for 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770287Metabolic stability in mouse liver microsomes assessed as half life at 1 uM in the presence of NADPH measured for 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1770277Metabolic stability in mouse liver microsomes assessed as parent compound remaining at 1 uM in the presence of NADPH measured after 60 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthesis and analysis of dihydrotetrabenazine derivatives as novel vesicular monoamine transporter 2 inhibitors.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,293)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990607 (46.95)18.7374
1990's135 (10.44)18.2507
2000's144 (11.14)29.6817
2010's317 (24.52)24.3611
2020's90 (6.96)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 82.05

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index82.05 (24.57)
Research Supply Index7.27 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index148.07 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (82.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials71 (5.22%)5.53%
Trials0 (0.00%)5.53%
Reviews116 (8.53%)6.00%
Reviews0 (0.00%)6.00%
Case Studies95 (6.99%)4.05%
Case Studies0 (0.00%)4.05%
Observational2 (0.15%)0.25%
Observational0 (0.00%)0.25%
Other1,076 (79.12%)84.16%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (17)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open Label, Balanced, Randomized, Two-treatment, Four-period, Two-sequence, Single Dose, Crossover, Fully Replicated Oral Bioequivalence Study of Tetrabenazine Tablets 25 mg of Dr. Reddy's Laboratories Limited, India Comparing With XENAZINE® (Tetrabena [NCT03702855]Phase 148 participants (Actual)Interventional2015-12-31Completed
Compassionate Use of Tetrabenazine in the Treatment of Hyperkinesias [NCT00642057]0 participants Expanded AccessNo longer available
An Open Label, Balanced, Randomized, Two-treatment, Four-period, Two-sequence, Single Dose, Crossover, Fully Replicated Oral Bioequivalence Study of Tetrabenazine Tablets 25 mg of Dr. Reddy's Laboratories Limited, India Comparing With XENAZINE® (Tetrabena [NCT03696329]Phase 148 participants (Actual)Interventional2015-10-31Completed
A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Tetrabenazine MR in Subjects Aged 5 up to 17 Years With Tourette's Syndrome [NCT01133353]Phase 20 participants (Actual)Interventional2011-03-31Withdrawn
Neuroleptic and Huntington Disease. Comparison of : Olanzapine, la Tetrabenazine and Tiapride. A Multicentric, Randomised, Controlled Study. [NCT00632645]Phase 3180 participants (Actual)Interventional2009-04-30Completed
Non-randomized Control Clinical Trial to Evaluate the Efficacy and Safety of Symptomatic Drug Therapy for Mild to Moderate Huntington's Disease Patients [NCT04071639]Phase 160 participants (Anticipated)Interventional2020-03-12Recruiting
Atypical Antipsychotics and Hyperglycemic Emergencies: Multicentre, Retrospective Cohort Study of Administrative Data [NCT02582736]725,489 participants (Actual)Observational2012-04-30Completed
Efficacy of Deutetrabenazine in Huntington's Disease Patients With Dysphagia: A Randomised, Placebo-controlled Pilot Study [NCT04301726]Phase 148 participants (Anticipated)Interventional2020-09-01Not yet recruiting
Effect of Tetrabenazine on Stroop Interference in Huntington Disease [NCT01834911]Phase 42 participants (Actual)Interventional2013-03-31Completed
A Randomized, Double-Blind, Placebo-Controlled Study of Tetrabenazine for the Treatment of Huntington's Chorea [NCT00219804]Phase 30 participants InterventionalCompleted
Study of Efficacy and Acceptability of Tetrabenazine in the Late Dyskinetic Syndrome With Neuroleptics: A Randomized, Parallel Group, Double-blind Placebo Controlled Multicentre Trial [NCT01543321]Phase 354 participants (Actual)Interventional2012-05-14Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled Study to Assess the Efficacy and Safety of NBI-98854 for the Treatment of Tardive Dyskinesia in Subjects With Schizophrenia or Schizoaffective Disorder [NCT01688037]Phase 2109 participants (Actual)Interventional2012-09-30Completed
A Pilot Study Assessing Impulsivity in Patients With Huntington's Disease on Xenazine (Tetrabenazine) [NCT02509793]Phase 420 participants (Anticipated)Interventional2018-08-01Recruiting
Augmentation of Antipsychotic Partial Responders With Tetrabenazine [NCT00362804]41 participants (Actual)Interventional2002-02-28Completed
Excessive Crying in Children With Cerebral Palsy and Communication Deficits -a Fixed-sequence, Crossover Clinical Trial [NCT04523935]Phase 4131 participants (Actual)Interventional2005-12-07Completed
A Phase 2, Double-Blind, Randomized, Placebo-Controlled, Two-Period Cross-Over Study to Evaluate the Efficacy and Safety of NBI-98854 for the Treatment of Tardive Dyskinesia in Subjects With Schizophrenia or Schizoaffective Disorder [NCT01393600]Phase 237 participants (Actual)Interventional2011-08-31Completed
A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Dose-Titration Study to Assess the Safety, Tolerability, and Efficacy of NBI-98854 for the Treatment of Tardive Dyskinesia [NCT01733121]Phase 2102 participants (Actual)Interventional2012-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01393600 (3) [back to overview]Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score
NCT01393600 (3) [back to overview]Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score for Combined NBI-98854 Dose Groups (Excluding 1 Site)
NCT01393600 (3) [back to overview]Clinical Global Impression - Global Improvement of TD (CGI-TD)
NCT01688037 (3) [back to overview]Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score Change From Baseline at Week 6
NCT01688037 (3) [back to overview]Clinical Global Impression - Global Improvement of TD (CGI-TD)
NCT01688037 (3) [back to overview]Clinical Global Impression - Global Improvement of TD (CGI-TD) at Week 2
NCT01733121 (3) [back to overview]Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score Change From Baseline at Week 6
NCT01733121 (3) [back to overview]AIMS Dyskinesia Total Score Change From Baseline at Week 6
NCT01733121 (3) [back to overview]Clinical Global Impression - Global Improvement of TD (CGI-TD) at Week 6

Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score

Severity of TD symptoms assessed by AIMS dyskinesia total score (sum of items 1 through 7), as assessed by blinded central AIMS video raters. The AIMS Total Dyskinesia Score rates a total of 7 items, rating involuntary movement from 0 (no dyskinesia) to 4 (severe dyskinesia). Items 1 through 7 include facial and oral movements (Items 1-4), extremity movements (Items 5-6), and trunk movements (Item 7). The AIMS dyskinesia total score for Items 1-7 ranges from 0 to 28; a higher score reflects increased severity. (NCT01393600)
Timeframe: Day 15 and 29, averaged

Interventionunits on a scale (Least Squares Mean)
Placebo9.9
Valbenazine 12.5 mg9.1
Valbenazine 50 mg8.8

[back to top]

Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score for Combined NBI-98854 Dose Groups (Excluding 1 Site)

Severity of TD symptoms assessed by AIMS dyskinesia total score (sum of items 1 through 7), as assessed by blinded central AIMS video raters. The AIMS Total Dyskinesia Score rates a total of 7 items, rating involuntary movement from 0 (no dyskinesia) to 4 (severe dyskinesia). Items 1 through 7 include facial and oral movements (Items 1-4), extremity movements (Items 5-6), and trunk movements (Item 7). The AIMS dyskinesia total score for Items 1-7 ranges from 0 to 28; a higher score reflects increased severity. (NCT01393600)
Timeframe: Day 15 and 29, averaged

Interventionunits on a scale (Least Squares Mean)
Placebo10.3
Valbenazine 12.5 mg9.9
Valbenazine 50 mg6.1

[back to top]

Clinical Global Impression - Global Improvement of TD (CGI-TD)

Clinician's perspective of the participant's overall improvement of TD symptoms over time. The CGI-TD is based on a 7-point scale (range: 1=very much improved to 7=very much worse). (NCT01393600)
Timeframe: Day 15 and 29, averaged

Interventionunits on a scale (Mean)
Valbenazine 12.5mg Placebo2.2
Valbenazine 12.5mg2.2
Valbenazine 50mg Placebo3.2
Valbenazine 50mg2.6

[back to top]

Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score Change From Baseline at Week 6

The AIMS Total Dyskinesia Score rates a total of 7 items, rating involuntary movement from 0 (no dyskinesia) to 4 (severe dyskinesia). Items 1 through 7 include facial and oral movements (Items 1-4), extremity movements (Items 5-6), and trunk movements (Item 7). The AIMS dyskinesia total score for Items 1-7 ranges from 0 to 28; a higher score reflects increased severity. The primary efficacy endpoint was the change from baseline in the AIMS dyskinesia total score at Week 6 between the pooled NBI-98854 50+100 mg group and placebo group analyzed using the ANCOVA model (LOCF, ITT analysis set). (NCT01688037)
Timeframe: Baseline and Week 6

Interventionunits on a scale (Least Squares Mean)
Placebo-2.5
All Valbenazine-3.3

[back to top]

Clinical Global Impression - Global Improvement of TD (CGI-TD)

Clinician's perspective of the participant's overall improvement of TD symptoms over time. The CGI-TD is based on a 7-point scale (range: 1=very much improved to 7=very much worse). The ANOVA analysis of CGI-TD was conducted for the pooled NBI-98854 50+100 mg group and placebo group. (NCT01688037)
Timeframe: Week 6

Interventionunits on a scale (Least Squares Mean)
Placebo3.2
Valbenazine 50mg and Valbenazine 100mg Then 50mg3.3

[back to top]

Clinical Global Impression - Global Improvement of TD (CGI-TD) at Week 2

Clinician's perspective of the participant's overall improvement of TD symptoms over time. The CGI-TD is based on a 7-point scale (range: 1=very much improved to 7=very much worse). (NCT01688037)
Timeframe: Week 2

Interventionunits on a scale (Least Squares Mean)
Placebo3.6
Valbenazine 50mg3.3
Valbenazine 100mg3.2

[back to top]

Abnormal Involuntary Movement Scale (AIMS) Dyskinesia Total Score Change From Baseline at Week 6

The AIMS Total Dyskinesia Score rates a total of 7 items, rating involuntary movement from 0 (no dyskinesia) to 4 (severe dyskinesia). Items 1 through 7 include facial and oral movements (Items 1-4), extremity movements (Items 5-6), and trunk movements (Item 7). The AIMS dyskinesia total score for Items 1-7 ranges from 0 to 28; a higher score reflects increased severity. (NCT01733121)
Timeframe: Baseline and Week 6

Interventionunits on a scale (Least Squares Mean)
Placebo-0.3
Valbenazine-3.4

[back to top]

AIMS Dyskinesia Total Score Change From Baseline at Week 6

The AIMS Total Dyskinesia Score rates a total of 7 items, rating involuntary movement from 0 (no dyskinesia) to 4 (severe dyskinesia). Items 1 through 7 include facial and oral movements (Items 1-4), extremity movements (Items 5-6), and trunk movements (Item 7). The AIMS dyskinesia total score for Items 1-7 ranges from 0 to 28; a higher score reflects increased severity. (NCT01733121)
Timeframe: Week 6

Interventionunits on a scale (Least Squares Mean)
Placebo-0.2
NBI-98854-2.6

[back to top]

Clinical Global Impression - Global Improvement of TD (CGI-TD) at Week 6

Clinician's perspective of the participant's overall improvement of TD symptoms over time. The CGI-TD is based on a 7-point scale (range: 1=very much improved to 7=very much worse). (NCT01733121)
Timeframe: Week 6

Interventionunits on a scale (Least Squares Mean)
Placebo3.1
Valbenazine2.2

[back to top]