Page last updated: 2024-12-04

cyclobenzaprine

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Description

cyclobenzaprine: RN given refers to parent cpd; Lisseril is synonymous for HCl; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cyclobenzaprine : 5-Methylidene-5H-dibenzo[a,d]cycloheptene in which one of the hydrogens of the methylidene group is substituted by a 2-(dimethylamino)ethyl group. A centrally acting skeletal muscle relaxant, it is used as its hydrochloride salt in the symptomatic treatment of painful muscle spasm. [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]

punicic acid: a conjugated linolenic acid [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

(9Z,11E,13Z)-octadecatrienoic acid : A 9,11,13-octadecatrienoic acid having its double bonds in cis, trans and cis configurations, respectively. It has been isolated from pomegranate (Punica granatum). [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 CID2895
CHEMBL ID669
CHEBI ID3996
SCHEMBL ID38527
MeSH IDM0045849
PubMed CID5281126
CHEMBL ID5205249
CHEBI ID8638
SCHEMBL ID158967
MeSH IDM0045849

Synonyms (177)

Synonym
BIDD:GT0485
BIDD:PXR0152
BRD-K42348709-003-05-7
5h-dibenzo(a,d)cycloheptene-.delta.5,.gamma.-propylamine, n,n-dimethyl-
1-propanamine, 3-(5h-dibenzo[a,d]cyclohepten-5-ylidene)-n,n-dimethyl-
3-(dibenzo[[?],[?]][7]annulen-11-ylidene)-n,n-dimethyl-propan-1-amine
lisseril
KBIO1_000047
DIVK1C_000047
NCI60_041725
ciclobenzaprina [inn-spanish]
n,n-dimethyl-3-(dibenzo(a,d)cycloheptene-4-ylidene)propylamine
cyclobenzaprinum [inn-latin]
proeptatriene [italian]
5-(3-dimetilaminopropiliden)-5h-dibenzo-(a,d)-ciclopentene [italian]
5h-dibenzo(a,d)cycloheptene-delta(sup 5),gamma-propylamine, n,n-dimethyl-
einecs 206-145-8
n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-delta(sup 5),gamma-propylamine
ro 4-1577
9715 r.p
mk 130
1-propanamine, 3-(5h-dibenzo(a,d)cyclohepten-5-ylidene)-n,n-dimethyl-
cyclobenzaprine [inn]
10,11-dehydroamitriptyline
proheptatriene
proheptatrien
SPECTRUM_001535
PRESTWICK2_000445
3-(5h-dibenzo[a,d]cyclohepten-5-ylidene)-n,n-dimethyl-1-propanamine
lopac-c-4542
NCGC00013841-03
NCGC00013841-02
OPREA1_534683
D07758
cyclobenzaprine (inn)
NCGC00013841
QTL1_000027
BPBIO1_000540
SPECTRUM5_001259
BSPBIO_000490
BSPBIO_003072
IDI1_000047
AB00514668
303-53-7
cyclobenzaprine
C06931
(3-dibenzo[a,d]cyclohepten-5-ylidene-propyl)-dimethyl-amine
DB00924
n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-delta5,gamma-propylamine
PRESTWICK3_000445
LOPAC0_000303
NCI78206 ,
KBIOSS_002015
KBIOGR_000643
KBIO2_002015
KBIO2_007151
KBIO3_002572
KBIO2_004583
SPECTRUM2_001534
PRESTWICK1_000445
PRESTWICK0_000445
NINDS_000047
SPBIO_001348
SPBIO_002429
NCISTRUC2_001486
NCISTRUC1_001572
SPECTRUM4_000162
SPECTRUM3_001566
NCGC00096951-01
NCGC00162122-01
NCGC00013841-06
mk-130 (as the base)
CHEMBL669
mk-130
L001021
3-(5h-dibenzo[a,d][7]annulen-5-ylidene)-n,n-dimethylpropan-1-amine
ciclobenzaprina
CHEBI:3996 ,
3-(5h-dibenzo[a,d]cyclohepten-5-ylidene)-n,n-dimethylpropan-1-amine
n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-delta(5,gamma)-propylamine
cyclobenzaprinum
proeptatriene
fexmid
hsdb 8305
unii-69o5wqq5ti
5-(3-dimetilaminopropiliden)-5h-dibenzo-(a,d)-ciclopentene
9715 r.p.
69o5wqq5ti ,
CCG-36511
NCGC00013841-05
NCGC00013841-04
dimethyl({3-[(2e)-tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-2-ylidene]propyl})amine
FT-0603167
NCGC00013841-08
bdbm112774
us8629135, sw-01
gtpl7152
3-(dibenzo[1,2-a:1',2'-e][7]annulen-11-ylidene)-n,n-dimethylpropan-1-amine
cyclobenzaprine [who-dd]
amitriptyline hydrochloride impurity b [ep impurity]
cyclobenzaprine [usp impurity]
3-(5h-dibenzo(a,d)(7)annulen-5-ylidene)-n,n-dimethylpropan-1-amine
cyclobenzaprine [vandf]
nortriptyline hydrochloride impurity e [ep impurity]
cyclobenzaprine [mi]
n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-(sup .delta.5,.gamma.)-propylamine
SCHEMBL38527
5-(3-dimethylaminopropylidene)- 5h-dibenzo[a,d]cycloheptene
5-(3-dimethylaminopropylidene)-5h-dibenzo[a,d]cycloheptene
cyclobenzaprine hydrochloride (salt/mix)
cycloflex (salt/mix)
flexeril (salt/mix)
amrix (salt/mix)
rp 9715
3-(5h-dibenzo[a,d]cyclohepten-5-ylidene)-n,n-dimethyl-1-propanamine #
n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-.delta.5,.gamma.-propylamine
AKOS025255657
DTXSID0046933 ,
BBL035415
STL416209
AB00053651_07
MRF-0000742
SBI-0050291.P003
n,n-dimethyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenylidene)propan-1-amine
Q5198674
BRD-K42348709-003-08-1
SDCCGSBI-0050291.P005
NCGC00013841-19
EN300-708806
dimethyl(3-{tricyclo[9.4.0.0,3,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-2-ylidene}propyl)amine
dtxcid8026933
(3-dibenzo(a,d)cyclohepten-5-ylidene-propyl)-dimethyl-amine
ciclobenzaprina (inn-spanish)
cyclobenzaprine (usp impurity)
3-(5h-dibenzo(a,d)cyclohepten-5-ylidene)-n,n-dimethylpropan-1-amine
cyclobenzaprinum (latin)
m03bx08
cyclobenzaprinum (inn-latin)
n,n-dimethyl-5h-dibenzo(a,d)cycloheptene-(sup delta5,gamma)-propylamine
9,11,13-octadecatrienoic acid, (9z,11e,13z)-
(z,e,z)-octadeca-9,11,13-trienoic acid
octadeca-9c,11t,13c-triensaeure
9cis,11trans,13cis-octadecatrienoic acid
(9z,11e,13z)-octadecatrienoic acid
CHEBI:8638 ,
(9z,11e,13z)-octadeca-9,11,13-trienoic acid
c18:3 n-5 cis, 7 trans, 9 cis
9c,11t,13c-18:3
octadeca-9c,11t,13c-trienoic acid
9c,11t,13c-linolenic acid
9-cis,11-trans,13-cis-octadecatrienoic acid
cis-9,trans-11,cis-13-octadecatrienoic acid
trichosanic acid
punicic acid
C08364
544-72-9
9z,11e,13z-octadecatrienoic acid
cis-9, trans-11, cis-13-octadecatrienoic acid
LMFA01030146
trichosanoic acid
unii-vfq03h211o
cis,trans,cis-9,11,13-octadecatrienoic acid
9z,11e,13z-octadeca-9,11,13-trienoic acid
9,11,13-octadecatrienoic acid, (z,z,e)-
vfq03h211o ,
SCHEMBL158967
9(z),11(e),13(z)-octadecatrienoic acid
cis,trans,cis-octadeca-9,11,13-trienoic acid
fatty acid 18:3 n-5
dtxcid801326803
DTXSID10897463 ,
CUXYLFPMQMFGPL-BGDVVUGTSA-N
Q201502
CS-0179308
HY-139066
PD088520
CHEMBL5205249

Research Excerpts

Overview

Cyclobenzaprine (CBP) is a tricyclic structurally related to the antidepressant amitriptyline. It is used clinically to decrease muscle spasm and hypercontractility, as well as acute musculoskeletal pain.

ExcerptReferenceRelevance
"Cyclobenzaprine is a tricyclic dimethylpropanamine skeletal muscle relaxant, which is used clinically to decrease muscle spasm and hypercontractility, as well as acute musculoskeletal pain. "( The Skeletal Muscle Relaxer Cyclobenzaprine Is a Potent Non-Competitive Antagonist of Histamine H1 Receptors.
Cheshmehkani, A; Karmokar, PF; Moniri, NH; Senatorov, IS; Singh, K, 2022
)
2.46
"Cyclobenzaprine is a muscle relaxant indicated for acute pain. "( Maternal cyclobenzaprine exposure and risk of birth defects in the National Birth Defects Prevention Study (1997-2011) and Birth Defects Study to Evaluate Pregnancy exposureS (2014-2018).
Ailes, EC; Browne, ML; Fisher, SC; Howley, MM; Nembhard, WN; Papadopoulos, EA; Tran, EL, 2023
)
2.77
"Cyclobenzaprine is a skeletal muscle relaxant primarily used in the treatment of pain. "( Transfer of Cyclobenzaprine into Human Milk and Subsequent Infant Exposure.
Baker, T; Burra, B; Datta, P; Hale, TW; Rewers-Felkins, K, 2019
)
2.34
"Cyclobenzaprine (CBP) is a tricyclic structurally related to the antidepressant amitriptyline, differing only by the presence of a double bond in the central ring."( Cyclobenzaprine Raises ROS Levels in Leishmania infantum and Reduces Parasite Burden in Infected Mice.
Abengózar, MA; Almeida-Amaral, EE; Andrade-Neto, VV; Barbas, C; Cunha-Júnior, EF; da Costa-Silva, TA; Galisteo Junior, AJ; Lima, ML; Rivas, L; Tempone, AG; Torres-Santos, EC, 2017
)
2.62
"Cyclobenzaprine is a muscle relaxant; however, its mechanism of action is unclear."( Treatment of levator ani syndrome with cyclobenzaprine.
Kunka, CA; Ota, KS; Sheikh, M, 2012
)
1.37
"Cyclobenzaprine hydrochloride is a muscle relaxant that is effective in improving muscle spasm, reducing local pain and tenderness, and increasing range of motion in acute, painful musculoskeletal conditions. "( Efficacy of a low-dose regimen of cyclobenzaprine hydrochloride in acute skeletal muscle spasm: results of two placebo-controlled trials.
Borenstein, DG; Korn, S, 2003
)
2.04
"Cyclobenzaprine (Flexeril) is a muscle relaxant, possessing a tricyclic structure. "( Identification of human liver cytochrome P450 isoforms involved in the in vitro metabolism of cyclobenzaprine.
Cheng, H; Liu, L; Wang, RW, 1996
)
1.96

Effects

Cyclobenzaprine hydrochloride has the most recent and largest clinical trials demonstrating its benefit. Carisoprodol and metaxalone also appear to be effective.

ExcerptReferenceRelevance
"Cyclobenzaprine (CBP) has a cyclic structure similar to amitriptyline. "( Five-year multicenter retrospective review of cyclobenzaprine toxicity.
Borys, DJ; Krenzelok, EP; Mann, KV; Muir, S; Spiller, HA; Winter, ML,
)
1.83
"Cyclobenzaprine has potential for sodium channel blockade and ventricular dysrhythmias although cardiac toxicity due to cyclobenzaprine alone is rare."( Cardiac sodium channel blockade after an intentional ingestion of lacosamide, cyclobenzaprine, and levetiracetam: Case report.
Cao, D; Chua-Tuan, JL; Hoyte, CO; Iwanicki, JL, 2015
)
1.37
"Cyclobenzaprine has been commonly compounded by pharmacists into topically applied dosage forms for the treatment of pain disorders. "( Skin Permeation and Antinociception of Compounded Topical Cyclobenzaprine Hydrochloride Formulations.
Arnold, J; Asbill, S; Bryson, E; Gorman, G; Hartman, R; Sweitzer, S,
)
1.82
"Cyclobenzaprine hydrochloride has the most recent and largest clinical trials demonstrating its benefit, but carisoprodol and metaxalone also appear to be effective."( Commonly used muscle relaxant therapies for acute low back pain: a review of carisoprodol, cyclobenzaprine hydrochloride, and metaxalone.
Toth, PP; Urtis, J, 2004
)
1.27
"Cyclobenzaprine (CBP) has a cyclic structure similar to amitriptyline. "( Five-year multicenter retrospective review of cyclobenzaprine toxicity.
Borys, DJ; Krenzelok, EP; Mann, KV; Muir, S; Spiller, HA; Winter, ML,
)
1.83

Treatment

Cyclobenzaprine-treated patients were 3 times as likely to report overall improvement and to report moderate reductions in individual symptoms, particularly sleep. Treatment with cyclobenzabrine alone had no effect on the ability of gaps to suppress the startle response.

ExcerptReferenceRelevance
"Cyclobenzaprine effectively treated our patient's LAS. "( Treatment of levator ani syndrome with cyclobenzaprine.
Kunka, CA; Ota, KS; Sheikh, M, 2012
)
2.09
"Cyclobenzaprine-treated patients were 3 times as likely to report overall improvement and to report moderate reductions in individual symptoms, particularly sleep."( Treatment of fibromyalgia with cyclobenzaprine: A meta-analysis.
Jackson, JL; O'Malley, PG; Tofferi, JK, 2004
)
2.05
"Treatment with cyclobenzaprine alone had no effect on the ability of gaps to suppress the startle response."( Partial to complete suppression of unilateral noise-induced tinnitus in rats after cyclobenzaprine treatment.
Blair, C; Le Prell, C; Lobarinas, E; Spankovich, C, 2015
)
0.98

Toxicity

ExcerptReferenceRelevance
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Given its tricyclic properties, serotonin syndrome is a potential side effect of this drug."( Neuropsychiatric side effects of cyclobenzaprine.
Sederholm, B; Shprecher, D; Sloan, CT, 2013
)
0.67
" Safety was assessed by adverse event (AE) reporting."( Efficacy and Safety of Sublingual Cyclobenzaprine for the Treatment of Fibromyalgia: Results From a Randomized, Double-Blind, Placebo-Controlled Trial.
Arnold, LM; Kelley, M; Lederman, S; Sullivan, GM; Vaughn, B, 2023
)
1.19
"In this phase III, randomized, controlled trial of patients with FM, treatment with TNX-102 SL was associated with significant reductions in daily pain and was safe and well tolerated."( Efficacy and Safety of Sublingual Cyclobenzaprine for the Treatment of Fibromyalgia: Results From a Randomized, Double-Blind, Placebo-Controlled Trial.
Arnold, LM; Kelley, M; Lederman, S; Sullivan, GM; Vaughn, B, 2023
)
1.19
"The use of physiologically based biopharmaceutics modeling (PBBM) and bioequivalence safe space is increasingly common for immediate-release drug products."( Development of Extended-Release Formulations Containing Cyclobenzaprine Based on Physiologically Based Biopharmaceutics Modeling and Bioequivalence Safe Space.
Duque, MD; Ferraz, HG; Issa, MG; Miranda Dos Santos, E, 2023
)
1.16

Pharmacokinetics

A review focuses on the pharmacokinetic profile of a new formulation, cyclobenzaprine extended-release (CER) CER delivers a sustained plasma cyclobensaprine concentration over 24 h, allowing once-daily dosing.

ExcerptReferenceRelevance
" There was about a fourfold accumulation of the drug in plasma on multiple dosing, corresponding to an effective half-life of 18 hours."( Cyclobenzaprine pharmacokinetics, including the effects of age, gender, and hepatic insufficiency.
Chavez-Eng, CM; Constanzer, ML; King, JD; Korn, SH; Winchell, GA, 2002
)
1.76
" Pharmacokinetic parameters were monitored through 168 hours after the last dose in each dose period; adverse events (AEs) were monitored during the study through 3 weeks after the last dose of study drug."( Single-dose pharmacokinetics of once-daily cyclobenzaprine extended release 30 mg versus cyclobenzaprine immediate release 10 mg three times daily in healthy young adults : a randomized, open-label, two-period crossover, single-centre study.
Darwish, M; Hellriegel, ET; Xie, F, 2008
)
0.61
" CER exhibited a consistent concentration-time profile with a single peak, in contrast to the pharmacokinetic profile for CIR, which displayed multiple peaks and troughs over the 24-hour period."( Single-dose pharmacokinetics of once-daily cyclobenzaprine extended release 30 mg versus cyclobenzaprine immediate release 10 mg three times daily in healthy young adults : a randomized, open-label, two-period crossover, single-centre study.
Darwish, M; Hellriegel, ET; Xie, F, 2008
)
0.61
"The pharmacokinetic profile of once-daily CER reflected the mode of administration, providing a controlled release of cyclobenzaprine with sustained plasma concentrations, in contrast to the fluctuating profile of CIR."( Single-dose pharmacokinetics of once-daily cyclobenzaprine extended release 30 mg versus cyclobenzaprine immediate release 10 mg three times daily in healthy young adults : a randomized, open-label, two-period crossover, single-centre study.
Darwish, M; Hellriegel, ET; Xie, F, 2008
)
0.82
" Outcome measures included area under the plasma cyclobenzaprine concentration versus time curve (AUC) to 168 hours (AUC168) and infinity (AUC infinity), peak plasma cyclobenzaprine concentration (Cmax), time to observed Cmax (tmax) and terminal elimination half-life of cyclobenzaprine."( Comparison of the single-dose pharmacokinetics of once-daily cyclobenzaprine extended-release 30 mg and cyclobenzaprine immediate-release 10 mg three times daily in the elderly: a randomized, open-label, crossover study.
Darwish, M; Xie, F, 2009
)
0.85
" Pharmacokinetic measures included area under the plasma cyclobenzaprine concentration versus time curve to 168 hours (AUC(168)) and infinity (AUC(infinity)), maximum plasma cyclobenzaprine concentration (C(max)), time to observed C(max) (t(max)), terminal elimination half-life (t(1/2beta)), and absorption lag time (t(lag))."( Effect of food on the pharmacokinetics of once-daily cyclobenzaprine extended-release 30 mg: a randomized, open-label, crossover, single-centre study.
Darwish, M; Xie, F, 2009
)
0.85
" The shapes of the pharmacokinetic profiles for CER 15 and 30 mg were parallel."( A pharmacokinetic comparison of single doses of once-daily cyclobenzaprine extended-release 15 mg and 30 mg: a randomized, double-blind, two-period crossover study in healthy volunteers.
Chang, S; Darwish, M; Hellriegel, ET, 2009
)
0.6
"Once-daily CER 15 and 30 mg exhibited similarly shaped pharmacokinetic profiles."( A pharmacokinetic comparison of single doses of once-daily cyclobenzaprine extended-release 15 mg and 30 mg: a randomized, double-blind, two-period crossover study in healthy volunteers.
Chang, S; Darwish, M; Hellriegel, ET, 2009
)
0.6
" This review focuses on the pharmacokinetic profile of a new formulation, cyclobenzaprine extended-release (CER), which delivers a sustained plasma cyclobenzaprine concentration over 24 h, allowing once-daily dosing."( Pharmacokinetic profile of once-daily cyclobenzaprine extended-release.
Darwish, M; Hellriegel, ET, 2010
)
0.86
"Results from CER pharmacokinetic studies conducted through August 2010 are summarized."( Pharmacokinetic profile of once-daily cyclobenzaprine extended-release.
Darwish, M; Hellriegel, ET, 2010
)
0.63
"This review provides information on the first four studies assessing the single-dose and steady-state pharmacokinetic profile of CER."( Pharmacokinetic profile of once-daily cyclobenzaprine extended-release.
Darwish, M; Hellriegel, ET, 2010
)
0.63
"Once-daily CER 30 mg and three-times-daily CIR 10 mg produced comparable systemic exposures to cyclobenzaprine, but pharmacokinetic profiles were qualitatively different."( Pharmacokinetic profile of once-daily cyclobenzaprine extended-release.
Darwish, M; Hellriegel, ET, 2010
)
0.85
"The single-dose pharmacokinetic profile of cyclobenzaprine extended-release (CER) has been previously characterized and compared with the pharmacokinetics of cyclobenzaprine immediate-release (CIR) administered 3 times daily for 3 doses."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.89
"The objective of this study was to characterize the multiple-dose pharmacokinetic properties of once-daily CER 30 mg and CIR 10 mg TID formulations in healthy volunteers."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.63
" Pharmacokinetic assessments at steady state included area under the plasma cyclobenzaprine concentration-time curve over the dosing interval (AUC(0-τ,ss)), peak plasma cyclobenzaprine concentration (C(max,ss)), time to observed C(max) (T(max,ss)), observed minimum cyclobenzaprine concentration (C(min,ss)), average cyclobenzaprine concentration (C(avg,ss)), accumulation ratio (R(ac)), and terminal elimination half-life (t(½))."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.86
" Because of a protocol violation (insufficient data), no steady-state pharmacokinetic assessments could be performed for CIR."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.63
" Owing to a protocol violation, steady-state pharmacokinetic properties for CIR could not be assessed."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.63
"A sensitive, rapid and simple liquid chromatography-electrospray ionization mass spectrometry (LC-ESI-MS/MS) method was developed for the quantitative determination of cyclobenzaprine in human plasma, to study the pharmacokinetic behavior of cyclobenzaprine capsule in healthy Chinese volunteers."( Determination of cyclobenzaprine in human plasma by liquid chromatography-electrospray ionization tandem mass spectrometry and its application in a pharmacokinetic study.
Chen, X; Jiang, H; Li, D; Peng, K; Qian, Z; Xiang, Y; Zheng, H; Zhou, L, 2012
)
0.91
" Pharmacokinetic parameters related to absorption, distribution, and elimination were calculated."( Pharmacokinetics and bioequivalence evaluation of cyclobenzaprine tablets.
Brioschi, TM; Ching, TH; Kano, EK; Koono, EE; Porta, V; Schramm, SG; Serra, CH, 2013
)
0.64

Bioavailability

The pharmacokinetics and bioavailability of cyclobenzaprine, a widely used muscle relaxant, were investigated in four clinical studies. Age, gender, and hepatic insufficiency were characterized.

ExcerptReferenceRelevance
"The pharmacokinetics and bioavailability of cyclobenzaprine, a widely used muscle relaxant, were investigated in four clinical studies, and the effects of age, gender, and hepatic insufficiency were characterized."( Cyclobenzaprine pharmacokinetics, including the effects of age, gender, and hepatic insufficiency.
Chavez-Eng, CM; Constanzer, ML; King, JD; Korn, SH; Winchell, GA, 2002
)
2.02
"Food can alter the bioavailability of the controlled-release formulations of many different drugs."( Effect of food on the pharmacokinetics of once-daily cyclobenzaprine extended-release 30 mg: a randomized, open-label, crossover, single-centre study.
Darwish, M; Xie, F, 2009
)
0.6
" The bioavailability of the 2 doses, as indicated by the least squares mean AUC(0-infinity), was 330."( A pharmacokinetic comparison of single doses of once-daily cyclobenzaprine extended-release 15 mg and 30 mg: a randomized, double-blind, two-period crossover study in healthy volunteers.
Chang, S; Darwish, M; Hellriegel, ET, 2009
)
0.6
"To evaluate the systemic bioavailability of a new controlled release cyclobenzaprine tablet, and the influence of a high fat meal on its bioavailability."( Bioavailability of a controlled-release cyclobenzaprine tablet and influence of a high fat meal on bioavailability.
Arancibia, A; Costa, E; Gai, MN, 2009
)
0.86
"24 and 12 healthy male subjects were recruited for the bioavailability and influence of diet studies, respectively."( Bioavailability of a controlled-release cyclobenzaprine tablet and influence of a high fat meal on bioavailability.
Arancibia, A; Costa, E; Gai, MN, 2009
)
0.62
"In the bioavailability study, plasma cyclobenzaprine profiles were in agreement with a controlled release system."( Bioavailability of a controlled-release cyclobenzaprine tablet and influence of a high fat meal on bioavailability.
Arancibia, A; Costa, E; Gai, MN, 2009
)
0.89
"The controlled release tablet showed a relative bioavailability comparable with equal dose of the immediate release product and produced a significantly lower Cmax, as expected in a controlled release formulation."( Bioavailability of a controlled-release cyclobenzaprine tablet and influence of a high fat meal on bioavailability.
Arancibia, A; Costa, E; Gai, MN, 2009
)
0.62
" This analytical method was applied in a relative bioavailability study in order to compare a test chlorpromazine 100 mg simple dose formulation versus a reference in 57 volunteers of both sexes."( Chlorpromazine quantification in human plasma by UPLC-electrospray ionization tandem mass spectrometry. Application to a comparative pharmacokinetic study.
Borges, DC; Borges, NC; Donato, JL; Moreira, RF; Moreira, RP; Moreno, P; Moreno, RA; Rezende, VM; Santana, JM, 2011
)
0.37
"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
" However, these bioactivities have been hampered by chemical instability, poor water solubility, rapid metabolism, and low bioavailability of PAP."( Preparation, optimization, and pharmacokinetic study of nanoliposomes loaded with triacylglycerol-bound punicic acid for increased antihepatotoxic activity.
Adu-Frimpong, M; Deng, W; Firempong, CK; Mukhtar, YM; Omari-Siaw, E; Wang, Q; Xu, X; Yu, J; Yu, Q, 2019
)
0.51

Dosage Studied

Cyclobenzaprine has been commonly compounded by pharmacists into topically applied dosage forms for the treatment of pain disorders. Five modified multivariate calibration models based on classical least squares (CLS) in addition to traditional CLS model are developed and validated. With once-daily dosing of CER, cyclobenzAPrine HCl (CZ) was found to have a positive therapeutic response.

ExcerptRelevanceReference
" A reduction in dose or dosing frequency should be considered in the elderly and in patients with liver disease."( Cyclobenzaprine pharmacokinetics, including the effects of age, gender, and hepatic insufficiency.
Chavez-Eng, CM; Constanzer, ML; King, JD; Korn, SH; Winchell, GA, 2002
)
1.76
" Sedation is the most common adverse event associated with its use at the usual dosage of 10 mg TID."( Efficacy of a low-dose regimen of cyclobenzaprine hydrochloride in acute skeletal muscle spasm: results of two placebo-controlled trials.
Borenstein, DG; Korn, S, 2003
)
0.6
"To determine the weight variation and calculated dosing variability of tablet fragments upon splitting unscored cyclobenzaprine hydrochloride 10 mg tablets using two common tablet splitting devices."( Variability in tablet fragment weights when splitting unscored cyclobenzaprine 10 mg tablets.
Cook, TJ; Edwards, S; Fox, T; Gyemah, C; Shah, I; Shah, M,
)
0.58
" Accordingly, splitting cyclobenzaprine 10 mg tablets to achieve 5 mg doses could result in unpredictable dosing and therapeutic response."( Variability in tablet fragment weights when splitting unscored cyclobenzaprine 10 mg tablets.
Cook, TJ; Edwards, S; Fox, T; Gyemah, C; Shah, I; Shah, M,
)
0.68
" Study comparisons included the plasma cyclobenzaprine AUC to 168 hours after dosing (AUC(0-168)), AUC(0-infinity), and C(max)."( A pharmacokinetic comparison of single doses of once-daily cyclobenzaprine extended-release 15 mg and 30 mg: a randomized, double-blind, two-period crossover study in healthy volunteers.
Chang, S; Darwish, M; Hellriegel, ET, 2009
)
0.87
" This case might be additional evidence for the necessity of appropriate dosage in case of liver impairment."( Torticollis under cyclobenzaprine.
Fischer, F; Jauss, M; Muller, SC; Reuss, R; Reuter, I; Stolz, E, 2009
)
0.69
" CIR is typically prescribed at a dosage of 10 mg three-times-daily."( Pharmacokinetic profile of once-daily cyclobenzaprine extended-release.
Darwish, M; Hellriegel, ET, 2010
)
0.63
"In this double-blind, single-center, 2-period crossover study, healthy subjects were randomized to dosing sequences with once-daily CER 30 mg or CIR 10 mg TID for 7 days."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.63
"A total of 36 subjects were randomized; 34 completed both dosing periods (1 subject was lost to follow-up, 1 withdrew consent)."( Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers.
Darwish, M; Hellriegel, ET, 2011
)
0.63
"Cyclobenzaprine has been commonly compounded by pharmacists into topically applied dosage forms for the treatment of pain disorders."( Skin Permeation and Antinociception of Compounded Topical Cyclobenzaprine Hydrochloride Formulations.
Arnold, J; Asbill, S; Bryson, E; Gorman, G; Hartman, R; Sweitzer, S,
)
1.82
" Cyclobenzaprine specimens were equally likely to be positive whether the dose was oral or topical, although mean levels after topical dosing were approximately 13-21% those after oral dosing."( Urinary Concentrations of Topically Administered Pain Medications.
Bell, P; Glinn, MA; Harvey, A; Lickteig, AJ; Rappold, B; Recer, S; Salske, M; Stensland, J; Weber, L, 2017
)
1.37
"Five modified multivariate calibration models based on classical least squares (CLS) in addition to traditional CLS model are developed and validated for assaying cyclobenzaprine HCl (CZ) with its major degradants; dibenzocycloheptatrienone (DZ) and anthraquinone (AQ), whether in its pure form or in pharmaceutical dosage form."( Five modified classical least squares based models for stability indicating analysis of cyclobenzaprine HCl with its major degradation products: A comparative study.
Darwish, HW; Darwish, IA; Naguib, IA, 2018
)
0.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
muscle relaxantA drug used to produce muscle relaxation (excepting neuromuscular blocking agents). Its primary clinical and therapeutic use is the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. Also used for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in multiple sclerosis.
tranquilizing drugA traditional grouping of drugs said to have a soothing or calming effect on mood, thought or behaviour.
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
plant metaboliteAny eukaryotic metabolite produced during a metabolic reaction in plants, the kingdom that include flowering plants, conifers and other gymnosperms.
[role 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]

Drug Classes (2)

ClassDescription
carbotricyclic compoundA carbopolyclic compound comprising of three carbocyclic rings.
9,11,13-octadecatrienoic acidAny octadecatrienoic acid with three fully-conjugated double bonds at positions 9, 11 and 13.
[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 (29)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
15-lipoxygenase, partialHomo sapiens (human)Potency39.81070.012610.691788.5700AID887
ATAD5 protein, partialHomo sapiens (human)Potency14.57500.004110.890331.5287AID493106
Fumarate hydrataseHomo sapiens (human)Potency33.17340.00308.794948.0869AID1347053
USP1 protein, partialHomo sapiens (human)Potency0.08910.031637.5844354.8130AID504865
PPM1D proteinHomo sapiens (human)Potency11.70860.00529.466132.9993AID1347411
ThrombopoietinHomo sapiens (human)Potency15.84890.02517.304831.6228AID917; AID918
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.94330.001318.074339.8107AID926; AID938
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency23.91850.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency18.77860.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
cytochrome P450 2D6Homo sapiens (human)Potency8.48660.00108.379861.1304AID1645840
polyproteinZika virusPotency33.17340.00308.794948.0869AID1347053
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency35.48130.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency13.97120.00207.533739.8107AID891
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.58930.316212.443531.6228AID902
D(1A) dopamine receptorHomo sapiens (human)Potency0.66320.02245.944922.3872AID488982; AID488983
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency37.93300.134610.395030.1313AID1347049
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency16.48160.00669.809418.4927AID1347050
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency21.30160.00378.618923.2809AID2667; AID2668
gemininHomo sapiens (human)Potency13.33590.004611.374133.4983AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency20.31480.005612.367736.1254AID624032
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.07190.00106.000935.4813AID943; AID944
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency18.85410.316212.765731.6228AID881
Interferon betaHomo sapiens (human)Potency11.70860.00339.158239.8107AID1347411
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency18.85410.00638.235039.8107AID881
D(1A) dopamine receptorSus scrofa (pig)Potency26.12160.00378.108123.2809AID2667
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency0.31621.000010.475628.1838AID1457
Ataxin-2Homo sapiens (human)Potency14.12540.011912.222168.7989AID588378
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)107.40000.11007.190310.0000AID1449628
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC50 (µMol)10.00000.04004.113710.0000AID1850268
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (83)

Processvia Protein(s)Taxonomy
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)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo 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)
modulation of chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
response to amyloid-betaVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (25)

Processvia Protein(s)Taxonomy
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)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo 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)
amyloid-beta bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
protein bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
ATP bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
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)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
synapseVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
neuronal cell bodyVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (113)

Assay IDTitleYearJournalArticle
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.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1210014Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation assessed as remaining activity at 30 uM after 5 mins by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1215127Ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay to fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
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.
AID1210013Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation assessed as remaining activity at 30 uM after 5 mins by LC-MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID298032Acid dissociation constant, pKa of the compound2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1850268Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay2022RSC medicinal chemistry, Feb-23, Volume: 13, Issue:2
Inhibition of N-type calcium ion channels by tricyclic antidepressants - experimental and theoretical justification for their use for neuropathic pain.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1053260Antagonist activity at human recombinant dopamine D2 long receptor expressed in CHOK1 cells coexpressing mitochondrial apoaequorin assessed as inhibition of agonist-induced effect at 50 uM after 15 mins by luminometric analysis relative to haloperidol2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID58617Evaluated for the antiarrhythmic activity in conscious dogs after myocardial infarction by observing 50% reduction in ectopic rate.. 1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Antiarrhythmic activity of amitriptyline analogues in conscious dogs after myocardial infarction: cyproheptadinium methiodide.
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.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1053264Antagonist activity at human recombinant dopamine D1 receptor expressed in CHOK1 cells assessed as inhibition of agonist-induced cAMP accumulation at 100 uM preincubated for 10 mins prior to agonist addition measured after 30 mins by HTRF assay relative t2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1053266Agonist activity at human recombinant dopamine D1 receptor expressed in CHOK1 cells assessed as stimulation of cAMP accumulation at 100 uM after 30 mins by HTRF assay relative to SKF812972013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID298031Lipophilicity, log D at pH7.42007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1053262Agonist activity at human recombinant dopamine D2 long receptor expressed in CHOK1 cells coexpressing mitochondrial apoaequorin at 100 uM by luminometric analysis relative to quinpirol2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID58619Evaluated for the antiarrhythmic activity in conscious dogs after myocardial infarction by observing for conversion to sinus rhythm.1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Antiarrhythmic activity of amitriptyline analogues in conscious dogs after myocardial infarction: cyproheptadinium methiodide.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1508628Confirmatory 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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1885158Growth inhibition of human T98 GBM cells2022Journal of medicinal chemistry, 07-14, Volume: 65, Issue:13
Glioblastoma: Current Status, Emerging Targets, and Recent Advances.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (260)

TimeframeStudies, This Drug (%)All Drugs %
pre-199040 (15.38)18.7374
1990's23 (8.85)18.2507
2000's51 (19.62)29.6817
2010's107 (41.15)24.3611
2020's39 (15.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 129.36

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 Index129.36 (24.57)
Research Supply Index5.63 (2.92)
Research Growth Index4.79 (4.65)
Search Engine Demand Index239.87 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (129.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials46 (19.91%)5.53%
Trials2 (3.64%)5.53%
Reviews21 (9.09%)6.00%
Reviews4 (7.27%)6.00%
Case Studies49 (21.21%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other115 (49.78%)84.16%
Other49 (89.09%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (44)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Parallel-Group,Double-Blind,Double-Dummy,Superiority Study of Etoricoxib90mg/ Cyclobenzaprine15mg From Eurofarma Versus Etoricoxib90mg (Arcoxia®) and Cyclobenzaprine15mg (XL - Mitrul®) for Muscle Spasm After Third Molar Extraction in Brazil [NCT05683574]Phase 3954 participants (Anticipated)Interventional2024-06-30Not yet recruiting
Efficacy and Safety of Cyclobenzaprine Hydrochloride Extended Release for the Treatment of Chronic Migraine: A Randomized, Double-Blind, Placebo-Controlled Trial [NCT01151787]Phase 335 participants (Actual)Interventional2010-07-31Terminated(stopped due to Study was never initiated under new location/provider group. Contract to continue was never signed between TEVA and Kennedy Headache Center)
A Phase 3, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study to Evaluate the Efficacy and Safety of TNX-102 SL in Participants With PTSD Taken Daily at Bedtime (Protocol No. TNX-CY-P302) [NCT03841773]Phase 3192 participants (Actual)Interventional2019-03-07Terminated(stopped due to Interim Analysis results)
A Phase 3, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study To Evaluate The Efficacy And Safety Of TNX-102 SL Taken Daily At Bedtime In Patients With Fibromyalgia [NCT04172831]Phase 3503 participants (Actual)Interventional2019-12-09Completed
Driving Simulation Cross-Over Study of Sedative Effects of Tolperisone Compared to Cyclobenzaprine and Placebo [NCT03353922]Phase 135 participants (Actual)Interventional2017-07-31Completed
A Phase 3, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study to Evaluate the Efficacy and Safety of TNX-102 SL Taken Daily at Bedtime in Patients With Military-Related PTSD [NCT03062540]Phase 3358 participants (Actual)Interventional2017-03-27Terminated(stopped due to Stopped early due to inadequate separation on primary efficacy endpoint at Week 12 according to Interim Analysis conducted on the first 274 (50%) patients.)
A Phase III, Randomized, Single-Blind, Superiority Study Comparing The Efficacy And Tolerability Of A New Drug Containing The Combination Meloxicam And Cyclobenzaprine And The Same Components Alone In The Treatment Of Acute Lumbago [NCT01587508]Phase 30 participants (Actual)Interventional2013-05-31Withdrawn(stopped due to The comparator product was withdrawn from the brazilian market not being possible to conduct the design regarding initially planned.)
A Randomized, 4-Period, Crossover Study to Investigate the Effects of Tolperisone on Measures of Drowsiness and Cognitive Function Compared to Cyclobenzaprine and Placebo [NCT04407377]Phase 139 participants (Actual)Interventional2020-06-20Completed
Pharmacokinetics and Safety of Commonly Used Drugs in Lactating Women and Breastfed Infants [NCT03511118]1,600 participants (Anticipated)Observational2018-10-04Recruiting
A Multiple-Dose, Randomized, Open-Label, Parallel Pharmacokinetic Comparison Study of TNX-102 SL (Cyclobenzaprine Hydrochloride [HCl] Sublingual Tablets) 2 x 2.8 mg Versus AMRIX® (Cyclobenzaprine HCl ER Capsules) 30 mg in Healthy Subjects Under Fasting Co [NCT03443960]Phase 160 participants (Actual)Interventional2018-01-29Completed
A Phase 3, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study To Evaluate The EFFIcacy and Safety of TNX-102 SL Tablets Taken Daily At Bedtime In Patients With FibRoMyalgia [NCT02829814]Phase 351 participants (Actual)Interventional2016-07-31Terminated(stopped due to For business reason unrelated to safety or tolerability,Tonix has discontinued the Fibromyalgia development with TNX102 SL.)
Medication Effects on Periurethral Sensation, Urethral Sphincter Activity and Pressure Flow Parameters [NCT01028014]56 participants (Actual)Interventional2010-04-30Completed
Phase III, National, Multicenter, Randomized, Double-blind, Double-masked, Compare the Efficacy of Ketoprofen, Cyclobenzaprine and Caffeine Association Versus Cyclobenzaprine and Caffeine (Miosan Caf®) in the Treatment of Osteomuscular Pain in Adults [NCT02862977]Phase 3414 participants (Actual)Interventional2017-11-10Completed
Prospective Analgesic Compound Efficacy (PACE) Study [NCT02403687]300 participants (Actual)Observational [Patient Registry]2015-06-30Completed
A 12-Week Open-Label Extension Study to Evaluate TNX-102 SL Taken Daily at Bedtime in Patients With PTSD [NCT03110575]Phase 3189 participants (Actual)Interventional2017-06-20Terminated(stopped due to Stopped early due to inadequate separation on primary efficacy endpoint in the lead-in HONOR study, TNX-CY-P301)
A Randomized, Double-Blind, Parallel-Group, Placebo-Controlled, Multicenter Trial to Study the Efficacy and Safety of Cyclobenzaprine HCl Extended Release (CER) 15 mg in Subjects With Acute Cervical and/or Lower Back Pain Due to Muscle Spasms of Local Ori [NCT02814565]Phase 3180 participants (Actual)Interventional2016-10-12Completed
An Open Label, Balanced, Randomized, Two-Treatment, Two-Sequence, Two-Period, Single-Dose, Crossover, Bioavailability Study Comparing Cyclobenzaprine Hydrochloride 10 mg Tablet of Ohm Labs Inc (A Subsidiary of Ranbaxy Pharmaceuticals Inc USA.) With Flexer [NCT00778037]40 participants (Actual)Interventional2006-09-30Completed
A Single-dose, Randomized, Open-label, 3-way Crossover Study to Evaluate the Dose-proportionality and Food Effect of TNX-102 SL (Cyclobenzaprine HCl Sublingual Tablets) in Healthy Subjects [NCT04164719]Phase 116 participants (Actual)Interventional2019-10-14Completed
The Short-term Use of Cyclobenzaprine in Patients Undergoing Vaginal Surgery [NCT01081990]63 participants (Actual)Interventional2010-04-30Completed
A Single-Dose, Open-Label, Randomized, Parallel-Design Study Of The Comparative Pharmacokinetics And Safety Of TNX-102 2.8 mg SL Tablets (With Potassium Phosphate) At 2.8 mg, TNX-102-B 2.8 mg SL Tablets (With Sodium Phosphate) At 2.8 mg, TNX-102-C 2.8 mg [NCT01889173]Phase 124 participants (Actual)Interventional2013-06-30Completed
Cyclobenzaprine Treatment for Muscle Cramps in Cirrhotic Patients [NCT02642861]Phase 3200 participants (Anticipated)Interventional2018-10-31Not yet recruiting
Bioavailability of Cyclobenzaprine HCl Tablets [NCT00913419]Phase 130 participants (Actual)Interventional1988-11-30Completed
A Phase 3, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study to Evaluate the Efficacy and Safety of TNX-102 SL Tablets Taken Daily at Bedtime in Patients With Fibromyalgia [NCT02436096]Phase 3519 participants (Actual)Interventional2015-04-30Completed
Opiate Free Multimodal Pain Pathway in Elective Foot and Ankle Surgery: A Prospective Study [NCT04771741]72 participants (Actual)Observational2020-12-01Completed
Trigger Point Injection for Myofascial Pain Syndrome in the Low Back (T-PIMPS): A Randomized Controlled Trial. [NCT04704297]Phase 4180 participants (Anticipated)Interventional2020-12-28Recruiting
A 12-Week, Open-Label, Multicenter, Extension Study To TNX-CY-P201 To Evaluate The Safety And Efficacy Of TNX-102 SL Taken Daily At Bedtime In Patients With Military-Related PTSD And Related Conditions [NCT02421679]Phase 2159 participants (Actual)Interventional2015-04-30Completed
An Eight Week, Double-Blind Efficacy Study of Cyclobenzaprine ER (Amrix TM) Augmentation to Alleviate Fibromyalgia Fatigue and Muscle Pain [NCT01041495]Phase 437 participants (Actual)Interventional2009-06-30Terminated(stopped due to ran out of funding short of enrollment expected)
A Single-Dose, Open-Label, Randomized, Parallel-Design Study of the Comparative Pharmacokinetics and Safety of TNX-102 2.4 mg SL Tablets (With Phosphate) at 2.4 mg and 4.8 mg, TNX-102-A 2.4 mg SL Tablets (Without Phosphate) at 2.4 mg and Cyclobenzaprine 5 [NCT01689259]Phase 124 participants (Actual)Interventional2012-09-30Completed
A Single-Dose, Open-Label, Randomized, Three-Way Crossover Study of the Comparative Bioavailability of TNX-102 2.4 mg and Cyclobenzaprine 5 mg Tablets and of the Effect of Food on the Pharmacokinetics of TNX-102 2.4 mg in Healthy Adults [NCT01490788]Phase 130 participants (Actual)Interventional2011-11-18Completed
UMCC 2013.051: Prospective Pilot Study Evaluating the Use of Cyclobenzaprine for Treatment of Sleep Disturbance, Fatigue, and Musculoskeletal Symptoms in Aromatase Inhibitor-treated Breast Cancer Patients [NCT01921296]Phase 22 participants (Actual)Interventional2013-08-31Terminated(stopped due to Accrual terminated early because of poor accrual)
Flexeril� (Cyclobenzaprine Hydrochloride) Community Based Study - An Evaluation of Cyclobenzaprine HCl Monotherapy and in Combination With Ibuprofen for Acute Back or Neck Muscle Pain With Muscle Spasm [NCT00246389]Phase 41,000 participants (Actual)InterventionalCompleted
A Phase 2, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study to Evaluate the Efficacy and Safety of Daily Bedtime TNX-102 SL in Participants With PTSD [NCT05372887]Phase 20 participants (Actual)Interventional2022-10-14Withdrawn(stopped due to The study was stopped due to business reasons.)
A Single-Dose, Open-Label, Randomized Study of the Comparative Pharmacokinetics of Sublingual TNX-102 2.4 mg at pH 3.5 and 7.1, Oral Cyclobenzaprine 5 mg Tablets, and Intravenous Cyclobenzaprine 2.4 mg in Healthy Adults [NCT01634412]Phase 124 participants (Actual)Interventional2012-06-30Completed
A Phase 2b, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study to Evaluate the Efficacy and Safety of TNX-102 SL Tablets Taken at Bedtime in Patients With Fibromyalgia [NCT01903265]Phase 2/Phase 3205 participants (Actual)Interventional2013-09-30Completed
A SINGLE-DOSE, RANDOMIZED, OPEN-LABEL, TWO-WAY CROSSOVER BIOEQUIVALENCE STUDY OF TNX-102 SL (CYCLOBENZAPRINE HCL SUBLINGUAL TABLETS) 2.8 mg FROM TWO MANUFACTURERS IN HEALTHY SUBJECTS UNDER FASTING CONDITIONS [NCT03168022]Phase 143 participants (Actual)Interventional2015-12-16Completed
Analysis of the Effects of the Osteopathic Manipulative Treatment in Carriers of Temporomandibular Disorders: Randomized Clinical Trial [NCT02974166]32 participants (Actual)Interventional2012-03-31Completed
A 12-Month, Multicenter, Open-Label Extension Study (F202) to Evaluate the Long-term Safety of TNX-102 SL Tablets Taken Daily at Bedtime in Patients With Fibromyalgia [NCT02015234]Phase 3158 participants (Actual)Interventional2013-12-31Completed
Phase III Randomized, Unicentric, Double-masked, Parallel Trial for the Efficacy and Tolerability of the Fixed Dose Combination of Etodolac 400 mg and Cyclobenzaprine 10 mg Versus the Isolated Active Substances (Flancox® 400 mg And Miosan® 10 mg) in Posto [NCT03127592]Phase 3140 participants (Actual)Interventional2020-10-05Terminated(stopped due to recruitment difficulty)
Phase III, National, Multicenter, Randomized, Double-blind, Double-Masked, Compare the Efficacy of Ketoprofen + Cyclobenzaprine Association Versus Cyclobenzaprine (Miosan®) in the Treatment of Osteomuscular Pain in Adults [NCT03025113]Phase 3416 participants (Actual)Interventional2018-03-08Completed
Comparison of Ibuprofen, Cyclobenzaprine, or Both for Acute Cervical Strain: A Randomized Clinical Trial [NCT00790270]Phase 261 participants (Actual)Interventional2003-01-31Completed
A Phase 3, Double-Blind, Randomized, Multicenter, Placebo-Controlled Study To Evaluate The Efficacy And Safety Of TNX-102 SL Taken Daily At Bedtime In Patients With Fibromyalgia [NCT04508621]Phase 3514 participants (Actual)Interventional2020-07-22Completed
A 3-Month, Multicenter, Open-Label Extension to Evaluate Safety and Efficacy of TNX-102 SL Tablets Taken Daily at Bedtime in Patients With Fibromyalgia [NCT02589275]Phase 3375 participants (Actual)Interventional2015-08-31Terminated(stopped due to For business reason unrelated to safety or tolerability,Tonix has discontinued the Fibromyalgia development with TNX102 SL.)
Multimodal Analgesia Effect on Post Surgical Patient [NCT04240626]Phase 460 participants (Anticipated)Interventional2021-01-20Recruiting
A Randomized Three-armed Comparative Effectiveness Study of Various Medications for Musculoskeletal Low Back Pain: Defining the Added Benefit of Muscle Relaxants and Opioids. [NCT01587274]Phase 4323 participants (Actual)Interventional2012-04-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00790270 (2) [back to overview]Use of Rescue Medications
NCT00790270 (2) [back to overview]Resumption of Work or School
NCT01028014 (3) [back to overview]Difference (Pre - Post) in Maximum Urine Flow Rate (Qmax) (Milliliters Per Second) as Measured by Pressure Flowmetry
NCT01028014 (3) [back to overview]Difference (Pre - Post) in Amplitude (Microvolts) of Urethral Sphincter Activity as Measured by Quantitative Concentric Needle EMG
NCT01028014 (3) [back to overview]Difference (Pre - Post) in Urethral Sensation (Milliamps) as Measured by Current Perception Threshold Testing.
NCT01041495 (3) [back to overview]Brief Fatigue Inventory at 8 Weeks Post Treatment
NCT01041495 (3) [back to overview]Fibromyalgia Impact Questionnaire Scores at 8 Weeks Post Treatment
NCT01041495 (3) [back to overview]Visual Analogue Pain Scale at 8 Weeks Post Treatment
NCT01490788 (2) [back to overview]Mean Plasma Concentration (AUC) of Cyclobenzaprine
NCT01490788 (2) [back to overview]Incidences of Adverse Events
NCT01587274 (1) [back to overview]Change in Functional Disability as Measured by the Roland Morris Disability Questionnaire
NCT01903265 (5) [back to overview]Mean Change From Baseline in Weekly Average of Daily Pain Scores at Week 12
NCT01903265 (5) [back to overview]Change From Baseline to Week 12 in PROMIS T-score for Sleep Disturbance
NCT01903265 (5) [back to overview]Change From Baseline to Week 12 in FIQ-R Total Score
NCT01903265 (5) [back to overview]30% Responder Analysis of IVRS NRS Pain Assessments at Week 12
NCT01903265 (5) [back to overview]"Patient Global Impression of Change (PGIC) Responder Status (Very Much Improved or Much Improved vs All Other Categories) at Week 12"
NCT01921296 (5) [back to overview]Change in Average Pain Between Baseline and Week 8 With Cyclobenzaprine Therapy
NCT01921296 (5) [back to overview]Percentage of Subjects Who Continue to Take Aromatase Inhibitor Therapy
NCT01921296 (5) [back to overview]Percentage of Patients That Experience Adverse Events
NCT01921296 (5) [back to overview]Number of Patients That Experience an Improvement in Sleep Quality as Assessed Using the Pittsburgh Sleep Quality Index (PSQI) With 8 Weeks of Cyclobenzaprine Therapy.
NCT01921296 (5) [back to overview]Change in Fatigue Between Baseline and Week 8 With Cyclobenzaprine Therapy
NCT02015234 (4) [back to overview]Newly-emergent Adverse Events (NEAEs) During Treatment With TNX-102 SL Tablets Taken Daily at Bedtime Over 12 Months in Patients With Fibromyalgia.
NCT02015234 (4) [back to overview]Responder Analysis of Patient's Global Impression of Change (PGIC)
NCT02015234 (4) [back to overview]Change From Baseline in Numerical Rating Scale (NRS) Assessments of Average Pain Based on a 7 Day Recall
NCT02015234 (4) [back to overview]Change From Baseline in Numerical Rating Scale (NRS) Assessments of Average Pain Based on 24 Hour Recall
NCT02814565 (10) [back to overview]Percentage of Participants With Physician's Clinical Global Assessment on Days 7 and 15 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Physician's Clinical Global Assessment on Day 3 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Subject's Rating of Medication Helpfulness Impression on Day 3 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Physician Rated Assessment of Presence of Muscle Spasm on Days 3, 7, and 15 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Physician Rated Assessment of Presence of Local Pain on Days 3, 7, and 15 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Physician Rated Assessment of Limitation of Range of Motion on Days 3, 7, and 15 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Physician Rated Assessment of Limitation of Activities of Daily Living on Days 3, 7, and 15 of Treatment
NCT02814565 (10) [back to overview]Percentage of Responders on Days 3, 7, and 14 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Subject's Rating of Medication Helpfulness Impression on Days 7 and 14 of Treatment
NCT02814565 (10) [back to overview]Percentage of Participants With Subject-Rated Global Impression on Days 3, 7, and 14 of Treatment
NCT03168022 (2) [back to overview]Mean Plasma Concentration (AUC) of Cyclobenzaprine
NCT03168022 (2) [back to overview]Number of Subjects With Treatment-emergent Adverse Events (TEAEs) of Treatment A and Treatment B, Administered as 1 x 2.8 mg TNX-102 SL Under Fasting Conditions.
NCT03353922 (4) [back to overview]Sleepiness Endpoint Karolinska Sleepiness Scale KSS
NCT03353922 (4) [back to overview]Steady State Standard Deviation of Lateral Position (SDLP) Day 3
NCT03353922 (4) [back to overview]Standard Deviation of Lateral Position (SDLP) in Simulated Driving Test of Tolperisone Compared to Placebo on Day 2 Next Day Residual Effect
NCT03353922 (4) [back to overview]Standard Deviation of Lateral Position (SDLP)
NCT04172831 (7) [back to overview]Change From Baseline to Week 14 in the Fibromyalgia Impact Questionnaire - Revised (FIQR) Symptoms Domain Score
NCT04172831 (7) [back to overview]Change From Baseline to Week 14 in the FIQR Function Domain Score
NCT04172831 (7) [back to overview]Change From Baseline to Week 14 in the Numerical Rating Scale (NRS) Weekly Average of Daily Self-reported Average Pain Severity Scores.
NCT04172831 (7) [back to overview]Change From Baseline to Week 14 in the Patient Reported Outcomes Measurement Information System (PROMIS) Score for Sleep Disturbance
NCT04172831 (7) [back to overview]Change From Baseline to Week 14 in the PROMIS Score for Fatigue
NCT04172831 (7) [back to overview]Change From Baseline to Week 14 in the Weekly Average of the Daily Diary Assessment of Sleep Quality
NCT04172831 (7) [back to overview]"Number of Patients With a Patient's Global Impression of Change (PGIC) Rating of Very Much Improved or Much Improved"
NCT04508621 (7) [back to overview]"Number of Patients With a Patient's Global Impression of Change (PGIC) Rating of Very Much Improved or Much Improved"
NCT04508621 (7) [back to overview]Change From Baseline to Week 14 in the FIQ-R Function Domain Score
NCT04508621 (7) [back to overview]Change From Baseline to Week 14 in the Numerical Rating Scale (NRS) Weekly Average of Daily Self-reported Average Pain Severity Scores.
NCT04508621 (7) [back to overview]Change From Baseline to Week 14 in the Patient Reported Outcomes Measurement Information System (PROMIS) Score for Sleep Disturbance
NCT04508621 (7) [back to overview]Change From Baseline to Week 14 in the PROMIS Score for Fatigue
NCT04508621 (7) [back to overview]Change From Baseline to Week 14 in the Weekly Average of the Daily Diary Assessment of Sleep Quality
NCT04508621 (7) [back to overview]Change From Baseline to Week 14 in the Fibromyalgia Impact Questionnaire - Revised (FIQ-R) Symptoms Domain Score.

Use of Rescue Medications

the number of patients taking additional rescue medications beyond the study meds (NCT00790270)
Timeframe: 24 hours

Interventionparticipants (Number)
Cyclobenzaprine13
Ibuprofen9
Ibuprophen Plus Cyclobenzaprine9

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Resumption of Work or School

number of patients resuming regular activity the day following enrollment. (NCT00790270)
Timeframe: next day

Interventionparticipants (Number)
Cyclobenzaprine8
Ibuprofen14
Ibuprophen Plus Cyclobenzaprine13

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Difference (Pre - Post) in Maximum Urine Flow Rate (Qmax) (Milliliters Per Second) as Measured by Pressure Flowmetry

Pressure Flowmetry was used to measure maximum urine flow rate (Qmax)before and after 2 weeks of therapy with one of 6 randomly assigned medications. A 300 cc bladder fill was performed through the catheter, the catheter was removed, and transurethral and transrectal pressure transducers were placed for the pressure flow study. Voiding was performed in the seated position. Information obtained for the database included Qmax, average flow rate, time to Qmax, detrusor pressure at maximum flow rate, voided volume, and a calculated post-void residual. (NCT01028014)
Timeframe: 2 weeks

Interventionmilliliters per second (Median)
Pseudoephedrine 120mg ER Daily-7.3
Solifenacin 5mg Daily5.0
Tamsulosin 0.4mg Daily-5.6
Imipramine 25mg Daily-6.6
Cyclobenzaprine 10mg Daily10.3
Lactose Capsules, One Daily10.4

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Difference (Pre - Post) in Amplitude (Microvolts) of Urethral Sphincter Activity as Measured by Quantitative Concentric Needle EMG

Concentric needle EMG was used to measure urethral sphincter activity at 2-3 sites around the urethral meatus before and after 2 weeks of therapy with one of 6 randomly assigned medications. Two methods of quantitative electromyography were performed on all subjects. (1) Multi-Motor Unit Action Potential (MUP) analysis, which has been shown to be the most sensitive technique in distinguishing neuropathic from control muscles; and (2) interference pattern analysis (IPA) which reflects changes in MUP recruitment from weak effort to maximal contraction. (NCT01028014)
Timeframe: 2 weeks

Interventionmicrovolts (Median)
Pseudoephedrine 120mg ER Daily-18
Solifenacin 5mg Daily10
Tamsulosin 0.4mg Daily11
Imipramine 25mg Daily-15
Cyclobenzaprine 10mg Daily12
Lactose Capsules, One Daily36

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Difference (Pre - Post) in Urethral Sensation (Milliamps) as Measured by Current Perception Threshold Testing.

Current Perception Threshold testing was used to measure urethral sensation before and after 2 weeks of therapy with one of 6 randomly assigned medications. We performed CPT testing in the urethra using a Neurometer®, which is a constant current stimulator capable of delivering sine wave electrical stimuli at 3 frequencies (2000 Hz, 250 Hz and 5 Hz). At all 3 frequencies, the stimulus intensity was gradually increased until first perceived, and then decreased until no longer perceptible. CPT values were obtained using a semi-automated forced choice paradigm. (NCT01028014)
Timeframe: 2 weeks

InterventionMilliamps (Median)
Pseudoephedrine 120mg ER Daily0.06
Solifenacin 5mg Daily0.06
Tamsulosin 0.4mg Daily-0.8
Imipramine 25mg Daily-0.12
Cyclobenzaprine 10mg Daily0.0
Lactose Capsules, One Daily0.03

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Brief Fatigue Inventory at 8 Weeks Post Treatment

Change in baseline subjective fatigue based on this scale (1= no fatigue, 10 = severe fatigue) from baseline (T=Zero, prior to drug/placebo treatment) to week 8 (NCT01041495)
Timeframe: baseline to 8 weeks

Interventionscore on a scale (Mean)
Cyclobenzaprine ER4.7
Placebo4.8

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Fibromyalgia Impact Questionnaire Scores at 8 Weeks Post Treatment

Change in baseline subjective fibromyalgia symptoms based on a 100 point scale (0 = no fibromyalgia or minimum score, 100 = severe fibromyalgia and maximal score) from baseline (T=Zero, prior to drug/placebo treatment) to week 8 (NCT01041495)
Timeframe: from baseline to 8 weeks

Interventionunits on a scale (Mean)
Cyclobenzaprine ER59
Placebo51

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Visual Analogue Pain Scale at 8 Weeks Post Treatment

Change in baseline subjective pain based on a 10 point scale (1= no pain, 10 = severe pain) from baseline (T=Zero, prior to drug/placebo treatment) to week 8 (NCT01041495)
Timeframe: 8 weeks

Interventionunits on a scale (Mean)
Cyclobenzaprine ER4.8
Placebo5.7

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Mean Plasma Concentration (AUC) of Cyclobenzaprine

Blood samples were collected pre-dose, 30 min, 1, 1.5, 2, 2.5, 3, 3.33, 3.67, 4, 4.67, 5, 5.5, 6, 8, 12, 16, 24, 36, 48, 72 and 96 hours post-dose for each treatment period. (NCT01490788)
Timeframe: 0 to 96 hours

Interventionpg.hr/mL (Mean)
Treatment A47,074.19
Treatment B94,874.26
Treatment C50,263.16

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Incidences of Adverse Events

Every adverse events occurring during the study period will be reported. (NCT01490788)
Timeframe: Continuously until the end (day 5) of each study period + 8-10 days after end of last period (total duration: about 1 month)

,,
InterventionParticipants (Count of Participants)
Subjects with Treatment-Emergent Adverse EventsSubjects with Serious Adverse EventsSubjects discontinued due to adverse event
Treatment A1400
Treatment B1500
Treatment C1000

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Change in Functional Disability as Measured by the Roland Morris Disability Questionnaire

"The Roland Morris Disability Questionnaire (RMDQ) is a 24 item instrument that evaluates the impact of low back pain on one's daily life. It is most sensitive for patients with mild to moderate disability due to acute, sub-acute or chronic low back pain. Each question can be answered as either a yes or no. The score ranges from 0 to 24 where a higher score reflects greater impairment and, therefore, worsening in the quality of life. The change in RMDQ is obtained by subtracting the RMDQ score at one week after discharge from the baseline score." (NCT01587274)
Timeframe: Baseline and one week after discharge from emergency department

Interventionunits on a scale (Median)
Opioid5
Skeletal Muscle Relaxant4
Naproxen Alone7

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Mean Change From Baseline in Weekly Average of Daily Pain Scores at Week 12

Daily pain scores were assessed using a 24-hour recall response provided by each patient via an interactive voice response system (IVRS) daily telephone diary. Average daily pain was measured using an 11-point (0-10) numerical rating scale (NRS), with higher scores representing worse pain. Jump to control was used to replace missing data in each treatment arm. (NCT01903265)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
TNX-102 SL 2.8 mg Tablets-1.39
Placebo-0.95

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Change From Baseline to Week 12 in PROMIS T-score for Sleep Disturbance

The Patient-Reported Outcome Measurement Information System (PROMIS) sleep disturbance instrument consists of 8 items in which responses are scored 1 to 5 for each item. A higher score on 5 of the 8 items reflects a worse outcome, whereas a higher score on 3 items reflects an improved outcome; therefore, the directionality of the 8 item scores are first synchronized prior to calculation of the total raw score. PROMIS scores are presented as T-scores in which the raw score has been rescaled into a standardized score with a mean of 50 and a standard deviation of 10. Higher T-scores represent more of the concept being measured (in this case, sleep disturbance). (NCT01903265)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
TNX-102 SL 2.8 mg Tablets-8.96
Placebo-5.13

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Change From Baseline to Week 12 in FIQ-R Total Score

"The Fibromyalgia Impact Questionnaire (revised) FIQ-R is made up of 3 domains: functional (9 questions), overall (2 questions) and symptoms (10 questions). All questions are based on an 11-point numerical rating scale (NRS) of 0-10, with 10 being worst. Total FIQ-R scores can range from 0-100, with higher scores reflecting worsening status. The patient's total score on the FIQ-R was assessed at Visits 2, 3, 4, 5, and 6 (Week 12). Jump to control was used to replace missing data in each treatment arm." (NCT01903265)
Timeframe: Baseline, Week 12

Interventionunits on a scale (Least Squares Mean)
TNX-102 SL 2.8 mg Tablets-15.59
Placebo-8.54

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30% Responder Analysis of IVRS NRS Pain Assessments at Week 12

"The weekly averages of daily pain scores were calculated using the daily, 24-hour-recall, IVRS NRS pain assessments.~Patients who had at least a 30% improvement from baseline to week 12 in weekly average of daily pain scores were considered responders." (NCT01903265)
Timeframe: Baseline, Week 12

Interventionpercentage of participants (Number)
TNX-102 SL 2.8 mg Tablets34
Placebo20.6

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"Patient Global Impression of Change (PGIC) Responder Status (Very Much Improved or Much Improved vs All Other Categories) at Week 12"

The PGIC is a 7-point scale (1=very much improved; 7=very much worse) that assesses the patient's perception of the overall change in his/her fibromyalgia symptoms since entering the study. Scores of 1 and 2 were considered responders. (NCT01903265)
Timeframe: Week 12

Interventionpercentage of participants (Number)
TNX-102 SL 2.8 mg Tablets30.1
Placebo16.7

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Change in Average Pain Between Baseline and Week 8 With Cyclobenzaprine Therapy

Will measure average pain using the Brief Pain Inventory at baseline and after 8 weeks of therapy with cyclobenzaprine. On the Brief Pain Inventory, average pain is reported using a 0-10 scale, with higher numbers reflecting more pain. Change is calculated by subtracting pain at baseline is from pain at 8 weeks. A positive value represents an increase in pain. (NCT01921296)
Timeframe: baseline and 8 weeks

Interventionchange in average pain (Mean)
Cyclobenzaprine-2

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Percentage of Subjects Who Continue to Take Aromatase Inhibitor Therapy

We will assess the number of patients who continue to take the original aromatase inhibitor medication at the 24 week timepoint, as assessed using patient self-report and medical records (NCT01921296)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
Cyclobenzaprine100

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Percentage of Patients That Experience Adverse Events

Persistence with cyclobenzaprine therapy for 24 weeks will be assessed using a medication diary. Safety will be assessed using CTCAE criteria (NCT01921296)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
Cyclobenzaprine100

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Number of Patients That Experience an Improvement in Sleep Quality as Assessed Using the Pittsburgh Sleep Quality Index (PSQI) With 8 Weeks of Cyclobenzaprine Therapy.

Will measure sleep quality using the Pittsburgh Sleep Quality Index at baseline and after 8 weeks of therapy with cyclobenzaprine. A total score is calculated for the Pittsburgh Sleep Quality Index. The total score ranges from 0-21, with higher scores representing worse sleep quality. Any reduction in PSQI total score was considered an improvement. (NCT01921296)
Timeframe: 8 weeks

Interventionparticipant (Number)
Cyclobenzaprine1

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Change in Fatigue Between Baseline and Week 8 With Cyclobenzaprine Therapy

Will measure fatigue using the PROMIS fatigue questionnaire at baseline and after 8 weeks of therapy with cyclobenzaprine. The PROMIS Fatigue 7a score was calculated according to the information provided on the website. The raw score ranges from 7-35. The raw score is then converted to a T score according to the instruction on the website, with higher scores representing more fatigue. The T score rescales the raw score into a standardized score with a mean of 50 and a standard deviation of 10. The change in fatigue is calculated by subtracting the T score at baseline from the T score at 8 weeks. Positive values represent worsening of fatigue. (NCT01921296)
Timeframe: baseline and 8 weeks

Interventionchange in T score (Mean)
Cyclobenzaprine1.3

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Newly-emergent Adverse Events (NEAEs) During Treatment With TNX-102 SL Tablets Taken Daily at Bedtime Over 12 Months in Patients With Fibromyalgia.

NEAEs and Serious Adverse events (SAEs) were collected and are coded using the latest version of the Medical Dictionary for Regulatory Activities (MedDRA). (NCT02015234)
Timeframe: Up to 12 months

,
InterventionParticipants (Count of Participants)
Patient with at least 1 NEAE reportedPatients withdrew due to NEAEPatient with at least 1 SAE
Placebo - TNX-102 SL 2.8 mg60183
TNX-102 SL 2.8 mg - TNX-102 SL 2.8 mg5495

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Responder Analysis of Patient's Global Impression of Change (PGIC)

"PGIC is a fibromyalgia-specific validated instrument to gauge the patient's assessment of change in condition.The scores are categorized as provided below. A responder was defined by a score of 1 (very much improved), or 2 (much improved).~= Very much improved~= Much improved~= Minimally improved~= No change~= Minimally worse~= Much worse~= Very much worse" (NCT02015234)
Timeframe: Months 1, 3, 6, 9, 12

InterventionParticipants (Count of Participants)
Month 172182920Month 172182923Month 372182920Month 372182923Month 672182920Month 672182923Month 972182920Month 972182923Month 1272182920Month 1272182923
Score 1 or 2Scores 3 to 7
Placebo - TNX-102 SL 2.8 mg16
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg25
Placebo - TNX-102 SL 2.8 mg63
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg54
Placebo - TNX-102 SL 2.8 mg23
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg29
Placebo - TNX-102 SL 2.8 mg56
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg50
Placebo - TNX-102 SL 2.8 mg22
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg26
Placebo - TNX-102 SL 2.8 mg57
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg53
Placebo - TNX-102 SL 2.8 mg21
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg27
Placebo - TNX-102 SL 2.8 mg58
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg52
Placebo - TNX-102 SL 2.8 mg17
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg32
Placebo - TNX-102 SL 2.8 mg62
TNX-102 SL 2.8mg - TNX-102 SL 2.8 mg47

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Change From Baseline in Numerical Rating Scale (NRS) Assessments of Average Pain Based on a 7 Day Recall

The NRS for average pain over the past 7 days was an 11-point scale (0=no pain → 10=worst pain imaginable) that was assessed on a 7-day recall basis. (NCT02015234)
Timeframe: Month 1, 3, 6, 9, 12

,
InterventionScores on a scale (Mean)
BaselineChange at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12
Placebo - TNX-102 SL 2.8 mg5.7-0.8-0.6-0.7-0.40.0
TNX-102 SL 2.8 mg - TNX-102 SL 2.8 mg4.80.10.10.20.00.2

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Change From Baseline in Numerical Rating Scale (NRS) Assessments of Average Pain Based on 24 Hour Recall

The NRS for average pain was an 11-point scale (0=no pain → 10=worst pain imaginable) that was assessed on a 24-hour recall basis. (NCT02015234)
Timeframe: Months 1, 3, 6, 9 and 12.

,
InterventionScores on a scale (Mean)
BaselineChange at Month 1Change at Month 3Change at Month 6Change at Month 9Change at Month 12
Placebo - TNX-102 SL 2.8 mg5.6-0.5-0.5-0.7-0.60.1
TNX-102 SL 2.8 mg - TNX-102 SL 2.8 mg5.0-0.2-0.3-0.20.0-0.0

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Percentage of Participants With Physician's Clinical Global Assessment on Days 7 and 15 of Treatment

"The investigator assessed their clinical global impression of change compared to Baseline, based on physical examination, degree of muscle spasm (presence of muscle spasm assessment), reaction to palpation (presence of local pain assessment), limitation of range of motion, and evaluation of the patient's reported functional assessment (limitation of activities of daily living assessment). The following 5-point rating scale was used: 1 = worse, 2 = no change, 3 = slight improvement, 4 = moderate improvement, 5 = marked improvement." (NCT02814565)
Timeframe: Days 7 and 15

,
Interventionpercentage of participants (Number)
Day 7, 1=worseDay 7, 2=no changeDay 7, 3=slight improvementDay 7, 4=moderate improvementDay 7, 5=marked improvementDay 15, 1=worseDay 15, 2=no changeDay 15, 3=slight improvementDay 15, 4=moderate improvementDay 15, 5=marked improvement
Cyclobenzaprine HCl 15 mg2.28.952.227.88.91.15.627.830.035.6
Placebo0.026.744.424.44.41.111.134.432.221.1

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Percentage of Participants With Physician's Clinical Global Assessment on Day 3 of Treatment

"The investigator assessed their clinical global impression of change compared to Baseline, based on physical examination, degree of muscle spasm (presence of muscle spasm assessment), reaction to palpation (presence of local pain assessment), limitation of range of motion, and evaluation of the patient's reported functional assessment (limitation of activities of daily living assessment). The following 5-point rating scale was used: 1 = worse, 2 = no change, 3 = slight improvement, 4 = moderate improvement, 5 = marked improvement." (NCT02814565)
Timeframe: Day 3

,
Interventionpercentage of participants (Number)
Day 3, 1=worseDay 3, 2=no changeDay 3, 3=slight improvementDay 3, 4=moderate improvementDay 3, 5=marked improvement
Cyclobenzaprine HCl 15 mg1.152.235.611.10.0
Placebo0.068.925.63.32.2

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Percentage of Participants With Subject's Rating of Medication Helpfulness Impression on Day 3 of Treatment

"Participants assessed the study medication helpfulness on a daily basis (in the daily diary), using the following 5-point rating scale: How would you rate this study medication in improving your condition? 0 = poor, 1 = fair, 2 = good, 3 = very good, 4 = excellent." (NCT02814565)
Timeframe: Day 3

,
Interventionpercentage of participants (Number)
Day 3, 0=poorDay 3, 1=fairDay 3, 2=goodDay 3, 3=very goodDay 3, 4=excellent
Cyclobenzaprine HCl 15 mg20.060.016.73.30.0
Placebo28.946.722.22.20.0

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Percentage of Participants With Physician Rated Assessment of Presence of Muscle Spasm on Days 3, 7, and 15 of Treatment

"The investigator assessment based on physical examination, presence of muscle spasm (presence of muscle spasm assessment). The following 5-point rating scale was used: 1 = none, 2 = mild, 3 = moderate, 4 = moderately severe, 5 = severe." (NCT02814565)
Timeframe: Days 3, 7, and 15

,
Interventionpercentage of participants (Number)
Day 3, 1=noneDay 3, 2=mildDay 3, 3=moderateDay 3, 4=moderately severeDay 3, 5=severeDay 7, 1=noneDay 7, 2=mildDay 7, 3=moderateDay 7, 4=moderately severeDay 7, 5=severeDay 15, 1=noneDay 15, 2=mildDay 15, 3=moderateDay 15, 4=moderately severeDay 15, 5=severe
Cyclobenzaprine HCl 15 mg2.227.862.27.80.014.447.837.80.00.048.937.813.30.00.0
Placebo2.221.166.710.00.05.653.338.92.20.032.247.820.00.00.0

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Percentage of Participants With Physician Rated Assessment of Presence of Local Pain on Days 3, 7, and 15 of Treatment

"The investigator assessed local pain based on physical examination, reaction to palpation (presence of local pain assessment). The following 5-point rating scale was used: 1 = none, 2 = mild, 3 = moderate, 4 = moderately severe, 5 = severe." (NCT02814565)
Timeframe: Days 3, 7, and 15

,
Interventionpercentage of participants (Number)
Day 3, 1=noneDay 3, 2=mildDay 3, 3=moderateDay 3, 4=moderately severeDay 3, 5=severeDay 7, 1=noneDay 7, 2=mildDay 7, 3=moderateDay 7, 4=moderately severeDay 7, 5=severeDay 15, 1=noneDay 15, 2=mildDay 15, 3=moderateDay 15, 4=moderately severeDay 15, 5=severe
Cyclobenzaprine HCl 15 mg1.124.466.77.80.06.755.636.71.10.035.651.112.21.10.0
Placebo1.121.166.711.10.02.250.046.71.10.025.650.024.40.00.0

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Percentage of Participants With Physician Rated Assessment of Limitation of Range of Motion on Days 3, 7, and 15 of Treatment

"The investigator assessed limitation of range of motion. The following 5-point rating scale was used: 1 = none, 2 = mild, 3 = moderate, 4 = moderately severe, 5 = severe." (NCT02814565)
Timeframe: Days 3, 7, and 15

,
Interventionpercentage of participants (Number)
Day 3, 1=noneDay 3, 2=mildDay 3, 3=moderateDay 3, 4=moderately severeDay 3, 5=severeDay 7, 1=noneDay 7, 2=mildDay 7, 3=moderateDay 7, 4=moderately severeDay 7, 5=severeDay 15, 1=noneDay 15, 2=mildDay 15, 3=moderateDay 15, 4=moderately severeDay 15, 5=severe
Cyclobenzaprine HCl 15 mg6.740.047.85.60.022.251.126.70.00.044.448.96.70.00.0
Placebo4.437.852.25.60.013.351.135.60.00.038.947.813.30.00.0

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Percentage of Participants With Physician Rated Assessment of Limitation of Activities of Daily Living on Days 3, 7, and 15 of Treatment

"The investigator assessed limitation of activities based on evaluation of the patient's reported functional assessment. The following 5-point rating scale was used: 1 = none, 2 = mild, 3 = moderate, 4 = moderately severe, 5 = severe." (NCT02814565)
Timeframe: Days 3, 7, and 15

,
Interventionpercentage of percentage (Number)
Day 3, 1=noneDay 3, 2=mildDay 3, 3=moderateDay 3, 4=moderately severeDay 3, 5=severeDay 7, 1=noneDay 7, 2=mildDay 7, 3=moderateDay 7, 4=moderately severeDay 7, 5=severeDay 15, 1=noneDay 15, 2=mildDay 15, 3=moderateDay 15, 4=moderately severeDay 15, 5=severe
Cyclobenzaprine HCl 15 mg4.446.746.72.20.018.962.217.81.10.050.045.64.40.00.0
Placebo5.650.038.95.60.010.063.326.70.00.041.153.35.60.00.0

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Percentage of Responders on Days 3, 7, and 14 of Treatment

"A responder was defined as a participant who had both a rating of either very good or excellent for the participant's rating of medication helpfulness." (NCT02814565)
Timeframe: Days 3, 7, and 14

,
Interventionpercentage of participants (Number)
Day 3Day 7Day 14
Cyclobenzaprine HCl 15 mg3.315.640.0
Placebo2.214.431.1

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Percentage of Participants With Subject's Rating of Medication Helpfulness Impression on Days 7 and 14 of Treatment

"Participants assessed the study medication helpfulness on a daily basis (in the daily diary), using the following 5-point rating scale: How would you rate this study medication in improving your condition? 0 = poor, 1 = fair, 2 = good, 3 = very good, 4 = excellent." (NCT02814565)
Timeframe: Days 7 and 14

,
Interventionpercentage of participants (Number)
Day 7, 0=poorDay 7, 1=fairDay 7, 2=goodDay 7, 3=very goodDay 7, 4=excellentDay 14, 0=poorDay 14, 1=fairDay 14, 2=goodDay 14, 3=very goodDay 14, 4=excellent
Cyclobenzaprine HCl 15 mg7.841.135.613.32.28.925.625.622.217.8
Placebo16.734.434.411.13.314.425.628.920.011.1

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Percentage of Participants With Subject-Rated Global Impression on Days 3, 7, and 14 of Treatment

"Participants assessed their clinical global impression based on relief from local pain, restriction in activities of daily living, restriction of movement and intensity of local pain on a daily basis. The following 5-point rating scale was used: 1 = worse, 2 = no change, 3 = slight improvement, 4 = moderate improvement, 5 = marked improvement." (NCT02814565)
Timeframe: Days 3, 7, and 14

,
Interventionpercentage of participants (Number)
Day 3, 1=worseDay 3, 2=no changeDay 3, 3=slight improvementDay 3, 4=moderate improvementDay 3, 5=marked improvementDay 7, 1=worseDay 7, 2=no changeDay 7, 3=slight improvementDay 7, 4=moderate improvementDay 7, 5=marked improvementDay 14, 1=worseDay 14, 2=no changeDay 14, 3=slight improvementDay 14, 4=moderate improvementDay 14, 5=marked improvement
Cyclobenzaprine HCl 15 mg3.345.647.83.30.04.413.352.222.27.81.114.424.427.832.2
Placebo1.156.733.37.81.11.125.643.325.64.41.126.720.028.923.3

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Mean Plasma Concentration (AUC) of Cyclobenzaprine

Blood samples were collected prior to drug administration and 0.083 (5 min), 0.167 (10 min),0.333 (20 min), 0.500 (30 min), 0.750 (45 min), 1.00, 1.50, 2.00, 2.50, 3.00, 3.33, 3.67, 4.00, 4.33, 4.67, 5.00, 5.50, 6.00, 8.00, 12.0, 16.0, 24.0, 36.0, 48.0, 72.0, and 96.0 hours post-dose in each period. (NCT03168022)
Timeframe: 0 to 96 hours

Interventionpg*h/mL (Mean)
Treatment A70066.90
Treatment B64711.53

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Number of Subjects With Treatment-emergent Adverse Events (TEAEs) of Treatment A and Treatment B, Administered as 1 x 2.8 mg TNX-102 SL Under Fasting Conditions.

The MedDRA® dictionary was used to classify all TEAEs reported during the study by System Organ Class (SOC) and Preferred Term (PT). (NCT03168022)
Timeframe: Continuously until the end (day 5) of each study period + 8-10 days after end of last period (total duration: about 1 month)

InterventionParticipants (Count of Participants)
Treatment A18
Treatment B19

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Sleepiness Endpoint Karolinska Sleepiness Scale KSS

assessment of self-reported motivation for driving performance where 1 equals alert and 9 equals extremely sleepy (NCT03353922)
Timeframe: at Tmax on Day 1

Interventionunits on a scale (Mean)
Tolperisone HCl 150 mg3.3
Placebo Oral Tablet3.4
Cyclobenzaprine 10 mg Oral Tablet5.6

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Steady State Standard Deviation of Lateral Position (SDLP) Day 3

SDLP measured on Day 3 at steady state following 3 days of dosing three times per day to achieve steady state drug concentration and effect on outcomes (NCT03353922)
Timeframe: Day 3

Interventioncm deviation from lateral position (Mean)
Tolperisone HCl 150 mg29.8
Placebo Oral Tablet29.6
Cyclobenzaprine 10 mg Oral Tablet31.7

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Standard Deviation of Lateral Position (SDLP)

In this crossover study, treatment effects were assessed following initial dose, the morning following nighttime dosing (to assess residual next day effects), and at steady state (i.e., following AM dosing on Day 3). (NCT03353922)
Timeframe: at time of peak concentration of drug (Tmax) on Day 1

Interventioncm of deviation of lateral position (Mean)
Tolperisone HCl 150 mg29.3
Placebo Oral Tablet29.7
Cyclobenzaprine 10 mg Oral Tablet38.6

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Change From Baseline to Week 14 in the Fibromyalgia Impact Questionnaire - Revised (FIQR) Symptoms Domain Score

The FIQ-R is a validated questionnaire. Scores on the symptoms domain range from 0 to 100 where a higher score means worse outcome. (NCT04172831)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablets, 5.6 mg-18.4
Placebo SL Tablet-14.0

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Change From Baseline to Week 14 in the FIQR Function Domain Score

The FIQ-R is a validated questionnaire. Scores on the function domain range from 0 to 90 where a higher score means worse outcome. (NCT04172831)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablets, 5.6 mg-13.6
Placebo SL Tablet-9.3

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Change From Baseline to Week 14 in the Numerical Rating Scale (NRS) Weekly Average of Daily Self-reported Average Pain Severity Scores.

Patients provide a daily numeric assessment of their average pain (24-hour recall), via an electronic diary, using an 11-point NRS. Scores range from 0 (no pain) to 10 (worst possible pain). (NCT04172831)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablets, 5.6 mg-1.9
Placebo SL Tablet-1.5

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Change From Baseline to Week 14 in the Patient Reported Outcomes Measurement Information System (PROMIS) Score for Sleep Disturbance

The PROMIS Sleep disturbance short form 8a consists of 8 questions on a 5-point scale (1 to 5) where a higher score indicates a worse outcome. The total score is reported on a range of 8 to 40. (NCT04172831)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablets, 5.6 mg-9.5
Placebo SL Tablet-6.5

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Change From Baseline to Week 14 in the PROMIS Score for Fatigue

The PROMIS fatigue short form 8a consists of 8 questions on a 5 point scale (1 to 5) where a higher score indicates a worse outcome. The total score is reported on a range of 8 to 40. (NCT04172831)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablets, 5.6 mg-8.0
Placebo SL Tablet-6.2

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Change From Baseline to Week 14 in the Weekly Average of the Daily Diary Assessment of Sleep Quality

Patients provide a daily numeric assessment of their sleep quality for the previous night, via an electronic diary, using an 11-point NRS. Scores range from 0 (best possible sleep) to 10 (worst possible sleep). (NCT04172831)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablets, 5.6 mg-2.0
Placebo SL Tablet-1.5

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"Number of Patients With a Patient's Global Impression of Change (PGIC) Rating of Very Much Improved or Much Improved"

The PGIC is a fibromyalgia specific validated instrument on a scale of 1 to 7, where a score of 1 indicates the highest level of improvement and a score of 7 indicates a much worse outcome. (NCT04172831)
Timeframe: 14 weeks

InterventionParticipants (Count of Participants)
TNX-102 SL Tablets, 5.6 mg93
Placebo SL Tablet75

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"Number of Patients With a Patient's Global Impression of Change (PGIC) Rating of Very Much Improved or Much Improved"

The PGIC is a fibromyalgia specific validated instrument on a scale of 1 to 7, where a score of 1 indicates the highest level of improvement and a score of 7 indicates a much worse outcome. (NCT04508621)
Timeframe: 14 weeks

InterventionParticipants (Count of Participants)
TNX-102 SL Tablet, 5.6 mg76
Placebo SL Tablet56

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Change From Baseline to Week 14 in the FIQ-R Function Domain Score

The FIQ-R is a validated questionnaire. Score on the function domain range from 0 to 90 where a higher score means worse outcome. (NCT04508621)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablet, 5.6 mg-8.8
Placebo SL Tablet-8.4

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Change From Baseline to Week 14 in the Numerical Rating Scale (NRS) Weekly Average of Daily Self-reported Average Pain Severity Scores.

Patients provide a daily numeric assessment of their average pain (24-hour recall), via an electronic diary, using an 11-point NRS. Scores range from 0 (no pain) to 10 (worst possible pain). (NCT04508621)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablet, 5.6 mg-1.6
Placebo SL Tablet-1.3

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Change From Baseline to Week 14 in the Patient Reported Outcomes Measurement Information System (PROMIS) Score for Sleep Disturbance

The PROMIS Sleep disturbance short form 8a consists of 8 questions on a 5-point scale (1 to 5) where a higher score indicates a worse outcome. The total score is reported on a range of 8 to 40. (NCT04508621)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablet, 5.6 mg-7.4
Placebo SL Tablet-5.1

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Change From Baseline to Week 14 in the PROMIS Score for Fatigue

The PROMIS fatigue short form 8a consist of 8 questions on a 5-point scale (1 to 5) where a higher score indicates a worse outcome. The total score is reported on a range of 8 to 40. (NCT04508621)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablet, 5.6 mg-6.6
Placebo SL Tablet-5.4

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Change From Baseline to Week 14 in the Weekly Average of the Daily Diary Assessment of Sleep Quality

Patients provide a daily numeric assessment of their sleep quality for the previous night, via an electronic diary, using an 11-point NRS. Scores range from 0 (best possible sleep) to 10 (worst possible sleep). (NCT04508621)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablet, 5.6 mg-1.5
Placebo SL Tablet-1.3

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Change From Baseline to Week 14 in the Fibromyalgia Impact Questionnaire - Revised (FIQ-R) Symptoms Domain Score.

The FIQ-R is a validated questionnaire. Scores on the symptoms domain range from 0 to 100 where a higher score means worse outcome. (NCT04508621)
Timeframe: 14 weeks

Interventionscore on a scale (Least Squares Mean)
TNX-102 SL Tablet, 5.6 mg-15.3
Placebo SL Tablet-12.0

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