Page last updated: 2024-12-05

metaxalone

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

Metaxalone is a muscle relaxant that is used to treat muscle spasms. It works by blocking nerve impulses in the brain that cause muscle spasms. Metaxalone is available by prescription only. Metaxalone is a synthetic compound, meaning that it is not found naturally in the body. It was first synthesized in the 1960s. Metaxalone is a white to off-white crystalline powder that is soluble in water. It is usually taken by mouth. The most common side effects of metaxalone are drowsiness, dizziness, and headache. Metaxalone can interact with other medications, so it is important to tell your doctor about all the medications you are taking before starting metaxalone. Metaxalone is a Schedule IV controlled substance. This means that it has a potential for abuse and addiction. It is important to take metaxalone only as prescribed by your doctor. Metaxalone is studied because it is a relatively safe and effective treatment for muscle spasms. Researchers are also looking into the potential uses of metaxalone for other conditions, such as fibromyalgia and chronic pain.'

Cross-References

ID SourceID
PubMed CID15459
CHEMBL ID1079604
CHEBI ID6797
SCHEMBL ID34908
MeSH IDM0057494

Synonyms (146)

Synonym
AKOS009035315
BRD-A94709349-001-02-6
methaxalonum
5-(3,5-xyloloxymethyl)oxazolidin-2-one
5-[(3,5-dimethylphenoxy)methyl]-2-oxazolidinone
metazolone
methoxolone
metazalone
2-oxazolidinone,5-dimethylphenoxy)methyl]-
ahr-438
mls003106749 ,
2-oxazolidinone,5-xylyloxy)methyl]-
metaxalon
nsc-170959
zorane
wln: t5mvotj d1or c1 e1
5-[(3,5-xylyloxy)methyl]-2-oxazolidinone
nsc170959
cl 39,148
skelaxin
DIVK1C_006752
5-{[(3,5-dimethylphenyl)oxy]methyl}-1,3-oxazolidin-2-one
SPECTRUM_001741
einecs 216-777-6
metaxalonum [inn-latin]
2-oxazolidinone, 5-((3,5-dimethylphenoxy)methyl)-
ahr 438
metaxalone [usan:inn:ban]
5-((3,5-xylyloxy)methyl)-2-oxazolidinone
metaxalonum [latin]
5-((3,5-dimethylphenoxy)methyl)-2-oxazolidinone
2-oxazolidinone, 5-((3,5-xylyloxy)methyl)-
nsc 170959
metaxalona [spanish]
metaxalona [inn-spanish]
hsdb 3236
metassalone [dcit]
brn 0884592
.meta.zolone
.meta.zalone
.meta.xalon
.meta.xalone
2-oxazolidinone, 5-[(3,5-dimethylphenoxy)methyl]-
2-oxazolidinone, 5-[(3,5-xylyloxy)methyl]-
5-((3,5-dimethylphenoxy)methyl)-1,3-oxazolidin-2-one
5-[(3,5-dimethylphenoxy)methyl]oxazolidin-2-one
SPECTRUM5_001685
OPREA1_438855
BSPBIO_003451
1665-48-1
metaxalone ,
C07934
DB00660
D00773
skelaxin (tn)
metaxalone (usp/inn)
NCGC00095116-01
NCGC00095116-02
KBIO2_002221
KBIO1_001696
KBIOSS_002221
KBIOGR_001164
KBIO3_002671
KBIO2_004789
KBIO2_007357
SPECTRUM3_001666
SPECTRUM4_000612
SPECTRUM2_000548
SPBIO_000595
SPECPLUS_000656
SPECTRUM1504229
NCGC00095116-03
HMS2093C22
smr001821638
5-[(3,5-dimethylphenoxy)methyl]-1,3-oxazolidin-2-one
HMS1922H07
flexura
CHEMBL1079604
chebi:6797 ,
A810747
metassalone
1nma9j598y ,
metaxalona
metaxalonum
unii-1nma9j598y
nsc758703
nsc-758703
pharmakon1600-01504229
tox21_111428
dtxcid103269
cas-1665-48-1
dtxsid3023269 ,
metaxolone
S3730
CCG-39592
5-((3,5-dimethylphenoxy)methyl)oxazolidin-2-one
FT-0603568
FS-3218
AM20060525
metaxalone [hsdb]
metaxalone [vandf]
105801-80-7
metaxalone [who-dd]
metaxalone [mi]
metaxalone [mart.]
metaxalone [usp-rs]
metaxalone [inn]
metaxalone [usp monograph]
metaxalone [usan]
metaxalone [orange book]
HY-B0678
gtpl7609
5-(3,5-dimethylphenoxymethyl)-1,3-oxazolidin-2-one
SCHEMBL34908
tox21_111428_1
NCGC00095116-05
5-(3,5-dimethylphenoxy)methyl-2-oxazolidinone
5-[(3,5-dimethylphenoxy)methyl]-1,3-oxazolidin-2-one #
5-(3,5-dimethylphenoxymethyl)-2-oxazolidinone
M2578
AB00053284_04
mfcd00867700
5-[(3,5-dimethylphenoxy)methyl]-4,5-dihydro-1,3-oxazol-2-ol
STL451511
STL450994
ahr438
SR-05000001978-3
sr-05000001978
metaxalone, united states pharmacopeia (usp) reference standard
SR-05000001978-1
metaxalone, >=98% (hplc)
J-010295
SBI-0052859.P002
Z106952910
BCP28377
Q6823309
BRD-A94709349-001-03-4
EN300-119839
SY052772
metaxalone (usp monograph)
metaxalonum (latin)
metaxalone (mart.)
metaxalonum (inn-latin)
metaxalone (usp-rs)
metaxalona (inn-spanish)
metaxalone tablet

Research Excerpts

Overview

Metaxalone is an FDA-approved muscle relaxant that has been reported to inhibit monoamine oxidase A (MAO-A). Metaxalone (Skelaxin) is a prescription medication used primarily as a skeletal muscle relaxer.

ExcerptReferenceRelevance
"Metaxalone (MTX) is a central nervous system (CNS) depressant used for the treatment of acute skeletal muscle pain. "( Metabolic activation and cytotoxicity of metaxalone mediated by cytochrome P450 enzymes and sulfotransferases.
Han, N; Hu, Z; Li, W; Liu, H; Peng, Y; Su, M; Yang, Y; Zhang, Y; Zhao, G; Zheng, J, 2023
)
2.62
"Metaxalone is an FDA-approved muscle relaxant that has been reported to inhibit monoamine oxidase A (MAO-A)."( MAO-A Inhibition by Metaxalone Reverts IL-1β-Induced Inflammatory Phenotype in Microglial Cells.
Altavilla, D; Bitto, A; Cardia, L; D'Ascola, A; Irrera, N; Mannino, F; Minutoli, L; Pallio, G; Picciolo, G; Squadrito, F; Squadrito, V, 2021
)
1.67
"Metaxalone (Skelaxin) is a prescription medication used primarily as a centrally acting skeletal muscle relaxer and is rarely implicated in drug fatalities. "( A rare fatality attributed solely to metaxalone.
Curtis, B; Jenkins, C; Wiens, AL, 2015
)
2.13
"Metaxalone is a skeletal muscle relaxant, an approved drug for pain relief. "( Metaxalone estimation in biological matrix using high-throughput LC-MS/MS bioanalytical method.
Goswami, D; Gurule, S; Khuroo, A; Monif, T; Saha, A; Vats, P, 2012
)
3.26

Effects

Metaxalone is confirmed as a Class II drug according to BCS. Metaxalone has only recently been associated with serotonin syndrome.

ExcerptReferenceRelevance
"Metaxalone has been confirmed as a Class II drug according to BCS. "( Development of a Clinically Relevant Dissolution Method for Metaxalone Immediate Release Formulations Based on an IVIVC Model.
Cetina-Čižmek, B; Filipović-Grčić, J; Khan, MZI; Radić, M; Špoljarić, D; Vuletić, L, 2018
)
2.17
"Metaxalone has only recently been associated with serotonin syndrome. "( Serotonin syndrome following metaxalone overdose and therapeutic use of a selective serotonin reuptake inhibitor.
Cobb, T; Haswell, D; Hodgman, M; Martini, DI; Nacca, N, 2015
)
2.15

Actions

ExcerptReferenceRelevance
"Metaxalone was found to suppress the activity of inflammatory macrophages in vitro."( Metaxalone Suppresses Production of Inflammatory Cytokines Associated with Painful Conditions in Mouse Macrophages RAW264.7 Cells
Levy, RM; Yamaguchi, M, 2020
)
3.44

Bioavailability

ExcerptReferenceRelevance
" Bioavailability studies performed in humans demonstrated that dissolution was the rate limiting step for bioavailability of the drug and one of the test products had significantly improved bioavailability compared to the marketed product Skelaxin®."( Development of a Clinically Relevant Dissolution Method for Metaxalone Immediate Release Formulations Based on an IVIVC Model.
Cetina-Čižmek, B; Filipović-Grčić, J; Khan, MZI; Radić, M; Špoljarić, D; Vuletić, L, 2018
)
0.72
"2% SLS (USP apparatus 2 at 50 rpm) is clinically relevant to predict bioavailability of the drug and is superior to the USP method in terms of the Quality by Design (QbD) concept."( Development of a Clinically Relevant Dissolution Method for Metaxalone Immediate Release Formulations Based on an IVIVC Model.
Cetina-Čižmek, B; Filipović-Grčić, J; Khan, MZI; Radić, M; Špoljarić, D; Vuletić, L, 2018
)
0.72
"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
" This suggests that Skelaxin Tablets should be considered a delayed release dosage form."( Comparison of the dissolution of metaxalone tablets (Skelaxin) using USP Apparatus 2 and 3.
Amann, A; Cacace, J; Reilly, EE, 2004
)
0.6
" Detailed stability exercises including drug stability in blood, hemolyzed, lipemic and normal plasma were conducted to extend the method applicability in vast majority of clinical studies using 800 mg metaxalone extended release oral dosage form."( Metaxalone estimation in biological matrix using high-throughput LC-MS/MS bioanalytical method.
Goswami, D; Gurule, S; Khuroo, A; Monif, T; Saha, A; Vats, P, 2012
)
2.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[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 (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency18.83360.006038.004119,952.5996AID1159521
AR proteinHomo sapiens (human)Potency14.83160.000221.22318,912.5098AID1259243; AID1259247
lamin isoform A-delta10Homo sapiens (human)Potency35.48130.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (72)

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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' 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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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.
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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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]
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
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 (50)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (8.00)18.7374
1990's1 (2.00)18.2507
2000's11 (22.00)29.6817
2010's24 (48.00)24.3611
2020's10 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 86.70

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 Index86.70 (24.57)
Research Supply Index4.01 (2.92)
Research Growth Index5.83 (4.65)
Search Engine Demand Index148.76 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (86.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (5.88%)5.53%
Reviews3 (5.88%)6.00%
Case Studies8 (15.69%)4.05%
Observational0 (0.00%)0.25%
Other37 (72.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Effect of Prolonged Multimodal Analgesic Regimen on Post Hospital Discharge Opioid Use and Pain Control After Primary Total Knee Arthroplasty [NCT04003350]216 participants (Actual)Interventional2017-12-21Completed
Effacacy of Modified Release Metaxalone 640 mg in Acute Lumbosacral Musculoskeletal Conditions With Spinal Stenosis and Sciatica [NCT06157177]Phase 450 participants (Anticipated)Interventional2023-11-15Recruiting
Ibuprofen Plus Metaxolone, Tizanidine, or Baclofen for Low Back Pain: A Randomized Trial [NCT03068897]Phase 4320 participants (Actual)Interventional2017-05-03Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT03068897 (4) [back to overview]Change in Functional Impairment as Measured by the Roland Morris Disability Questionnaire (RMDQ)
NCT03068897 (4) [back to overview]Levels of Disability
NCT03068897 (4) [back to overview]Number of Participants Who Experience Change in Low Back Pain
NCT03068897 (4) [back to overview]Number of Participants With Need for Medication for Low Back Pain

Change in Functional Impairment as Measured by the Roland Morris Disability Questionnaire (RMDQ)

"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." (NCT03068897)
Timeframe: Baseline and 7 days

Interventionunits on a scale (Mean)
Metaxalone10.1
Tizanidine11.2
Baclofen10.6
Placebo11.1

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Levels of Disability

Disability will be assessed with the Roland-Morris Disability Questionnaire (RMDQ) where patients are asked to tick a box if they agree with 24 statements regarding their ability to perform certain activities (dressing, housework, walking). If the don't agree with the statement (able to perform those activities) they need to leave the tick-box blank or unchecked. Every agreement (tick) counts as a point and an absolute value is formed (min: 0, max: 24). The higher the value the higher the disability level. (NCT03068897)
Timeframe: 7 days

Interventionunits on a scale (Median)
Metaxalone5
Tizanidine3
Baclofen6
Placebo3

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Number of Participants Who Experience Change in Low Back Pain

Change is assessed by verbal numerical scale of which 0 represents no pain and 10 represents the worst pain imaginable between the baseline ED visit and the one week follow-up (baseline - 1 week ). The baseline questions will refer to the time period immediately prior to ED presentation (Before you came to the ER today, were you able to…..) (NCT03068897)
Timeframe: Baseline and 7 days

InterventionParticipants (Count of Participants)
Metaxalone28
Tizanidine25
Baclofen26
Placebo22

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Number of Participants With Need for Medication for Low Back Pain

Patients will be asked what medications they have used for low back pain (NCT03068897)
Timeframe: 7 days

InterventionParticipants (Count of Participants)
Metaxalone49
Tizanidine48
Baclofen49
Placebo46

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