Page last updated: 2024-12-05

methyclothiazide

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Description

Methyclothiazide is a thiazide diuretic medication used to treat high blood pressure. It works by reducing the amount of sodium and water in the body, which helps to lower blood pressure. Methyclothiazide is generally well-tolerated, but it can cause side effects such as dehydration, low blood pressure, and electrolyte imbalances. It is important to note that methyclothiazide is not a first-line treatment for high blood pressure and should be used only under the supervision of a doctor.'

Methyclothiazide: A thiazide diuretic with properties similar to those of HYDROCHLOROTHIAZIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4121
CHEMBL ID1577
CHEBI ID6847
SCHEMBL ID49396
MeSH IDM0013609

Synonyms (127)

Synonym
smr001550236
methyclothiazidum [inn-latin]
(+-)-6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
ci-625
naturon (van)
meticlotiazide [dcit]
6-chloro-3-chloromethyl-2-methyl-7-sulfamyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide
hsdb 3363
nsc 110431
2h-1,2,4-benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide, (+-)-
einecs 205-172-2
meticlotiazida [inn-spanish]
6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
brn 0765361
6-chloro-3-(chloromethyl)-2-methyl-3,4-dihydro-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
2h-1,2,4-benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide
6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-2h-1,2, 4-benzothiadiazine-7-sulfonamide 1,1-dioxide
6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
mls002704228 ,
methyclothiazid
ciba 7272-su
aquatensen
aquaresen
duretic
enduronum
methycyclothiazide
methylclothiazide
2h-1,4-benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide
nsc-110431
enduron
methyclothiazide
6-chloro-3-(chloromethyl)-3,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
methylcyclothiazide
methychlothiazide
nsc110431
wln: t66 bswn em dhj c1 d1g hg iszw
135-07-9
methylchlorothiazide
C07765
DB00232
methyclothiazide (jan/usp/inn)
enduron (tn)
D00656
NCGC00167446-01
CHEMBL1577
chebi:6847 ,
FT-0654252
A806880
6-chloranyl-3-(chloromethyl)-2-methyl-1,1-bis(oxidanylidene)-3,4-dihydro-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
HMS3264D19
tox21_112450
dtxsid6023313 ,
cas-135-07-9
dtxcid403313
pharmakon1600-01503841
nsc760078
nsc-760078
S4057
methyclothiazidum
meticlotiazide
l3h46uac61 ,
meticlotiazida
methyclothiazide [usan:usp:inn:ban:jan]
unii-l3h46uac61
AKOS015896465
gtpl7235
methyclothiazide [usan]
methyclothiazide [jan]
methyclothiazide [usp monograph]
methyclothiazide component of eutron
diutensen-r component methyclothiazide
2h-1,2,4-benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide, (+/-)-
methyclothiazide [orange book]
methyclothiazide [inn]
methyclothiazide component of enduronyl
methyclothiazide component of diutensen-r
methyclothiazide [usp-rs]
enduronyl component methyclothiazide
eutron component methyclothiazide
methyclothiazide [who-dd]
methyclothiazide [vandf]
methyclothiazide [hsdb]
methyclothiazide [mart.]
methyclothiazide [mi]
(+/-)-6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide
CCG-213705
HY-B0562
SCHEMBL49396
tox21_112450_1
NCGC00167446-02
KS-5138
96783-15-2
CESYKOGBSMNBPD-UHFFFAOYSA-N
6-chloro-3-(chloromethyl)-2-methyl-3,4-dihydro-2h-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide #
AB01014600_04
AB01014600_03
6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-2h-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
HMS3652E06
6-chloro-3-chloromethyl-3,4-dihydro-2-methyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide
NCGC00167446-03
6-chloro-3-(chloromethyl)-2-methyl-3,4-dihydro-2h-benzo[e][1,2,4]thiadiazine-7-sulfonamide 1,1-dioxide
SW219271-1
Z1541759222
methyclothiazide, (+)-
2h-1,2,4-benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide, (-)-
r6kdh2s0sx ,
unii-r00uul4srn
unii-r6kdh2s0sx
methyclothiazide, (-)-
r00uul4srn ,
96783-14-1
2h-1,2,4-benzothiadiazine-7-sulfonamide, 6-chloro-3-(chloromethyl)-3,4-dihydro-2-methyl-, 1,1-dioxide, (+)-
aquatensen;enduron
AS-12982
Q6823919
6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-1lambda6,2,4-benzothiadiazine-7-sulfonamide
BRD-A95340155-001-05-5
EN300-122353
6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-2h-1lambda6,2,4-benzothiadiazine-7-sulfonamide
3-amino-3-(2,5-dihydroxy-phenyl)-propionicacid
methyclothiazide (usp monograph)
meticlotiazida (inn-spanish)
c03aa08
methyclothiazide (usp-rs)
methyclothiazide (usan:usp:inn:ban:jan)
methyclothiazidum (inn-latin)
methyclothiazide (mart.)

Research Excerpts

Overview

Methyclothiazide would seem to be a suitable choice for the treatment of mild hypertension.

ExcerptReferenceRelevance
"Methyclothiazide would seem to be a suitable choice for the treatment of mild hypertension in general practice."( Methyclothiazide in hypertension. A report from the General Practitioner Research Group.
, 1978
)
2.42

Treatment

ExcerptReferenceRelevance
"Pretreatment with methyclothiazide also attenuated the elevation in blood pressure but did not affect the responsiveness to hypothalamic stimulation; hence increased natriuresis or diuresis alone could not account for the effects induced by KCl."( KCl inhibits hypothalamic activity to attenuate hypertension in DOCA-salt rats.
Ijichi, H; Iyoda, I; Okajima, H; Sasaki, S; Takahashi, H; Takeda, K; Yoneda, S; Yoshimura, M, 1984
)
0.59

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" There were no significant differences in late response among patients who continued on the usual dose of methyclothiazide compared to those whose dosage was doubled, suggesting that the late response was not due to increasing the dose of the drug."( Influence of dosage and duration of therapy on the rate of response to methyclothiazide in essential hypertension.
Bartenbach, DE; Soghikian, K, 1977
)
0.7
" The lack of effect on blood pressure was probably not attributable to dosage employed, as doubling the dose (5 to 10 mg) in the normal subjects (who were equilibrated on constant diet) did not significantly increase changes in plasma volume, plasma renin activity, aldosterone excretion, urine sodium or blood pressure."( Failure of methyclothiazide to lower home blood pressure level in "essential" hypertensive and normotensive young men, despite significant plasma volume contraction.
Gordon, RD; Mortimer, RH; Saar, N, 1977
)
0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzothiadiazineHeterocyclic compound of a ring with sulfur and two nitrogen atoms fused to a benzene ring. Members inhibit sodium-potassium-chloride symporters and are used as diuretics.
[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]

Pathways (1)

PathwayProteinsCompounds
Methyclothiazide Action Pathway319

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ClpPBacillus subtilisPotency14.12541.995322.673039.8107AID651965
GALC proteinHomo sapiens (human)Potency0.707928.183828.183828.1838AID1159614
TDP1 proteinHomo sapiens (human)Potency22.65720.000811.382244.6684AID686978; AID686979
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.04110.00419.984825.9290AID504444
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency24.27890.000627.21521,122.0200AID743202; AID743219
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency0.16140.005612.367736.1254AID624032
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (82)

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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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]
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).
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).
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).
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]
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).
AID409959Inhibition of bovine liver MAOB2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
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).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID409957Inhibition of bovine liver MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
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).
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).
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' 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]
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).
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
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]
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).
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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).
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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).
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
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).
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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' 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]
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.
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).
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
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).
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (131)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990106 (80.92)18.7374
1990's3 (2.29)18.2507
2000's7 (5.34)29.6817
2010's9 (6.87)24.3611
2020's6 (4.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.32

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index33.32 (24.57)
Research Supply Index5.09 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index47.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (33.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials21 (15.00%)5.53%
Reviews2 (1.43%)6.00%
Case Studies4 (2.86%)4.05%
Observational0 (0.00%)0.25%
Other113 (80.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Prospective, Randomised, Controlled, Single Centre, Blinded Study of the Wear Characteristics of Two Polyethylene Bearing Surfaces, Enduron vs. Marathon [NCT00208442]Phase 4122 participants (Actual)Interventional2001-06-01Completed
A Prospective, Randomized Clinical Study Comparing Marathon Polyethylene and Enduron Polyethylene Acetabular Liners Used in Total Hip Arthroplasty at Long-Term Follow-up [NCT02508428]230 participants (Actual)Interventional1999-01-06Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02508428 (5) [back to overview]"Patients Who Answered Yes to the Question, Are You Satisfied With the Results of Your Hip Operation?"
NCT02508428 (5) [back to overview]Harris Hip Score
NCT02508428 (5) [back to overview]Incidence of Clinically Important Osteolysis Among Unrevised THAs
NCT02508428 (5) [back to overview]Percentage of Hips Surviving at 15 Years
NCT02508428 (5) [back to overview]Polyethylene Wear

"Patients Who Answered Yes to the Question, Are You Satisfied With the Results of Your Hip Operation?"

"Patient satisfaction was quantified by asking participants to respond yes or no to the question, Are you satisfied with the results of your hip operation? Because some patients had both of their hips included in the study, these patients responded to the question, Are you satisfied with the results of your hip operation? for their right and left hips. As a consequence, the Units Analyzed is reported as hips while the Number of Participants Analyzed reflects the number of patients." (NCT02508428)
Timeframe: At minimum 14-year follow-up and every 5 years after from the date of the patient's primary total hip arthroplasty for the duration of the patient's life or until revision of the polyethylene liner (estimated to be 25 years)

Interventionhips (Count of Units)
Crosslinked Marathon Polyethylene53
Non-crosslinked Enduron Polyethylene48

[back to top]

Harris Hip Score

The Harris Hip Score measures outcome after hip replacement and is based on a scale from 0 (worst) to 100 (best). The score includes assessments of pain, functional ability, deformity and range of motion. (NCT02508428)
Timeframe: At minimum 14-year follow-up and every 5 years after from the date of the patient's primary total hip arthroplasty for the duration of the patient's life or until revision of the polyethylene liner (estimated to be 25 years)

Interventionunits on a scale (Median)
Crosslinked Marathon Polyethylene96
Non-crosslinked Enduron Polyethylene92

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Incidence of Clinically Important Osteolysis Among Unrevised THAs

The incidence of clinically important osteolysis is based on the number of unrevised THAs (total hip arthroplasties) with at least 1.5 square centimeters of pelvic and/or femoral osteolysis. Osteolysis was defined as an area of localized loss of trabecular bone or cortical erosion that was not apparent on the pre-operative or immediate postoperative radiograph. To obtain lesion sizes, the defects were outlined on the anteroposterior pelvic and lateral radiographs. The area of the osteolysis was measured using Martell's Hip Analysis Suite software. Lesions were considered clinically important if the total area of osteolysis around a hip replacement was at least 1.5 square centimeters on either the AP or lateral view. (NCT02508428)
Timeframe: At minimum 14-year radiographic follow-up and every 5 years after from the date of the patient's primary total hip arthroplasty for the duration of the patient's life or until revision of the polyethylene liner (estimated to be 25 years)

Interventionhips (Count of Units)
Crosslinked Marathon Polyethylene1
Non-crosslinked Enduron Polyethylene28

[back to top]

Percentage of Hips Surviving at 15 Years

Kaplan-Meier survivorship was calculated using revision for wear/osteolysis as an endpoint. (NCT02508428)
Timeframe: At 15-year follow-up and every 5 years after from the date of the patient's primary total hip arthroplasty for the duration of the patient's life or until revision of the polyethylene liner (estimated to be 25 years)

Interventionpercentage of hips surviving at 15-years (Number)
Crosslinked Marathon Polyethylene100
Non-crosslinked Enduron Polyethylene86

[back to top]

Polyethylene Wear

A single reviewer, blinded to the type of polyethylene liner, evaluated femoral head penetration among all hips using serial anteroposterior pelvic radiographs. Two-dimensional head penetration was determined for each follow-up radiograph using Hip Suite Analysis version 8.0 with elliptical correction, a validated, computer-assisted technique. A linear wear rate was evaluated for each hip that had a minimum of three follow-up radiographs using a least-squares linear regression to calculate the slope of the best-fit line for the wear vector magnitude versus time in situ data. The slope from this regression represented the steady-state linear wear rate. The steady-state linear wear rate data from all hips in a group was used to compute a mean polyethylene wear value. (NCT02508428)
Timeframe: At minimum 14-year radiographic follow-up and every 5 years after from the date of the patient's primary total hip arthroplasty for the duration of the patient's life or until revision of the polyethylene liner (estimated to be 25 years)

Interventionmm/yr (Mean)
Crosslinked Marathon Polyethylene0.03
Non-crosslinked Enduron Polyethylene0.25

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