Page last updated: 2024-11-04

tolperisone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Tolperisone: A centrally acting muscle relaxant that has been used for the symptomatic treatment of spasticity and muscle spasm. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1211) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5511
CHEMBL ID1076211
CHEBI ID93835
SCHEMBL ID148499
MeSH IDM0021637

Synonyms (87)

Synonym
AC-12150
5-20-02-00357 (beilstein handbook reference)
unii-f5eom0ld8e
tolperisona
tolperisonum
f5eom0ld8e ,
BRD-A27732521-003-02-6
KBIO1_000288
DIVK1C_000288
2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one
SPECTRUM_001960
brn 1285666
tolperisone [inn:ban]
propiophenone, 2,4'-dimethyl-3-piperidino-
tolperisona [inn-spanish]
einecs 211-976-4
nsc 107321
tolperisonum [inn-latin]
IDI1_000288
BCBCMAP01_000036
SPECTRUM5_001115
menopatol
nsc107321
atmosgen (free base)
mideton
roystajin (free base)
1-propanone, 2-methyl-1-(4-methylphenyl)-3-(1-piperidinyl)-
728-88-1
1-piperidino-2-methyl-3-(p-tolyl)-3-propanone
besnoline (free base)
mydocalm
2,4'-dimethyl-3-piperidinopropiophenone
wln: t6ntj a1y1&vr d1
nsc-107321
mydeton
2-methyl-3-piperidino-1-p-tolylpropan-1-one
propiophenone,4'-dimethyl-3-piperidino-
tolperisone
BSPBIO_003446
KBIOSS_002514
KBIOGR_000772
KBIO2_005074
KBIO2_002506
KBIO3_002666
KBIO2_007642
SPECTRUM2_000851
SPBIO_000861
SPECTRUM4_000276
NINDS_000288
SPECTRUM3_001743
NCGC00178060-01
fskfpvlpfljrqb-uhfffaoysa-
2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydrochloride
inchi=1/c16h23no/c1-13-6-8-15(9-7-13)16(18)14(2)12-17-10-4-3-5-11-17/h6-9,14h,3-5,10-12h2,1-2h3
AKOS000281128
musclex (tn)
tolperisone (inn)
D08617
n-553 free base
CHEMBL1076211
n-553 [as hydrochloride]
mydetone
2-methyl-3-(piperidin-1-yl)-1-p-tolylpropan-1-one
A19106
2-methyl-1-(4-methylphenyl)-3-(1-piperidinyl)-1-propanone
tolperisone [who-dd]
tolperisone [mi]
tolperisone [inn]
AKOS022350563
SCHEMBL148499
2-methyl-1-(4-methylphenyl)-3-(1-piperidinyl)-1-propanone #
dl-tolperisone
W-104475
AB00053613_02
AB00053613_03
DTXSID8023686
2-methyl-1-(4-methylphenyl)-3-(piperidin-1-yl)propan-1-one
STL483404
CHEBI:93835
tolperison
SBI-0051686.P002
NCGC00178060-04
tolperisone free base
2-methyl-3-(piperidin-1-yl)-1-(p-tolyl)propan-1-one
DB06264
Q369648
bdbm442744

Research Excerpts

Overview

Tolperisone is a nonopioid, centrally acting muscle relaxant in clinical development in the USA for the treatment of symptoms associated with acute, painful muscles spasms of the back. It acts by blocking voltage-gated sodium and calcium channels. Tolperis one is a safe, effective and non sedative alternative in management of acute painful spasm conditions.

ExcerptReferenceRelevance
"Tolperisone is a centrally acting muscle relaxant under development in the United States as a treatment for acute and painful symptoms of muscle spasms. "( An assessment of the centrally acting muscle relaxant tolperisone on driving ability and cognitive effects compared to placebo and cyclobenzaprine.
Caron, J; Halseth, A; Kay, G; Kaye, R; Wessel, T, 2020
)
2.25
"Tolperisone is a nonopioid, centrally acting muscle relaxant in clinical development in the USA for the treatment of symptoms associated with acute, painful muscles spasms of the back. "( RESUME-1: a Phase III study of tolperisone in the treatment of painful, acute muscle spasms of the back.
Kaye, R; Torres, K; Vaughan, SA, 2022
)
2.45
"Tolperisone is a voltage gated sodium channel blocker, centrally acting muscle relaxant drug, with a very advantageous side effect profile. "( Effect of tolperisone on the resting brain and on evoked responses, an phMRI BOLD study.
Deli, L; Gajári, D; Gőcze, KZ; Kocsis, P; Pozsgay, Z; Tihanyi, K, 2013
)
2.23
"Tolperisone is a centrally acting muscle relaxant that acts by blocking voltage-gated sodium and calcium channels. "( Acute toxicity profile of tolperisone in overdose: Observational poison centre-based study.
Ceschi, A; Hofer, KE; Kupferschmidt, H; Martos, V; Rauber-Lüthy, C; Schenk-Jaeger, KM, 2015
)
2.16
"Tolperisone (Mydocalm) is a centrally acting muscle relaxant with few sedative side effects that is used for the treatment of chronic pain conditions. "( Fatal tolperisone poisoning: autopsy and toxicology findings in three suicide cases.
Augsburger, MP; Brunel, C; Mangin, P; Sporkert, F, 2012
)
2.3
"Tolperisone is a safe, effective and non sedative alternative in management of acute painful spasm conditions associated with degenerative or inflammatory diseases of the musculoskeletal system. "( A phase IV observational multi-centre, open-label study on efficacy and safety of tolperisone 150 mg in patients with painful muscle spasm associated with degenerative or inflammatory diseases of the musculoskeletal system.
Keny, S; Prabhoo, R; Prabhoo, T; Rana, R; Singh, A, 2011
)
2.04

Toxicity

Tolperisone was proved to be a safe & effective alternative to skeletal muscle relaxants in the management of acute painful spasm conditions associated with degenerative or inflammatory diseases of the musculoskeletal system.

ExcerptReferenceRelevance
" Adverse events occurred less often on active treatment (n = 19) than on placebo (n = 26) and were mostly of mild-to-moderate intensity."( A randomized, double-blind, placebo-controlled study of the efficacy and safety of tolperisone in spasticity following cerebral stroke.
Hansen, C; Horvath, F; Koytchev, R; Kuhn, K; Pongratz, D; Ramm, S; Stamenova, P, 2005
)
0.55
" Their use is frequently associated with dose-limiting adverse effects."( Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.
Berzsenyi, P; Farkas, S; Kárpáti, E; Kocsis, P; Tarnawa, I,
)
0.13
" For detecting side effect liability (ataxia, sedation, impairment of voluntary motor functions), (1) the rota-rod test, (2) measurement of spontaneous motility, (3) the weight-lifting test and (4) the thiopental sleep test were used."( Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.
Berzsenyi, P; Farkas, S; Kárpáti, E; Kocsis, P; Tarnawa, I,
)
0.13
"Therapeutic indices calculated from the results of these in vivo experiments for the clinically used muscle relaxants are in agreement with their adverse effect profiles in humans."( Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.
Berzsenyi, P; Farkas, S; Kárpáti, E; Kocsis, P; Tarnawa, I,
)
0.13
" Adverse events occurred less often on active treatment (n=19) than on placebo (n=26) and were mostly of mild-to-moderate intensity."( [A randomized, double blind, placebo-controlled study of the efficacy and safety of tolperisone in spasticity following cerebral stroke].
Hanasen, C; Horvath, F; Koytchev, R; Kuhn, K; Pongratz, D; Ramm, S; Stamenova, P, 2006
)
0.56
" Adverse events were monitored for safety and global efficacy assessment was done by clinicians and patients at the end of study period."( A phase IV observational multi-centre, open-label study on efficacy and safety of tolperisone 150 mg in patients with painful muscle spasm associated with degenerative or inflammatory diseases of the musculoskeletal system.
Keny, S; Prabhoo, R; Prabhoo, T; Rana, R; Singh, A, 2011
)
0.59
" The incidence of common adverse effects like nausea, gastric irritation was less than 2%."( A phase IV observational multi-centre, open-label study on efficacy and safety of tolperisone 150 mg in patients with painful muscle spasm associated with degenerative or inflammatory diseases of the musculoskeletal system.
Keny, S; Prabhoo, R; Prabhoo, T; Rana, R; Singh, A, 2011
)
0.59
" In this open-labelled, non-comparative, prospective study tolperisone was proved to be a safe & effective alternative to skeletal muscle relaxants in the management of acute painful spasm conditions associated with degenerative or inflammatory diseases of the musculoskeletal system."( A phase IV observational multi-centre, open-label study on efficacy and safety of tolperisone 150 mg in patients with painful muscle spasm associated with degenerative or inflammatory diseases of the musculoskeletal system.
Keny, S; Prabhoo, R; Prabhoo, T; Rana, R; Singh, A, 2011
)
0.84
" Adverse events in the mydocalm group have been identified more rarely than in the control group."( [Evaluation of efficacy and safety of mydocalm in the early rehabilitation of stroke].
Kovalchuk, VV, 2013
)
0.39
" Based on the results, tolpersione injection and per os formulations can be considered an effective and safe drugs in the combined therapy for patients with acute nonspecific back pain."( [Results of a randomized double blind parallel study on the efficacy and safety of tolpersione in patients with acute nonspecific low back pain].
Brylev, LV; Chefranova, ZY; Guekht, AB; Kukushkin, ML; Laskov, VB; Makarov, NS; Pizova, NV; Sholomov, II; Sokov, EL,
)
0.13
" The objectives of this study were to compare the efficacy and adverse effects of tolperisone compared to baclofen among patients with spasticity associated with spinal cord injury."( Efficacy and safety of tolperisone versus baclofen among Chinese patients with spasticity associated with spinal cord injury: a non-randomized retrospective study.
Chen, R; Fang, S; Huang, Y; Li, M; Liu, N, 2021
)
1.16

Pharmacokinetics

Oral tolperisone hydrochloride was tested in healthy volunteers. Very large interindividual differences in the AUC and Cmax were detected.

ExcerptReferenceRelevance
"The aim of this study was to determine the pharmacokinetic profiles of oral tolperisone hydrochloride in healthy volunteers."( Considerable interindividual variation in the pharmacokinetics of tolperisone HCl.
Bae, JW; Jang, CG; Kim, MJ; Lee, SY; Myung, CS; Park, YS, 2007
)
0.81
"Very large interindividual differences in the AUC and Cmax were detected after oral tolperisone HCl."( Considerable interindividual variation in the pharmacokinetics of tolperisone HCl.
Bae, JW; Jang, CG; Kim, MJ; Lee, SY; Myung, CS; Park, YS, 2007
)
0.8
" We aimed to identify the influence of polymorphism of two main enzymes (CYP2D6 and CYP2C19) on pharmacokinetic profile of parent drug."( Influence of CYP2D6 and CYP2C19 genetic polymorphism on the pharmacokinetics of tolperisone in healthy volunteers.
Bogiel, M; Duda, J; Pawlowska, M; Sieradzki, E, 2015
)
0.64
" Although CYP2C19 *1/*2 subjects had higher AUCt, AUC(inf), and Cmax values than *1/*1, no statistically significant differences were observed."( Influence of CYP2D6 and CYP2C19 genetic polymorphism on the pharmacokinetics of tolperisone in healthy volunteers.
Bogiel, M; Duda, J; Pawlowska, M; Sieradzki, E, 2015
)
0.64

Compound-Compound Interactions

ExcerptReferenceRelevance
"A randomized double-blind study of the efficacy of midocalm combined with tractional therapy has been carried out in 24 patients (indexed group) comparing to the tractional therapy without midocalm (the drug has been substituted with placebo) in 25 patients (comparison group)."( [Use of local injections of tolperisone (midocalm) in combination with tractional therapy in the treatment of vertebral static syndrome].
Kutarev, RV; Shelkov, SN; Suslov, SA; Zakharov, IaIu, 2007
)
0.63

Bioavailability

ExcerptReferenceRelevance
"High variability (exceeded 100%) of main bioavailability parameters (AUCt, AUC(inf), C(max)) was observed in the whole group of subjects."( Influence of CYP2D6 and CYP2C19 genetic polymorphism on the pharmacokinetics of tolperisone in healthy volunteers.
Bogiel, M; Duda, J; Pawlowska, M; Sieradzki, E, 2015
)
0.64
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"Mydocalm was used for the treatment of 31 patients, mean age 45 +/- 4 years, with chronic headache of tension in a dosage of 150 mg 3 times per day during 4 weeks."( [A study of mydocalm efficiency in the treatment of chronic headache of tension].
Akarachkova, ES; Gordeev, SA; Solov'eva, AD, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)1.00000.00001.23808.1590AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.45600.00020.725710.0000AID625202
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.01300.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.00560.00000.490110.0000AID625223
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (16)

Processvia Protein(s)Taxonomy
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (156)

TimeframeStudies, This Drug (%)All Drugs %
pre-199043 (27.56)18.7374
1990's25 (16.03)18.2507
2000's48 (30.77)29.6817
2010's27 (17.31)24.3611
2020's13 (8.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 87.98

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 Index87.98 (24.57)
Research Supply Index5.27 (2.92)
Research Growth Index4.52 (4.65)
Search Engine Demand Index156.23 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (87.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials30 (18.29%)5.53%
Reviews7 (4.27%)6.00%
Case Studies10 (6.10%)4.05%
Observational2 (1.22%)0.25%
Other115 (70.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (8)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
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 1 Crossover Study of Single and Multiple Dose Pharmacokinetics, and Dose Linearity, of Tolperisone in Healthy Subjects [NCT04465266]Phase 127 participants (Actual)Interventional2020-07-28Completed
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
The Prognostic Value of Biomarkers and the Effect of Tolperisone in Acute Low Back Pain -BETA. A Phase 3 Investigator Initiated Study [NCT05544656]Phase 3150 participants (Anticipated)Interventional2019-12-13Recruiting
AV650-014: A Four Week, Prospective, Randomized, Double Blind, Placebo-Controlled Trial to Assess Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of AV650 in Patients With Spasticity Due to Spinal Cord Injury [NCT00531466]Phase 2120 participants (Anticipated)Interventional2007-09-30Terminated
AV650-018: A Two-Part (Double-Blind Followed by Open-Label), Placebo Controlled, Randomized Trial to Assess the Safety, Tolerability, and Preliminary Efficacy of AV650 (Tolperisone HCl) in Subjects With Spasticity Associated With Multiple Sclerosis [NCT00532532]Phase 2150 participants (Anticipated)Interventional2007-09-30Terminated
A Phase 3, 14-Day, Double-blind, Randomized, Placebo-Controlled, Multicenter Study of the Efficacy and Safety of Tolperisone in Subjects With Pain Due to Acute Back Muscle Spasm [NCT04671082]Phase 31,004 participants (Actual)Interventional2020-12-15Completed
Dose Ranging Study of Tolperisone in Acute Muscle Spasm of the Back [NCT03802565]Phase 2415 participants (Actual)Interventional2019-02-01Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT03353922 (4) [back to overview]Sleepiness Endpoint Karolinska Sleepiness Scale KSS
NCT03353922 (4) [back to overview]Standard Deviation of Lateral Position (SDLP)
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]Steady State Standard Deviation of Lateral Position (SDLP) Day 3
NCT03802565 (1) [back to overview]Mean Effect Size in Subjected-Rated Pain

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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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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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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Mean Effect Size in Subjected-Rated Pain

"Mean effect size between Tolperisone and Placebo of subject-rated pain due to acute back spasm using a Numerical Rating Scale (NRS; 0-10 scale, from no pain to worst possible pain) on Day 14 right now." (NCT03802565)
Timeframe: Day 1 to Day 14

Interventionscore on a scale (Mean)
Tolperisone 50 mg-4.2
Tolperisone 100 mg-4.0
Tolperisone 150 mg-3.7
Tolperisone 200 mg-4.4
Placebo-3.5

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