Page last updated: 2024-11-09

methimazole

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Description

Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID1349907
CHEMBL ID1515
CHEBI ID50673
SCHEMBL ID41647
MeSH IDM0013573

Synonyms (243)

Synonym
AC-785
BIDD:GT0163
3-methyl-1h-imidazole-2-thione
AB00443630-04
AB00443630-03
smr000058376
MLS000028413
2h-imidazole-2-thione, 1,3-dihydro-1-methyl-
strumazol
frentirox
imidazole, 1-methyl-2-mercapto-
thycapsol
danantizol
metothyrin
mercasolyl
mercazole
metotirin
metazolo
thiamazol
imidazole-2-thiol, 1-methyl-
2-mercapto-1-methylimidazole
nsc-38608
favistan
methiamazole
n-methyl-2-mercaptoimidazole
methimazol
1-methyl-2-mercaptoimidazole
thycapzol
methylmercaptoimidazole
mercazolyl
metothyrine
mercaptazole
basolan
thymidazole
2h-imidazole-2-thione,3-dihydro-1-methyl-
1-methylimidazole-2-thiol
thacapzol
merkastan
1-methyl-2-imidazolethiol
nsc38608
tapazole
usaf el-30
2-mercaptomethylimidazole
wln: t5n cnj a bsh
tapuzole
thymidazol
DIVK1C_000188
KBIO1_000188
1-methyl-1,3-dihydro-2h-imidazole-2-thione
MMZ ,
1,3-dihydro-1-methyl-2h-imidazole-2-thione
thimazol
ai3-60285
merkazolil
einecs 200-482-4
1-methyl-1,3-dihydroimidazole-2-thione
thiamazolum [inn-latin]
4-imidazoline-2-thione, 1-methyl-
methimazolum
tiamazol [inn-spanish]
nsc 38608
metimazol
tiamazolo [dcit]
1-metylo 2 merkaptoimidazolem [polish]
methymazol
thiamazol [inn-french]
mercazolylum
tiamazol
hsdb 3361
1-methyl-imidazole-2-thiol
SPECTRUM_000995
PRESTWICK3_000786
PRESTWICK2_000786
PRESTWICK_1010
cas-60-56-0
NCGC00016273-01
BSPBIO_001989
NCGC00178875-01
metizol
SPECTRUM5_000954
BPBIO1_000982
IDI1_000188
1-methyl-1h-imidazole-2-thiol
STK300018
60-56-0
methimazole
thiamazole
C07190
1-methylimidazole-2(3h)-thione
DB00763
methimazole (usp)
D00401
thiamazole (jp17/inn)
tapazole (tn)
BSPBIO_000892
2-mercapto-1-methylimidazole, >=99%
NCGC00094721-01
NCGC00094721-02
KBIO3_001489
KBIOSS_001475
KBIO2_001475
KBIO2_004043
KBIOGR_000515
KBIO2_006611
SPECTRUM4_000048
PRESTWICK0_000786
SPBIO_001266
NINDS_000188
SPECTRUM2_001273
PRESTWICK1_000786
SPECTRUM3_000495
SPBIO_002831
SPECTRUM1500396
CHEBI:50673 ,
NCGC00016273-02
HMS2094C05
HMS2090B17
HMS2091D12
bdbm50241361
CHEMBL1515 ,
mercaptizole
AKOS000269708
HMS500J10
M0868 ,
HMS1570M14
HMS1920L17
STK802184
AKOS000119427
A832780
NCGC00094721-03
NCGC00094721-06
NCGC00094721-05
NCGC00094721-04
HMS2097M14
HMS3259L09
tox21_201341
tox21_300532
NCGC00254307-01
NCGC00258893-01
nsc-757111
pharmakon1600-01500396
MLS002548853
nsc757111
dtxsid4020820 ,
dtxcid20820
tox21_110341
CCG-39656
NCGC00016273-03
methamazole
thimazole
2-mercapto-1-methyl-1h-imidazole
strumazole
unii-554z48xn5e
felimazole
thiamazolum
tiamazolo
thiamazole [inn]
554z48xn5e ,
methimazole [usp]
1-metylo 2 merkaptoimidazolem
FT-0603253
methimazole [mi]
methimazole [orange book]
methimazole [vandf]
thiamazole [mart.]
methimazole [usp-rs]
methimazole [usp monograph]
thiamazole [who-dd]
methimazole [iarc]
methimazole [hsdb]
thiamazole [jan]
thiamazole [ep monograph]
S1609
1-methyl-3h-imidazole-2-thione
gtpl6649
CCG-220786
HY-B0208
NC00636
SCHEMBL41647
NCGC00094721-07
tox21_110341_1
tiamazole
2-mercapto-1-methyl-imidazole
1-methyl-2-mercapto-imidazole
2-mercapto-3-methylimidazole
n-methyl imidazole-2-thiol
2-mercapto-1-methylimidazol
2-mercapto-n-methylimidazole
1-methyl-2-mercapto imidazole
1-methyl-1h-immidazole-2-thiol
2-mecapto 1-methylimidazole
1-methyl-1-h-imidazole-2-thiol
F0001-2396
Q-201364
1-methyl-1h-imidazole-2(3h)-thione
STR03572
BS-3743
1-methyl-1h-imidazole-2-thiol #
imidazole-2-thio, 1-methyl-
1-methylimidazole-2-thione
AB00443630_06
AB00443630_07
mfcd00179321
1-methyl-2,3-dihydro-1h-imidazole-2-thione
F1679-0258
sr-01000695434
SR-01000695434-2
SR-05000001672-2
sr-05000001672
methimazole, united states pharmacopeia (usp) reference standard
methimazole, vetranal(tm), analytical standard
HMS3651I13
SR-05000001672-1
methimazole, analytical standard
thiamazole, european pharmacopoeia (ep) reference standard
SBI-0206922.P004
SBI-0206922.P001
HMS3714M14
223768-14-7
Z57901905
SW197088-3
methimazole-d3(methyl-d3)
Q419663
methimazole (tapazole, northyx)
thiamazole,(s)
BCP02147
AMY11202
BRD-K54416256-001-15-7
H10722
85916-84-3
EN300-18327
methimazol 100 microg/ml in acetonitrile
1-methyl-1h-imidazol-2-ylhydrosulfide
methimazole (iarc)
metimazolo
thiamazolum (inn-latin)
thiamazole (ep monograph)
h03bb02
methimazole (usp monograph)
methimazole (usp-rs)
thiamazol (inn-french)
thiamazole (mart.)
tiamazol (inn-spanish)

Research Excerpts

Overview

Methimazole (MMI) is an antithyroid drug that is widely used for the treatment of hyperthyroidism. It is metabolized by cytochrome P450 enzymes and flavin-containing monooxygenases in mammals.

ExcerptReferenceRelevance
"Methimazole (MMI) is a widely used antithyroid drug, but it can cause hepatotoxicity by unknown mechanisms. "( Role of CYP2A6 in Methimazole Bioactivation and Hepatotoxicity.
Hussain, Z; Lei, S; Li, J; Lu, J; Ma, X; Zhu, J, 2021
)
2.4
"Methimazole is an antithyroid drug and is used clinically in hyperthyroidism. "( Comparison of antithyroid effects and hepatic complications of methimazole with catechin and its nanoencapsulation form in adult male rats.
Arabi, MS; Hojati, V; Hosseini, SM; Mohamadizadeh, E; Vaezi, G, 2022
)
2.4
"Methimazole-induced IAS is a clinically rare autoimmune disease with hypoglycaemia that occurs during medication treatment that should be treated promptly."( Analysis of the clinical characteristics of insulin autoimmune syndrome induced by methimazole.
Fang, W; Sun, L; Sun, W; Wang, C; Yi, D, 2021
)
2.29
"Methimazole (MMI) is an antithyroid agent widely used in the treatment of hyperthyroidism, and metabolized by cytochrome P450 enzymes and flavin-containing monooxygenases in mammals. "( Effects of methimazole on Drosophila glucolipid metabolism in vitro and in vivo.
Hu, B; Mburu, DK; Su, J; Tao, X; Wei, Q; Xue, Y, 2017
)
2.29
"Methimazole is an antithyroid drug that is widely used for the treatment of hyperthyroidism. "( A rare case of methimazole-induced cholestatic jaundice in an elderly man of Asian ethnicity with hyperthyroidism: A case report.
Ji, H; Song, J; Yue, F; Zhou, X, 2017
)
2.25
"Methimazole is a high-affinity substrate of hFMO3 and can competitively suppress the metabolism of other compounds."( Binding of methimazole and NADP(H) to human FMO3: In vitro and in silico studies.
Catucci, G; Gao, C; Gilardi, G; Sadeghi, SJ, 2018
)
1.59
"Methimazole (MMI) is a widely used drug for hyperthyroidism. "( Potentiating effect of rifampicin on methimazole induced hepatotoxicity in mice.
Bakhtiar, S; Hakim, B; Hakim, Z; Hasan, N; Waheed, A, 2018
)
2.2
"Methimazole (MMI) is an anti-thyroid drug used in the treatment of chronic hyperthyroidism. "( Maternal transfer of methimazole and effects on thyroid hormone availability in embryonic tissues.
Ahmed, RG; Bald, E; Chwatko, G; Darras, VM; Delezie, E; Dianati, E; Geysens, S; Van Herck, SL, 2013
)
2.15
"Methimazole (MMI) is a first-line therapy used to manage hyperthyroidism and Graves' disease. "( Novel spiroimidazopyridine derivative SAK3 improves methimazole-induced cognitive deficits in mice.
Fukunaga, K; Noreen, H; Yabuki, Y, 2017
)
2.15
"Methimazole is an oral antithyroid compound that exhibits a skin-depigmenting effect when used topically. "( Safety of topical methimazole for the treatment of melasma. Transdermal absorption, the effect on thyroid function and cutaneous adverse effects.
Eshraghian, A; Handjani, F; Kasraee, B; Nikbakhsh, M; Omrani, GR; Parhizgar, A; Safaee Ardekani, GH; Samani, M; Saurat, JH; Sorg, O; Tanideh, N, 2008
)
2.12
"Methimazole (MeimzH) is an anti-thyroid drug and the first choice for patients with Grave's disease. "( Copper(II) complexes of methimazole, an anti Grave's disease drug. Synthesis, characterization and its potential biological behavior as alkaline phosphatase inhibitor.
Dellmans, RA; Ferrer, EG; Lezama, L; Manca, SG; Moyano, MA; Naso, LG; Rojo, T; Urquiza, NM; Williams, PA, 2010
)
2.11
"Methimazole is a widely used antithyroid agent. "( Steroids for the treatment of methimazole-induced severe cholestatic jaundice in a 74-year-old woman with type 2 diabetes.
Di, F; He, R; Yang, L; Yang, T; Zhang, M; Zhou, H, 2010
)
2.09
"Methimazole (thiamazole) is an antithyroid drug commonly used to treat feline hyperthyroidism. "( Serum concentrations of methimazole in cats after a single oral dose of controlled-release carbimazole or sugar-coated methimazole (thiamazole).
Longhofer, SL; Martín-Jiménez, T; Soni-Gupta, J, 2010
)
2.11
"Methimazole is an antithyroid drug widely used in the treatment of hyperthyroidism. "( Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes.
Babaei, H; Eghbal, M; Heidari, R, 2013
)
2.19
"Methimazole is an antithyroid agent orally used in humans since several decades and has been shown that when applied topically, it inhibits melanin synthesis and causes skin depigmentation in lab animals as well as human subjects."( Successful treatment of hydroquinone-resistant melasma using topical methimazole.
Abbas, O; Barouti, N; Chedraoui, A; Ghosn, S; Malek, J; Nikolic, D,
)
1.09
"Methimazole is an antithyroid drug that can induce loss of smell and taste in humans. "( Methimazole-induced damage in the olfactory mucosa: effects on ultrastructure and glutathione levels.
Bergström, U; Brittebo, EB; Giovanetti, A; Piras, E,
)
3.02
"Methimazole is a widely used and generally well-tolerated antithyroid agent. "( Methimazole-induced cholestatic jaundice.
Mikhail, NE, 2004
)
3.21
"Methimazole is a compound administered to humans for the treatment of hyperthyroidism and is used experimentally as a model substrate for the flavin-containing monooxygenase (FMO) system. "( Olfactory toxicity of methimazole: dose-response and structure-activity studies and characterization of flavin-containing monooxygenase activity in the Long-Evans rat olfactory mucosa.
Blake, BL; Deamer, NJ; Genter, MB; Levi, PE; Wesley, DS,
)
1.89
"Methimazole acts as a radical scavenger, maintaining the glutathione pool in the kidney."( Protective effects of methimazole against cisplatin-induced nephrotoxicity in rats.
Appenroth, D; Bräunlich, H; Fleck, C,
)
1.17
"Methimazole is an antithyroid drug reported to affect the sense of smell and taste in humans. "( Methimazole toxicity in rodents: covalent binding in the olfactory mucosa and detection of glial fibrillary acidic protein in the olfactory bulb.
Bergman, U; Brittebo, EB, 1999
)
3.19

Effects

Methimazole (MMI) has been used for the treatment of Graves' Disease (GD) for more than half a century. Drug-induced liver injury (DILI) is one of the most deleterious side effects. Methimazol has become the most frequently prescribed antithyroid drug.

ExcerptReferenceRelevance
"Methimazole (MMI) has been shown to induce several patterns of liver injury."( Graves' disease overlapping with chronic hepatitis B and methimazole-induced liver injury and autoimmune hepatitis: a case report.
Brigstock, DR; Cui, S; Gao, R; Zhang, W; Zheng, M, 2022
)
1.69
"Methimazole (MMI) has been used for the treatment of Graves' Disease (GD) for more than half a century. "( Association of HLA-C*03:02 with methimazole-induced liver injury in Graves' disease patients.
Cai, W; Fan, X; Fan, Y; Jin, S; Li, X; Tang, Z; Xiang, X; Yang, J, 2019
)
2.24
"Methimazole (MMI) has been used in the therapy of Grave's disease (GD) since 1954, and drug-induced liver injury (DILI) is one of the most deleterious side effects. "( Association between genetic polymorphisms of SLCO1B1 and susceptibility to methimazole-induced liver injury.
Cai, W; Dai, Y; Fan, X; Fan, Y; Jin, S; Li, X; Lin, H; Xiang, X; Yang, J, 2019
)
2.19
"Oral methimazole has been widely used to treat hyperthyroidism, but its usage is restricted by its adverse systemic effects. "( Efficacy and safety of methimazole ointment for patients with hyperthyroidism.
Gu, M; Liu, H; Liu, Z; Shen, J; Shi, Y; Song, Z; Wu, X; Zhu, X, 2013
)
1.21
"Methimazole has become the most frequently prescribed antithyroid drug. "( Shifts in propylthiouracil and methimazole prescribing practices: antithyroid drug use in the United States from 1991 to 2008.
Cooper, DS; Emiliano, AB; Governale, L; Parks, M, 2010
)
2.09
"Methimazole has improved thyrotoxic symptoms in a 3-year-old male with thyroid hormone resistance. "( Treatment with methimazole in a 3-year-old male with thyroid hormone resistance.
Ahmet, A; Tsai, SL, 2012
)
2.17
"The methimazole has long been used for treating Graves' disease to decrease thyroid hormone production and obtain a thyroid normofunction, but this drug has also immunosuppressive and immunomodulation effects."( [Effects of methimazole on the evolution of the allergic rhinitis of patients with Graves' disease].
Cortinas López, L; Duarte Díaz, RJ; León Oviedo, C; Montes Montes, J; Sánchez Olivas, JA; Sánchez Olivas, MA; Valencia Zavala, MP,
)
1.07
"Methimazole has been found to trap superoxide (O2.-) radicals and to decrease the level of blood prostaglandin E2."( Anti-inflammatory action of methimazole.
Buxeraud, J; Comby, F; Lagorce, JF; Moulard, T; Raby, C; Rousseau, A, 1997
)
1.31
"Methimazole has been reported to produce extensive degenerative changes in olfactory epithelium and a severe deficit in odor detection [Genter BM, Owens DM, Carlone HB, Crofton KM. "( Olfaction and peripheral olfactory connections in methimazole-treated rats.
Slotnick, B; Xu, W, 1999
)
2
"Methimazole (MMI) has been reported to affect prognosis in hyperthyroid Graves' disease patients treated with radioiodine (131I). "( Antithyroid drugs inhibit radioiodine-induced increases in thyroid autoantibodies in hyperthyroid Graves' disease.
Ito, S; Kiso, Y; Mori, K; Nakagawa, Y; Nakazato, N; Sayama, N; Tani, JI; Yoshida, K, 1999
)
1.75

Actions

Methimazole was found to inhibit thyroxine production in 4 of the 6 adult possums although it had no effect on body weight. It may protect against gentamicin-induced nephrotoxicity by acting as an antioxidant within the kidneys.

ExcerptReferenceRelevance
"Methimazole may cause "methimazole embryopathy"."( [Current problems in the treatment of Graves' disease in pregnancy and in lactation].
Momotani, N, 2006
)
1.06
"Methimazole did not inhibit GM renal uptake but may protect against GM-induced nephrotoxicity by acting as an antioxidant within the kidneys."( Methimazole protection of rats against gentamicin-induced nephrotoxicity.
Cooley, AJ; Duescher, RJ; Elfarra, AA; O'Hara, TM; Sausen, PJ, 1994
)
2.45
"Methimazole was found to inhibit thyroxine production in 4 of the 6 adult possums although it had no effect on body weight."( The effect of methimazole on the growth of the developing brushtail possum, Trichosurus vulpecula.
Buaboocha, W; Gemmell, RT,
)
1.21
"Methimazole did not inhibit gentamicin renal uptake but may protect against gentamicin-induced nephrotoxicity by acting as an antioxidant within the kidneys."( Effect of methimazole and fish oil treatment on gentamicin nephrotoxicity in rats.
el Daly, ES,
)
1.26

Treatment

Methimazole treatment produced no significant change in SOD-like activity and Cu, Zn-SOD concentration when patients with Graves' disease had normal thyroid function.

ExcerptReferenceRelevance
"Methimazole treatment reversed these parameters."( Regulation of the cellular redox state and the expression of DNA methyltransferase-1 in peripheral blood mononuclear cells from patients with Graves' disease.
Barreiro Arcos, ML; Costilla, M; Cremaschi, G; Curria, MI; Di Cugno, M; Klecha, AJ; Saban, M,
)
0.85
"Methimazole (MMI) is the treatment of choice for patients with Graves' disease. "( Efficacy of low-dose methimazole in control of multiple relapses of Graves' hyperthyroidism: a case report.
Abdi, H; Amouzegar, A; Azizi, F, 2021
)
2.38
"Methimazole treatment significantly decreased serum OC concentration by 21% (P=0.02) and increased CTX-I concentration by 17% (P=0.06)."( Effects of long-term oral administration of methimazole on femur and tibia properties in male Wistar rats.
Bieńko, M; Gołyński, M; Krupski, W; Radzki, RP; Tatara, MR, 2017
)
1.44
"LT methimazole treatment of 96 to 120 months is safe and effective for treatment of juvenile Graves' disease. "( Long-term Methimazole Therapy in Juvenile Graves' Disease: A Randomized Trial.
Amouzegar, A; Azizi, F; Madreseh, E; Takyar, M, 2019
)
1.54
"Premethimazole treatment, eight hyperthyroid cats received CT scans from the head to heart, which were compared to CT of seven euthyroid cats."( COMPUTED TOMOGRAPHIC CHARACTERISTICS OF THE THYROID GLANDS IN EIGHT HYPERTHYROID CATS PRE- AND POSTMETHIMAZOLE TREATMENT COMPARED WITH SEVEN EUTHYROID CATS.
Bobe, G; Bush, JL; Gordon, J; Nemanic, S, 2017
)
1.19
"Methimazole treatment to ZDF rats significantly reduced blood glucose levels, food intake, body weight, and serum T3 levels."( Effects of methimazole on the onset of type 2 diabetes in leptin receptor-deficient rats.
Hwang, IK; Ju, EJ; Kim, IY; Kim, YN; Lee, IS; Lee, YH; Park, IS; Seong, JK; Won, MH; Yi, SS; Yoon, YS, 2009
)
1.46
"Methimazole-treated rat kidneys exhibited leucocytic infiltrations, vascular congestion and narrowed Bowman's space."( Protective effects of selenium on methimazole nephrotoxicity in adult rats and their offspring.
Ben Amara, I; Boudawara, T; Garoui, E; Hakim, A; Troudi, A; Zeghal, KM; Zeghal, N, 2011
)
1.37
"Methimazole treatment decreased femur length and weight in 14-day-old rats, when compared to controls. "( Toxicity of methimazole on femoral bone in suckling rats: alleviation by selenium.
Ben Amara, I; Guermazi, F; Soudani, N; Troudi, A; Zeghal, N, 2012
)
2.2
"Methimazole-treated subjects also had higher head-dip scores than controls at 40 days while no differences were observed at 60 days."( Perinatal hypothyroidism effects on neuromotor competence, novelty-directed exploratory and anxiety-related behaviour and learning in rats.
Balada, F; Darbra, S; Garau, A; Martí-Carbonell, MA; Sala, J, 2003
)
1.04
"Methimazole pretreatment attenuates the 131I-induced rise in serum TRAb levels. "( Serum thyrotropin-receptor autoantibodies levels after I therapy in Graves' patients: effect of pretreatment with methimazole evaluated by a prospective, randomized study.
Andrade, VA; Gross, JL; Maia, AL, 2004
)
1.98
"Methimazole treatment resulted in all markers being normalized in the patients without infiltrative ophthalmopathy, yet oxidative stress was still present in the ophthalmopathy group."( Oxidative stress peripheral parameters in Graves' disease: the effect of methimazole treatment in patients with and without infiltrative ophthalmopathy.
Bednarek, J; Sowiński, J; Wysocki, H, 2005
)
1.28
"Methimazole treatment did not relieve TSH suppression in 17 cats."( Effects of methimazole on thyroid gland uptake of 99mTC-pertechnetate in 19 hyperthyroid cats.
Chew, DJ; DiBartola, SP; Drost, WT; Fischetti, AJ; Meadows, C; Schenck, PA,
)
1.24
"In methimazole-treated rats, the contractile force, the maximum velocity of tension development and relaxation were significantly decreased, however, the time to peak tension remained unchanged."( The effect of hypothyroidism on myocardial contractility and sarcoplasmic reticulum function in rats.
Szabó, J; Szegi, J; Szentmiklósi, AJ; Takács, IE, 1982
)
0.78
"Only methimazole-treated males showed a significant increase (P less than 0.01) in the total number of fibers of the two muscles (tibialis posterior and flexor digitorum) studied."( Influence of experimental hypothyroidism on chick myogenesis.
Bacou, F; Jallageas, M; Nougues, J; Vigneron, P, 1980
)
0.72
"Methimazole dose, pretreatment serum T3 levels, and goitre size are the main determinants of the therapeutic response to methimazole in Graves' disease, at least in areas comprising low, subnormal and normal iodine supply."( Response to methimazole in Graves' disease. The European Multicenter Study Group.
Benker, G; Hirche, H; Kahaly, G; Raue, F; Reinwein, D; Tegler, L; Vitti, P, 1995
)
2.11
"The methimazole-treated pups were demonstrated to be hypothyroid, with markedly higher TSH and lower T4 concentrations, until weaning occurred between weeks three and four, after which they transiently became hyperthyroid at week five (T4 = 17 +/- 5 micrograms/dL vs."( Thyroid hormone status correlates inversely with expression of the growth hormone receptor gene in rats immediately after birth.
Franz, B; Menon, RK; Sperling, MA; Stephan, DA, 1993
)
0.77
"Methimazole treatment produced no significant change in SOD-like activity and Cu, Zn-SOD concentration when patients with Graves' disease had normal thyroid function."( [Serum superoxide dismutase in patients with Graves' disease].
Ban, Y; Hara, H; Sato, R, 1993
)
1.01
"Methimazole-treated hypothyroid rats were fed low-fat chow or chow supplemented with 10% corn oil or fish oil, and were studied before and after thyroid hormone treatment."( Thyroid hormone is required for dietary fish oil to induce hypersecretion of biliary cholesterol in the rat.
Gebhard, RL; Ketover, SR; Prigge, WF, 1995
)
1.01
"Methimazole treatment was initiated with a dosage of 40 mg/d, tapered to 20 mg/d after two weeks and maintained until complete remission in both groups."( [Effect of methimazole and dexamethasone on leucocyte glucocorticoid receptor, plasma ACTH, and cortisol levels in Graves' disease].
Gao, Y; Li, X; Zhang, C, 1996
)
1.41
"Methimazole treatment significantly affected phospholipid content and phospholipid fatty acid composition."( Thermogenesis and fatty acid composition of brown adipose tissue in rats rendered hyperthyroid and hypothyroid-with special reference to docosahexaenoic acid.
Kuroshima, A; Ohinata, H; Ohno, T; Saha, SK, 1998
)
1.02
"In methimazole-pretreated rats, the kinetic of DNA fragmentation was nearly the same; apoptosis increased for the first 6 hours and then decreased at 12 hours after KI administration."( Excess iodine induces apoptosis in the thyroid of goitrogen-pretreated rats in vivo.
Burikhanov, RB; Matsuzaki, S, 2000
)
0.82
"Methimazole-treated thyrocytes induced FasL-dependent apoptosis in cocultured lymphocytes, whereas methimazole treatment of lymphocytes grown in the absence of thyrocytes had no such effect."( Fas ligand expression in thyroid follicular cells from patients with thionamide-treated Graves' disease.
Chrousos, GP; Koutras, DA; Mitsiades, N; Poulaki, V; Tseleni-Balafouta, S, 2000
)
1.03
"Methimazole treatment of estrogen-primed males and intact females inhibited tumor formation by 78 and 95%, respectively."( Control of cell growth. II. Requirement of thyroid hormones for the in vivo estrogen-dependent growth of rat pituitary tumor cells.
Kirkland, WL; Sirbasku, DA; Sorrentino, JM, 1976
)
0.98
"Methimazole-treated G2K-1 C rats showed reductions in heart rate, ventricular weight, ventricular/body weight ratio and mortality in comparison with rats not treated with methimazole."( Methimazole treatment reduces cardiac hypertrophy and mortality without a concomitant reduction in blood pressure in established Goldblatt two-kidney one clip hypertension.
Castillo, MA; Haro, JM; Vargas, F, 1992
)
2.45
"In methimazole-treated rats, elevated blood pressure induced 5 weeks previously returned to normotensive levels."( Effects of methimazole on low-renal-mass hypertension: changes in blood pressure and pressor responsiveness to vasoconstrictors.
Andrade, JL; Castillo, MA; de Luna, JD; Haro, JM; Vargas, F, 1992
)
1.19
"Methimazole treatment did not potentiate diabetes induced by a single high dose of streptozotocin (175 mg/kg)."( Methimazole treatment aggravates low-dose streptozotocin-induced diabetes.
Hibbe, T; Kiesel, U; Kolb, H; Kolb-Bachofen, V, 1991
)
2.45
"Methimazole-treated hypothyroid rats were injected intravenously with triacylglycerol/cholesteryl oleate/cholesterol/phospholipid emulsions designed to model the composition of chylomicrons. "( Effects of hypothyroidism on the metabolism of lipid emulsion models of triacylglycerol-rich lipoproteins in rats.
Callow, MJ; Elsegood, CL; Mamo, JC; Redgrave, TG, 1991
)
1.72
"Methimazole treatment was accompanied by a gradual reduction in circulating levels of thyrotropin-receptor, microsomal, and thyroglobulin autoantibodies."( Induction of circulating activated suppressor-like T cells by methimazole therapy for Graves' disease.
Bengtsson, M; Karlsson, FA; Mendel-Hartvig, I; Tötterman, TH, 1987
)
1.23
"Methimazole-treated birds have an exaggerated pituitary protein kinase response to cold stress when compared with controls."( The effects of castration and/or methimazole feeding on the pituitary response to temperature extremes by cockerels.
Carr, BL; Chiasson, RB, 1985
)
1.27
"In methimazole-treated rats infused with 3 nmol T4/day/100 g BW, the nafenopin inhibitory effect was not significantly different from that in euthyroid rats."( Increased plasma clearance rate of thyroxine despite decreased 5'-monodeiodination: study with a peroxisome proliferator in the rat.
Burger, AG; Giacobino, JP; Girardier, L; Kaiser, CA; Seydoux, J, 1988
)
0.79
"In methimazole-treated patients with T3-suppressible thyroid uptake, anti-DNA antibody was found in 9% (3 of 35)."( Presence of antideoxyribonucleic acid antibody in patients with hyperthyroidism of Graves' disease.
Aizawa, T; Hiramatsu, K; Ishihara, M; Kameko, M; Kanai, M; Katakura, M; Maruyama, K; Takasu, N; Yamada, T; Yukimura, Y, 1987
)
0.79
"Methimazole treatment in utero did not produce significant changes in noradrenaline, dopamine or tyrosine content in either the hypothalamus or striatum."( The effects of neonatal hypothyroidism on brain catecholamine turnover in adult rats: assessment by a steady-state method.
Dieguez, C; Hall, R; Harris, PE; Lewis, BM; Scanlon, MF, 1987
)
0.99
"Ten methimazole and 12 untreated litters were studied."( The behavioral effects of perinatal methimazole administration in Swiss Webster mice.
Millan, DP; Rice, SA; West, JA, 1987
)
1.03
"Methimazole treatment caused a significant reduction in the magnitude of the responses to noradrenaline and in its potency (2.8 fold)."( Influence of thyroid status on responses of rat isolated pulmonary artery, vas deferens and trachea to smooth muscle relaxant drugs.
Mustafa, MB; O'Donnell, SR; Wanstall, JC, 1987
)
0.99
"Treatment with methimazole, propranolol, hydrocortisone, and Lugol's iodine solution was used."( Thyroid Storm in a Toddler Presenting as a Febrile Seizure.
Ladd, JM; Sabsabi, B; von Oettingen, JE, 2020
)
0.9
"Treatment with methimazole exacerbated an underlying hypersensitivity disorder leading to marked generalized lymphadenopathy that histologically mimicked lymphoma."( Cutaneous lymphoid hyperplasia mimicking cutaneous lymphoma in a hyperthyroid cat.
Kerr, M; Macdonald, V; Snead, E, 2013
)
0.73
"Treatment with methimazole 30 mg and propranolol 30 mg was started, and her thyroid function showed improvement."( [Case of graves' disease with remarkable psychiatric symptoms].
Arao, T; Kuno, F; Kurozumi, A; Okada, Y; Tanaka, Y, 2015
)
0.76
"Treatment with methimazole was discontinued, and therapy with antibiotics, granulocyte colony-stimulating factor, and ibuprofen was initiated."( Successful treatment of thyroid storm with plasmapheresis in a patient with methimazole-induced agranulocytosis.
Fillipon, NL; Trivedi, N; Vijayakrishnan, R; Vyas, AA; Vyas, P,
)
0.7
"Treatment with methimazole resolved the hyperthyroidism, and the cholestasis improved, as well."( Graves' disease presenting with severe cholestasis.
Arnon, R; Kerkar, N; Miloh, T; Morotti, R; Rapaport, R; Regelmann, MO, 2012
)
0.72
"Treatment with methimazole (MMI) reduces serum CXCL10 in patients with Graves' disease."( Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes.
Annunziato, F; Borgogni, E; Cosmi, L; Crescioli, C; Francalanci, M; Gelmini, S; Mazzinghi, B; Perigli, G; Pezzatini, A; Santarlasci, V; Sarchielli, E; Serio, M; Sottili, M; Vannelli, GB, 2007
)
2.12
"Treatment with methimazole was effective in reducing her tremor and tachycardia; however, she was often nonadherent with her antithyroid medication because of improvement of her symptoms."( Graves' disease with intractable diarrhea, chylous ascites, and chylothorax: a case report.
Higa, M; Hiroi, N; Kuboki, K; Sakamoto, Y; Urita, Y; Yoshino, G, 2007
)
0.68
"Treatment with methimazole in post-menopausal women with endogenous subclinical hyperthyroidism associated with multinodular goitre can prevent excessive loss of bone, at least in the distal forearm."( Bone metabolism during anti-thyroid drug treatment of endogenous subclinical hyperthyroidism.
Houben, AJ; Mudde, AH; Nieuwenhuijzen Kruseman, AC, 1994
)
0.64
"This treatment with methimazole causes an increase in renal excretion of PAH in rats of various age groups, statistically significant in 5-, 10- and 20-day-old rats."( Renal excretion and renal tubular transport of p-aminohippurate (PAH) in methimazole treated, hypothyroid rats of different ages.
Bräunlich, H; Reimann, IR, 1994
)
0.83
"Treatment with methimazole increased the magnesium concentration both in erythrocytes (2.00 +/- 0.18 vs."( Magnesium metabolism in hyperthyroidism.
Disashi, T; Fujimoto, Y; Inoue, J; Iwaoka, T; Naomi, S; Tomita, K; Umeda, T, 1996
)
0.63
"Treatment with methimazole and correction of the thyroid condition led to rapid disappearance of the disorders."( [Acute myopathy and hyperthyroidism].
Bottacchi, E; Camerlingo, M; Cornelio, F; Daniel, S; Mamoli, A; Morandi, L, 1986
)
0.61

Toxicity

Methimazole is usually used at an initial dose of 30 mg/day for severe Graves' disease (GD) hyperthyroidism. Adverse effects are more frequent at this dose than at MMI 15  mg/day. The proposed mechanism of action is intracellular: it lowers the level of proliferating cell nuclear antigen (PCNA)

ExcerptReferenceRelevance
"The authors studied 389 Graves' hyperthyroid patients receiving either high propylthiouracil (PTU) or methimazole (MMI) daily doses or low doses to evaluate whether adverse effects were related to the thionamide drugs or its daily dose regimen."( Adverse effects related to thionamide drugs and their dose regimen.
Bromberg, N; Farah, CS; Romaldini, JH; Werner, MC; Werner, RS, 1989
)
0.49
"The role of S-oxidation in the toxic bioactivation of alpha-naphthylisothiocyanate (ANIT) was investigated."( Effect of inhibitors of alpha-naphthylisothiocyanate-induced hepatotoxicity on the in vitro metabolism of alpha-naphthylisothiocyanate.
Hanzlik, RP; Traiger, GJ; Vyas, KP, 1985
)
0.27
" While pharmacodynamically caused therapy effects are generally to be avoided, when considering the pathophysiology of the regulation of the thyroid gland, this is not the case as to allergic side effects and only to a limited extent with regard to toxic side effects."( [Thyrostatic therapy of hyperthyroidism with special reference to drug side effects].
Heberling, HJ; Lohmann, D, 1983
)
0.27
"The aims of the present study were to investigate the incidence of adverse effects of thioureylene antithyroid drugs and to see if there were any factors related to the development of the adverse effects."( [The adverse effects of thioureylene antithyroid drugs (author's transl)].
Inoue, K; Nakashima, T; Nishitani, H; Okabe, N; Okamura, K; Omae, T; Shiroozu, A; Yoshinari, M, 1982
)
0.26
"In thyreostatic treatment the loss of taste combined with discreetly increasing hepatic enzymes has been observed as a toxic effect of thiamazole in a female patient."( [Reversible loss of taste as a side effect in thiamazole therapy].
Reck, R; von Mengden, HJ, 1982
)
0.26
" Two structurally related compounds, methylimidazole and methylpyrrole, were not olfactory toxicants, suggesting that a reactive intermediate generated in the course of metabolizing methimazole to an S-oxide is the olfactory toxic species."( Olfactory toxicity of methimazole: dose-response and structure-activity studies and characterization of flavin-containing monooxygenase activity in the Long-Evans rat olfactory mucosa.
Blake, BL; Deamer, NJ; Genter, MB; Levi, PE; Wesley, DS,
)
0.64
" In conclusion, 1) amiodarone had a cytotoxic effect in CHO fibroblasts, a nonthyroid cell line; 2) this cytotoxic effect occurred in thyroid cells independent of their ability to organify iodide; 3) however, the toxic effect of amiodarone was greater and occurred at a lower molar concentration in freshly prepared human thyroid follicles that trap and organify iodide; and 4) in the latter culture system, methimazole, an inhibitor of iodide organification, partially, but significantly, reduced the cytotoxic effect of amiodarone."( Studies on the in vitro cytotoxic effect of amiodarone.
Braverman, LE; Chiovato, L; Lapi, P; Mammoli, C; Martino, E; Pinchera, A; Santini, F; Tonacchera, M, 1994
)
0.45
" Possible adverse effects of this therapy include cardiovascular changes (shortening of systolic time intervals, increased frequency of atrial premature beats and, possibly, left ventricular hypertrophy) and bone changes (reduced bone density and bone mass), but the risk of these adverse effects can be minimised by carefully monitoring serum free thyroxine and free liothyronine (triiodothyronine) measurements and adjusting the dosage accordingly."( Adverse effects of thyroid hormone preparations and antithyroid drugs.
Bartalena, L; Bogazzi, F; Martino, E, 1996
)
0.29
"In vivo ethylenebisdithiocarbamates and ETU are toxic to the thyroid gland."( Thyroid peroxidase as toxicity target for dithiocarbamates.
Corsini, E; Galli, CL; Ghilardi, F; Guizzetti, M; Marinovich, M; Viviani, B, 1997
)
0.3
" Hydrazine has been reported to be metabolised by NADPH cytochrome P-450 reductase (reductase) to reactive and potentially toxic intermediates."( The role of l-thyroxine and hepatic reductase activity in isoniazid-induced hepatotoxicity in rabbits.
Adams, SP; Sarich, TC; Wright, JM, 1998
)
0.3
" Histological examination of kidney confirmed the toxic effect of cisplatin."( Prevention of cisplatin-induced nephrotoxicity by methimazole.
Al-Hyder, A; Attia, AS; El-Demerdash, E; El-Didi, M; El-Sayed, EM; Hamada, FM; Osman, AM, 2000
)
0.56
" Similarly, ring fusion of a benzene nucleus to the C-4,5 double bond, forming 2-mercapto-1-methylbenzimidazole, abolished the toxic potency."( Evidence for the involvement of N-methylthiourea, a ring cleavage metabolite, in the hepatotoxicity of methimazole in glutathione-depleted mice: structure-toxicity and metabolic studies.
Kawazoe, S; Mizutani, T; Murakami, M; Shirai, M; Yoshida, K, 2000
)
0.52
"To determine whether once daily administration of methimazole was as effective and safe as twice daily administration in cats with hyperthyroidism."( Efficacy and safety of once versus twice daily administration of methimazole in cats with hyperthyroidism.
Challoner, L; Hoffman, SB; Kroll, M; Rodan, I; Trepanier, LA, 2003
)
0.81
" Percentages of cats with adverse effects (primarily gastrointestinal tract upset and facial pruritus) were not significantly different between groups."( Efficacy and safety of once versus twice daily administration of methimazole in cats with hyperthyroidism.
Challoner, L; Hoffman, SB; Kroll, M; Rodan, I; Trepanier, LA, 2003
)
0.56
"The objective of this study was to determine whether transdermal methimazole was as safe and effective as oral methimazole for the control of hyperthyroidism in cats."( Efficacy and safety of transdermal methimazole in the treatment of cats with hyperthyroidism.
Challoner, L; Kroll, MM; Rodan, I; Sartor, LL; Trepanier, LA,
)
0.65
" Recently, attention has focused on the estrogen-like and carcinogenic adverse effects of BPA and HQ."( Cytotoxicity and apoptosis-inducing activity of bisphenol A and hydroquinone in HL-60 cells.
Fujisawa, S; Kadoma, Y; Sakagami, H; Terasaka, H,
)
0.13
" Further studies of the effectiveness of continuous thionamide therapy in patients with thyrotoxicosis need to be designed and implemented to determine indications for such therapy in children, adolescents and adults with diffuse toxic goiter, in particular, in those who have had recurrence of hyperthyroidism after discontinuation of one complete course of treatment."( The safety and efficacy of antithyroid drugs.
Azizi, F, 2006
)
0.33
" Only 1 cat showed a cutaneous adverse reaction along with a marked thrombocytopenia."( Clinical efficacy and safety of transdermal methimazole in the treatment of feline hyperthyroidism.
Doucet, MY; Dunn, ME; Lécuyer, M; Prini, S, 2006
)
0.59
" Cutaneous adverse effects of topical methimazole were determined."( Safety of topical methimazole for the treatment of melasma. Transdermal absorption, the effect on thyroid function and cutaneous adverse effects.
Eshraghian, A; Handjani, F; Kasraee, B; Nikbakhsh, M; Omrani, GR; Parhizgar, A; Safaee Ardekani, GH; Samani, M; Saurat, JH; Sorg, O; Tanideh, N, 2008
)
0.95
" Over the years that these medications have been used, reports of adverse events involving hepatotoxicity have appeared."( Dissimilar hepatotoxicity profiles of propylthiouracil and methimazole in children.
Rivkees, SA; Szarfman, A, 2010
)
0.6
" Food and Drug Administration's Adverse Event Reporting System (AERS)."( Dissimilar hepatotoxicity profiles of propylthiouracil and methimazole in children.
Rivkees, SA; Szarfman, A, 2010
)
0.6
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" Is the 'see-saw' relationship actually a therapeutic side effect of antithyroid drug? The proposed mechanism of methimazole action is intracellular: it lowers the level of proliferating cell nuclear antigen (PCNA)."( Myasthenic crisis as a side effect of methimazole therapy: case report.
Balić, S; Baretić, M; Gudelj, G, 2010
)
0.84
"To compare the therapeutic effect and side effect of the treatments on hyperthyroid exophthalmos with the combination of acupuncture and medication and with medication only."( [Therapeutic effect and side effect of treatment on hyperthyroid exophthalmos with the combination of acupuncture and medication].
He, JS; Li, Y; Liu, SM; Shu, S; Xia, Y, 2010
)
0.36
" We examined the occurrence of adverse events in GD patients treated with RTX."( Systemic adverse events following rituximab therapy in patients with Graves' disease.
El Fassi, D; Hasselbalch, HC; Hegedüs, L; Junker, P; Nielsen, CH,
)
0.13
" Adverse events were recorded, and the presence of circulating immune complexes (CIC) was measured as IgG, IgM and complement component 3 (C3) depositing on normal monocytes following incubation with patient plasma."( Systemic adverse events following rituximab therapy in patients with Graves' disease.
El Fassi, D; Hasselbalch, HC; Hegedüs, L; Junker, P; Nielsen, CH,
)
0.13
"Five patients had benign infusion-related adverse events at first infusion."( Systemic adverse events following rituximab therapy in patients with Graves' disease.
El Fassi, D; Hasselbalch, HC; Hegedüs, L; Junker, P; Nielsen, CH,
)
0.13
"We report articular adverse events in 3 and gastrointestinal symptoms in 2 out of 10 GD patients who received RTX without concurrent immunosupression."( Systemic adverse events following rituximab therapy in patients with Graves' disease.
El Fassi, D; Hasselbalch, HC; Hegedüs, L; Junker, P; Nielsen, CH,
)
0.13
"Once daily transdermal administration of a novel lipophilic formulation of methimazole is as safe and effective as oral carbimazole in treating hyperthyroidism in cats."( The efficacy and safety of a novel lipophilic formulation of methimazole for the once daily transdermal treatment of cats with hyperthyroidism.
Bridges, J; Chambers, P; Gieseg, MA; Hill, KE; Kingsbury, D; Lopez-Villalobos, N,
)
0.6
"In this 12-week trial, once daily application of a novel formulation of transdermal methimazole applied to the pinnae was as effective and safe as twice daily oral carbimazole in the treatment of cats with hyperthyroidism."( The efficacy and safety of a novel lipophilic formulation of methimazole for the once daily transdermal treatment of cats with hyperthyroidism.
Bridges, J; Chambers, P; Gieseg, MA; Hill, KE; Kingsbury, D; Lopez-Villalobos, N,
)
0.6
"Agranulocytosis is a rare adverse effect of methimazole."( Sudden onset agranulocytosis and hepatotoxicity after taking methimazole.
Hong, T; Wen, GB; Xiao, XH; Yang, J; Zhong, J; Zhou, LZ, 2012
)
0.88
" Administration of this drug, often in a chronic manner, is associated with several adverse drug reactions in humans, including life-threatening hepatotoxicity."( Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes.
Babaei, H; Eghbal, M; Heidari, R, 2013
)
0.75
"The duration of time required for normalization of serum free T4 on initial treatment and the incidence of adverse effects for 1 year after the start of MMI were compared."( Higher dose of methimazole causes frequent adverse effects in the management of Graves' disease in children and adolescents.
Inomata, H; Kazukawa, I; Kohno, Y; Konda, S; Minagawa, M; Minamitani, K; Sanayama, K; Sasaki, N; Sato, H; Sugihara, S; Wataki, K, 2012
)
0.73
" No major adverse reactions were observed."( Higher dose of methimazole causes frequent adverse effects in the management of Graves' disease in children and adolescents.
Inomata, H; Kazukawa, I; Kohno, Y; Konda, S; Minagawa, M; Minamitani, K; Sanayama, K; Sasaki, N; Sato, H; Sugihara, S; Wataki, K, 2012
)
0.73
"Oral methimazole has been widely used to treat hyperthyroidism, but its usage is restricted by its adverse systemic effects."( Efficacy and safety of methimazole ointment for patients with hyperthyroidism.
Gu, M; Liu, H; Liu, Z; Shen, J; Shi, Y; Song, Z; Wu, X; Zhu, X, 2013
)
1.21
"Agranulocytosis is a serious adverse effect of antithyroid drugs (ATDs) and mainly develops within three months after the start of uninterrupted ATD treatment."( Characteristics of agranulocytosis as an adverse effect of antithyroid drugs in the second or later course of treatment.
Ito, K; Iwaku, K; Kobayashi, S; Kunii, Y; Matsumoto, M; Mukasa, K; Noh, JY; Ohye, H; Sugino, K; Suzuki, M; Watanabe, N; Yoshihara, A, 2014
)
0.4
"In mice treated with PTU or MMI, no significant histopathological abnormalities or external gross malformations, and no adverse effects on placental weight, litter size, resorption rates, or fetal weight were observed at GD 18."( Evaluation of developmental toxicity of propylthiouracil and methimazole.
Booth, CJ; Mallela, MK; Poulsen, RR; Rivkees, SA; Strobl, M; Wendler, CC, 2014
)
0.64
"Methimazole (MMI) is usually used at an initial dose of 30 mg/day for severe Graves' disease (GD) hyperthyroidism, but adverse effects are more frequent at this dose than at MMI 15 mg/day."( Comparison of efficacy and adverse effects between methimazole 15 mg+inorganic iodine 38 mg/day and methimazole 30 mg/day as initial therapy for Graves' disease patients with moderate to severe hyperthyroidism.
Ito, K; Kunii, Y; Matsumoto, M; Mukasa, K; Nagataki, S; Noh, JY; Sato, S; Sugino, K; Suzuki, M; Taniyama, M; Yasuda, S, 2015
)
2.11
" MMI 30 mg/day (M30)) in terms of therapeutic effect, adverse effects, and remission rate."( Comparison of efficacy and adverse effects between methimazole 15 mg+inorganic iodine 38 mg/day and methimazole 30 mg/day as initial therapy for Graves' disease patients with moderate to severe hyperthyroidism.
Ito, K; Kunii, Y; Matsumoto, M; Mukasa, K; Nagataki, S; Noh, JY; Sato, S; Sugino, K; Suzuki, M; Taniyama, M; Yasuda, S, 2015
)
0.67
" Adverse effects that required discontinuation of MMI were more frequent in the M30-treated than in the M15+I-treated group (14."( Comparison of efficacy and adverse effects between methimazole 15 mg+inorganic iodine 38 mg/day and methimazole 30 mg/day as initial therapy for Graves' disease patients with moderate to severe hyperthyroidism.
Ito, K; Kunii, Y; Matsumoto, M; Mukasa, K; Nagataki, S; Noh, JY; Sato, S; Sugino, K; Suzuki, M; Taniyama, M; Yasuda, S, 2015
)
0.67
" Antithyroid arthritis syndrome presenting as a migratory polyarthritis is a severe adverse effect of a common pediatric disease and should therefore be recognized by pediatricians."( Migratory polyarthritis as an adverse effect of thiamazole use in a 13-year-old girl with Graves' disease.
de Laat, P; Draaisma, JM; Janson, JA, 2015
)
0.42
"The management of melasma is still challenging, and new treatment modalities with favorable side effect profile are required."( The efficacy and safety of topical 5% methimazole vs 4% hydroquinone in the treatment of melasma: A randomized controlled trial.
Dadkhahfar, S; Gheisari, M; Moghimi, HR; Najar Nobari, N; Niknejad, N; Olamaei, E, 2020
)
0.83
"This study indicates that Tripterygium glycosides enhances the effect of thiamazole and prednisone in the treatment of hyperthyroidism and without increasing the risk of adverse events."( Efficacy and safety of tripterygium glycosides in the treatment of hyperthyroidism: A systemic review and meta-analysis.
Gao, J; He, C; Jia, S; Xie, C, 2020
)
0.56
" The secondary outcomes were liver function indexes and adverse reactions in MMI and PTU groups."( The efficiency and safety of methimazole and propylthiouracil in hyperthyroidism: A meta-analysis of randomized controlled trials.
Chen, L; Fu, X; Jin, L; Tan, S, 2021
)
0.91
"This study compared the degree of sustained control of hyperthyroidism in patients with toxic multinodular goiter (TMNG) treated with long-term methimazole (LT-MMI) or radioactive iodine (RAI)."( Efficacy and Safety of Long-Term Methimazole versus Radioactive Iodine in the Treatment of Toxic Multinodular Goiter.
Abdi, H; Amouzegar, A; Azizi, F; Mehran, L; Saadat, N; Takyar, MA, 2022
)
1.2
" No major treatment-related adverse events were observed in either group."( Efficacy and Safety of Long-Term Methimazole versus Radioactive Iodine in the Treatment of Toxic Multinodular Goiter.
Abdi, H; Amouzegar, A; Azizi, F; Mehran, L; Saadat, N; Takyar, MA, 2022
)
1
" There was no significant difference in the adverse events between the two groups."( Comparative effectiveness and safety of topical methimazole 5% monotherapy versus combination of Q-Switched Nd: YAG Laser and topical methimazole 5% in patients with refractory melasma.
Beyzaee, AM; Goldust, M; Golpour, M; Mostaghiman, R; Patil, A; Rokni, GR, 2023
)
1.17
" Prophylaxis is safe and effective in this setting, especially in cardiopathic patients."( Safety and efficacy of prophylactic treatment for hyperthyroidism induced by iodinated contrast media in a high-risk population.
Bardi, M; Censi, S; Clausi, C; Manso, J; Merante Boschin, I; Mian, C; Piva, I; Schiavon, B; Tona, F, 2023
)
0.91
" Leukocytoclastic vasculitis is described among dermatologic adverse effects of PTU."( [Leukocytoclastic vasculitis as an adverse effect of propylthiouracil. A case report].
Cortés-Guzmán, JS; Domínguez, JD; Pinzón-Tovar, A; Veloza, KT, 2023
)
0.91

Pharmacokinetics

Methimazole affects the disposition of ethionamide mediated by FMO3. The time at maximal concentration and elimination half-life were longer for 10 mg transdermal methimazoles (5.2 mg)

ExcerptReferenceRelevance
" A one-compartment model was used for the analysis of examined pharmacokinetic parameters."( [Comparison of thiamazole pharmacokinetics in healthy individuals and patients with hyperthyroidism].
Czekalski, S; Gawrońska-Szklarz, B; Syrenicz, A; Wójcicki, J,
)
0.13
" No evidence was found for the importance of initial plasma levels of thyroxine or triiodothyronine on pharmacokinetic parameters of thiamazole."( Pharmacokinetic parameters of thiamazole in hyperthyroid patients responding rapidly and slowly to the treatment.
Czekalski, S; Gawrońska-Szklarz, B; Syrenicz, A; Wójcicki, J,
)
0.13
"05) shorter in the cats with hyperthyroidism than in the normal cats, but there was no significant difference between the mean values for total body clearance (CL), steady state volume of distribution (Vdss), terminal elimination rate constant (ke), or serum terminal half-life (t1/2) in the two groups of cats."( Pharmacokinetics of methimazole in normal cats and cats with hyperthyroidism.
Aucoin, DP; Peterson, ME; Trepanier, LA, 1991
)
0.6
"The performed studies covered 48 subjects, inhabiting the Western Pomerania, therein 40 patients with hyperthyroidism in the course of Graves-Basedow's disease (32 females and 8 males, aged 21-64 years) as well as 8 healthy individuals (5 females and 3 males, aged 23-36 years, with negative anamnesis towards thyroid diseases), who made up the control group at determining the pharmacokinetic parameters after a single oral dose containing 60 mg of thiamazole."( [Serum thyroxine and triiodothyronine levels after a single dose and after 2-month-long thiamazole treatment of Graves' disease with reference to drug's pharmacokinetics].
Syrenicz, A, 1990
)
0.28
" These pharmacokinetic parameters showed a wide variation among the patients, but were quite reproducible in the same subject."( Pharmacokinetics of methimazole in children and adolescents with Graves' disease. Studies on plasma and intrathyroidal concentrations.
Inyaku, F; Kumai, M; Naitoh, Y; Okuno, A; Sanae, N; Suzuki, Y; Yano, K, 1987
)
0.6
" The pharmacokinetic parameters of MMI were estimated in 5 normal subjects and 15 hyperthyroid patients according to a two-compartment model after intravenous injection of a 10 mg dose."( Pharmacokinetics of methimazole in normal subjects and hyperthyroid patients.
Okamura, Y; Shigemasa, C; Tatsuhara, T, 1986
)
0.59
" The volume of distribution approximated total body water; the biological half-life was 2-3 h in euthyroid and about 6 h in hyperthyroid patients."( Pharmacokinetics of methimazole in humans.
Hengstmann, JH; Hohn, H, 1985
)
0.59
" Blood and urine samples for pharmacokinetic analysis were collected over a 24-hour period."( Pharmacokinetics and short-term clinicopathologic changes after intravenous administration of a high dose of methimazole in dogs.
Elfarra, AA; Hutson, PR; Panciera, DL; Vail, DM, 1994
)
0.5
" In a pharmacokinetic study, MMI treatment significantly decreased the peak plasma concentration of the active, P450-generated metabolite 4-hydroxy-CPA, from 84."( Impact of liver P450 reductase suppression on cyclophosphamide activation, pharmacokinetics and antitumoral activity in a cytochrome P450-based cancer gene therapy model.
Huang, Z; Raychowdhury, MK; Waxman, DJ, 2000
)
0.31
" Mild hyperthyroidism showed nearly no effect on the plasma concentration, Cmax and AUC of diazepam in the rats."( [Effects of different thyroid status on the pharmacokinetics of diazepam].
Lou, Y; Xu, F; Zhang, Y, 1998
)
0.3
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"Hyperthyroid patients showed significantly lower serum digoxin concentrations, shorter T1/2 beta and a significantly smaller area under the concentration curve (AUC) that the control group."( [Pharmacokinetics of digoxin in hyperthyroidism. Effect of methimazole].
Dec, R; Gasińska, T; Izbicka, M, 2010
)
0.6
" The time at maximal concentration and elimination half-life were longer for 10 mg transdermal methimazole (5."( The pharmacokinetics of methimazole in a novel lipophilic formulation administered transdermally to healthy cats.
Bridges, J; Chambers, JP; Gieseg, MA; Hill, KE, 2014
)
0.93
" The drug-drug interaction leading to methimazole affecting the disposition of ethionamide mediated by FMO3 was then quantitated using a bottom-up approach with a physiologically based pharmacokinetic framework."( Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions With Ethionamide Involving Impact of Genetic Polymorphism on FMO3.
Ahn, S; Ghim, JL; Kim, MJ; Nguyen, PTT; Parvez, MM; Shin, JG; Yoo, SE, 2019
)
0.78

Compound-Compound Interactions

Methimazole (Y-M) can effectively improve thyroid function and decrease thyrotropin-receptor antibody level. The drug-drug interaction leading to methimazoles affecting the disposition of ethionamide mediated by FMO3 was then quantitated using a bottom-up approach.

ExcerptReferenceRelevance
"The authors analyzed clinically the results of treatment of 237 patients with diffuse toxic goiter with radioactive iodine in combination with prolonged antithyroidal therapy (12--18 months)."( [Treatment of diffuse toxic goiter with radioactive iodine in combination with prolonged antithyroid therapy].
Khramtsova, VIa; Potin, VV; Shliakhtina, LG,
)
0.13
" Group A patients (n = 31) received either methimazole (40-100 mg daily) or propylthiouracil (400-900 mg daily) combined with T3 daily throughout treatment."( The evolution of Graves' ophthalmopathy during treatment with antithyroid drug alone and combined with triiodothyronine.
Bromberg, N; Romaldini, JH; Sgarbi, JA; Werner, MC; Werner, RS, 1992
)
0.55
"We have carried out a prospective study to investigate whether orbital radiotherapy combined with high dose systemic glucocorticoids is more effective than orbital radiotherapy alone for Graves' ophthalmopathy."( Orbital radiotherapy combined with high dose systemic glucocorticoids for Graves' ophthalmopathy is more effective than radiotherapy alone: results of a prospective randomized study.
Bartalena, L; Bogazzi, F; Bruno-Bossio, G; Lepri, A; Marcocci, C; Pinchera, A, 1991
)
0.28
" Free T3 levels combined with concurrent TSH levels permit differentiation of mild hyperthyroidism from delayed pituitary recovery."( Effective methimazole dose for childhood Graves' disease and use of free triiodothyronine combined with concurrent thyroid-stimulating hormone level to identify mild hyperthyroidism and delayed pituitary recovery.
Boudreau, C; Slyper, AH; Wyatt, D, 2005
)
0.73
" The octreotide in combination with thiamazole treatment for 14 months controlled thyroid hormone concentration and decreased the thyroid mass, and ultimately, the thiamazole could be stopped."( A case of TSH-producing adenoma treated with octreotide in combination with thiamazole for the control of TSH and thyroid hormones after trans-sphenoidal neurosurgery.
Fukushima, S; Haruki, T; Hashimoto, N; Kawamata, T; Koike, M; Kubo, O; Matsuura, H; Ogino, J; Takahashi, M; Yoneda, C, 2011
)
0.37
" Overall, the results presented herein show that PCLS are a useful and reliable tool for short-term studies on metabolic drug-drug interactions in the bovine species."( Assessment of liver slices for research on metabolic drug-drug interactions in cattle.
García, JP; Lanusse, CE; Lifschitz, AL; Maté, ML; Quiroga, MA; Virkel, GL; Viviani, P, 2017
)
0.46
" Former studies have shown Yingliu mixture combined with methimazole (Y-M) can effectively improve thyroid function and decrease thyrotropin-receptor antibody level."( Clinical efficacy of Yingliu mixture combined with metimazole for treating diffuse goitre with hyperthyroidism and its impact on related cytokines.
Cong, Y; Lian, Z; Ma, M; Tang, H; Wu, T; Yang, H; Yang, X; Zeng, J; Zhang, W, 2017
)
0.7
" The drug-drug interaction leading to methimazole affecting the disposition of ethionamide mediated by FMO3 was then quantitated using a bottom-up approach with a physiologically based pharmacokinetic framework."( Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions With Ethionamide Involving Impact of Genetic Polymorphism on FMO3.
Ahn, S; Ghim, JL; Kim, MJ; Nguyen, PTT; Parvez, MM; Shin, JG; Yoo, SE, 2019
)
0.78
"A patient with underlying Hashimoto's thyroiditis developed amiodarone-induced thyrotoxicosis type 1 that was successfully treated using methimazole in combination with potassium iodide."( Successful Treatment of Amiodarone-induced Thyrotoxicosis Type 1 in Combination with Methimazole and Potassium Iodide in a Patient with Hashimoto's Thyroiditis.
Hirose, T; Ikehara, K; Katoh, D; Kumashiro, N; Tsuboi, K; Uchino, H; Yoshino, H, 2020
)
0.98
"To investigate the effects of levothyroxine combined with methimazole on the clinical efficacy of hyperthyroidism treatment."( The effects of levothyroxine combined with methimazole on the clinical efficacy of hyperthyroidism treatment.
An, Y; Hou, B; Liu, H; Sun, L; Wu, L; Zhang, M, 2022
)
1.23

Bioavailability

Methimazole decreased sperm forward motility, in vivo fertilizing ability, bioavailability of androgens, AR status, and secretory activity of the epididymis in adult rats. The absolute bioavailability after oral administration of 10mg methimazoles in the fasting state was high, with a mean of 93%.

ExcerptReferenceRelevance
" The bioavailability of two 5 mg tablet formulations of carbimazole (Neomercazole [A] and Carbazole [B]) have been compared in six euthyroid subjects."( Bioavailability of two tablet preparations of carbimazole in man.
Ilett, KF; Shenfield, GM; Tearne, P; Tjokrosetio, R,
)
0.13
" The bioavailability of MMI ranged from 27% to 100% (mean = 81."( Pharmacokinetics of intravenous and oral methimazole following single- and multiple-dose administration in normal cats.
Aucoin, DP; Peterson, ME; Trepanier, LA, 1991
)
0.55
"The effects of methimazole (MTZ), metyrapone (MTP) and quinine (QNE) on the pharmacokinetics and bioavailability of parenterally administered netobimin (NTB) and its major metabolites, albendazole sulphoxide (ABZSO) and albendazole sulphone (ABZSO2), were studied in sheep."( Enhancement of the plasma concentration of albendazole sulphoxide in sheep following coadministration of parenteral netobimin and liver oxidase inhibitors.
Lanusse, CE; Prichard, RK, 1991
)
0.63
" After oral administration, the mean bioavailability of methimazole was high in both the normal cats (77."( Pharmacokinetics of methimazole in normal cats and cats with hyperthyroidism.
Aucoin, DP; Peterson, ME; Trepanier, LA, 1991
)
0.85
" The absolute bioavailability after oral administration of 10mg methimazole in the fasting state was high, with a mean of 93%."( Pharmacokinetic properties and bioavailability of methimazole.
Dahlberg, PA; Jansson, R; Lindström, B,
)
0.62
"In this study we investigated the oral bioavailability of therapeutic doses of two antithyroid drugs, methimazole and carbimazole, in seven euthyroid subjects."( Comparative bioavailability of carbimazole and methimazole.
Dahlberg, PA; Jansson, R; Lindström, B, 1983
)
0.74
" Area under the concentration-time curve (AUC), maximum concentration (Cmax), and absolute bioavailability were all significantly lower for the transdermal route (0."( Bioavailability of transdermal methimazole in a pluronic lecithin organogel (PLO) in healthy cats.
Hoffman, SB; Trepanier, LA; Yoder, AR, 2002
)
0.6
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" The absolute bioavailability of carbimazole was around 88 +/- 11%."( Pharmacokinetics of controlled-release carbimazole tablets support once daily dosing in cats.
Burgaud, S; Frénais, R; Horspool, LJ, 2008
)
0.35
" Bioavailability of androgens was assessed by quantifying testosterone in serum and testicular interstitial fluid and epididymal 5alpha-reductase activity/mRNA expression."( Mechanism underlying transient gestational-onset hypothyroidism-induced impairment of posttesticular sperm maturation in adult rats.
Anbalagan, J; Aruldhas, MM; Neelamohan, R; Sashi, AM; Stanley, JA; Vengatesh, G, 2010
)
0.36
"Gestational exposure to methimazole decreased sperm forward motility, in vivo fertilizing ability, bioavailability of androgens, AR status, and secretory activity of the epididymis in adult rats."( Mechanism underlying transient gestational-onset hypothyroidism-induced impairment of posttesticular sperm maturation in adult rats.
Anbalagan, J; Aruldhas, MM; Neelamohan, R; Sashi, AM; Stanley, JA; Vengatesh, G, 2010
)
0.67
" The authors also extensively discuss the details regarding the pharmacology, bioactivation, biodisposition, bioavailability and pharmacokinetic properties of the two main ATD (MMI and PTU)."( Toxicological considerations for antithyroid drugs in children.
Karras, S; Krassas, GE; Tzotzas, T, 2011
)
0.37
" The mean relative bioavailability of 10 mg transdermal methimazole compared to oral carbimazole was 48 (min 43, max 55)%."( The pharmacokinetics of methimazole in a novel lipophilic formulation administered transdermally to healthy cats.
Bridges, J; Chambers, JP; Gieseg, MA; Hill, KE, 2014
)
0.96
"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

Until 1996, we had typically prescribed 30 mg/d of methimazole (MMI) as the initial dosage for the treatment of Graves' disease at our institution. The present studies were undertaken to determine the dose-response relationship for methiazole-induced olfactory mucosal damage.

ExcerptRelevanceReference
" The first group received metizol (thiamazol) in a daily dosage of 60 mg, the second group lithium carbonate (1."( [Short-term use of lithium carbonate in the treatment of thyrotoxicosis].
Jonderko, G; Marcisz, C, 1979
)
0.26
" It has been demonstrated that dosage is higher and duration of treatment has been more protracted in antibody-positive thyrotoxicosis than in patients without these antibodies."( [Pathogenesis of Basedow's disease].
Wuttke, H, 1978
)
0.26
" Two features of the previously proposed scheme were tested:1) the effects of drug dosage and 2) the effects of iodine deficiency."( Mechanism of action of thioureylene antithyroid drugs: factors affecting intrathyroidal metabolism of propylthiouracil and methimazole in rats.
Nakashima, T; Riesco, G; Taurog, A, 1978
)
0.47
" Cause of these changes was the high thiamazole dosage (160 and 120 mg/d)."( [Taste disorders and liver parenchymal damage after administration of thiamazole (author's transl)].
Kolenda, KD, 1976
)
0.26
" Rat liver and kidney microsomes produced dose-response curves that were essentially parallel to that of LAP-744."( A radioimmunoassay of rat type I iodothyronine 5'-monodeiodinase.
Chopra, IJ; Santini, F, 1992
)
0.28
" Patient 3 fell into hypothyroidism when receiving a small dosage of methimazole."( Three patients who spontaneously developed persistent hypothyroidism during or following treatment with antithyroid drugs for Graves' hyperthyroidism.
Adachi, T; Mashiba, H; Mitani, Y; Miyazaki, S; Shigemasa, C; Tanaka, T; Taniguchi, S; Ueta, Y; Urabe, K; Yoshida, A, 1990
)
0.51
" The aim of the present study was to examine the apparently very steep dose-response relationship between elevated plasma TSH and thyroid vascular C/mass."( Thyroid vascular conductance: differential effects of elevated plasma thyrotropin (TSH) induced by treatment with thioamides or TSH-releasing hormone.
Chang, BS; Connors, JM; Dey, RD; Hedge, GA; Huffman, LJ; Michalkiewicz, M, 1991
)
0.28
" The values for mean residence time, ke and serum terminal t1/2 after oral dosing were significantly shorter in the cats with hyperthyroidism than in the normal cats."( Pharmacokinetics of methimazole in normal cats and cats with hyperthyroidism.
Aucoin, DP; Peterson, ME; Trepanier, LA, 1991
)
0.6
"To evaluate the dose-response relationship between thyroxine and tibial growth, 60 male rats age 21 days were rendered hypothyroid by administration of methimazole in the drinking water."( Biphasic response of rat tibial growth to thyroxine administration.
Cassorla, F; Huang, Z; Malozowski, S; Ren, SG; Sweet, DE, 1990
)
0.48
" Five dosage regimens ranging from 5 mg carbimazole twice daily to 15 mg methimazole twice daily were studied."( Kinetics of [123I]iodide uptake and discharge by perchlorate in studies of inhibition of iodide binding by antithyroid drugs.
Alexander, WD; Connell, JM; Hilditch, TE; McCruden, DC, 1985
)
0.5
" Although most side effects were not dangerous, in normal instances the lowest possible dosage should be administered to control hyperthyroid metabolism."( [Side effects of antithyroid therapy of hyperthyroidism. A study of 1256 continuously treated patients].
Benker, G; Cissewski, K; Meyer-Gessner, M; Olbricht, T; Reiners, C; Reinwein, D; Windeck, R, 1989
)
0.28
" A relatively low dosed thiamazol therapy has influence on haematopoiesis and peripheral blood picture only at a very small percentage, in which cases the changes mostly are fully reversible."( [Changes in the blood picture in hyperthyroidism].
Fischer, H; Hambsch, K; Herrmann, F; Langpeter, D; Mäller, P; Sorger, D, 1989
)
0.28
" In 6 of 25 patients, however, a discordant behaviour was clearly documented including dose-response curves."( Prognostic value of thyroid stimulating antibodies and TSH-binding inhibiting immunoglobulins in the follow-up of Graves' disease.
Hörmann, R; Mann, K; Müller, R; Saller, B, 1985
)
0.27
"Thyrotrophin-releasing hormone (TRH) occurs in high concentrations in the rat ventral prostate and its concentrations is regulated in a positive dose-response manner by testosterone in castrated rats."( Thyroid hormone modulation of thyrotrophin-releasing hormone (TRH) and TRH-Gly levels in the male rat reproductive system.
Bhasin, S; Hershman, JM; Pekary, AE; Smith, V; Sugawara, M; Swerdloff, RS, 1987
)
0.27
" There is a lack of controlled prospective trials studying the results of antithyroid drug therapy while considering the many variables such as disease heterogeneity, regional differences, drug dosage and duration of treatment."( Effects of high and low doses of methimazole in patients with Graves' thyrotoxicosis.
Alexander, WD; Benker, G; Beyer, J; Creutzig, H; Galvan, G; Hirche, H; Kahály, G; Lazarus, JH; McCruden, D; Reinwein, D, 1987
)
0.55
"To investigate the dose-response relationship between thyroid hormone and linear growth, we studied 10 castrated prepubertal cynomolgus monkeys."( Dose-response relationship between thyroid hormone and growth velocity in cynomolgus monkeys.
Caruso-Nicoletti, M; Cassorla, F; Cutler, GB; Garcia, H; Malozowski, S; Ren, SG; Simoni, C, 1988
)
0.27
" No specific clinical subgroup at high risk can be identified, and manifestations may occur at any dosage and at any time during therapy."( Adverse immunologic effects of antithyroid drugs.
Fantus, IG; Wing, SS, 1987
)
0.27
" During the follow-up period a transient rise in T4 and T3 concentrations was observed in two patients in Group I when the methimazole dosage was tapered or stopped because of agranulocytosis."( Effect of amiodarone on serum T4 and T3 levels in hyperthyroid patients treated with methimazole.
Decoster, C; Unger, J; Van Reeth, O, 1987
)
0.7
" In anaprilin therapy the drug should be individually dosed out with regard to its basal concentration in the blood and the degree of pulse retardation at rest."( [Pharmcodynamic evaluation of the use of anaprilin combined with merkazolil for the therapy of thyrotoxicosis].
Lebedeva, EA; Verbovaia, NI,
)
0.13
" Furthermore, they support the hypothesis that the dosage of thionamide compounds and the duration of therapy with the initial doses necessary to induce euthyroidism may vary in various parts of the world."( Environmental iodine intake affects the response to methimazole in patients with diffuse toxic goiter.
Azizi, F, 1985
)
0.52
" In general, there are no pharmacokinetic reasons to adjust dosage in the treatment of thyrotoxicosis, except in the rare case of concomitant advanced hepatic insufficiency."( Pharmacokinetic properties and bioavailability of methimazole.
Dahlberg, PA; Jansson, R; Lindström, B,
)
0.38
" The mean daily dosage of PTU was 827 (n=11) and of MMI was 88 (n=8)."( Triiodothyronine and thyroxine in hyperthyroidism. Comparison of the acute changes during therapy with antithyroid agents.
Abuid, J; Larsen, PR, 1974
)
0.25
" No detectable change in T(4) deiodination rate was observed with these agents in the dosage ranges employed in this study."( A new method for the measurement of acute alterations in thyroxine deiodination rate in man.
Nicoloff, JT, 1970
)
0.25
" Some dosage schedules of antithyroid drugs are considered, and some techniques for predicting remission status and relapse of disease are reported."( [Hyperthyroidism in children (author's transl)].
Bozzola, M; Cisternino, M; Larizza, D; Livieri, C; Lorini, R; Salvatoni, A; Severi, F,
)
0.13
"Appropriate dosage of levothyroxine for the treatment of hypothyroidism is assessed by determining the serum thyroxine (T4) concentration in secondary and tertiary types."( Laboratory tests for evaluating thyroid therapy.
Kabadi, UM, 1982
)
0.26
" These results support the hypothesis that large antithyroid drug doses may have greater immunosuppressive effects than low dosage regimens."( Comparison of effects of high and low dosage regimens of antithyroid drugs in the management of Graves' hyperthyroidism.
Bromberg, N; Farah, CS; Reis, LC; Rodrigues, HF; Romaldini, JH; Tanaka, LM; Werner, MC; Werner, RS, 1983
)
0.27
" For hyperthyroidism, the dosage of MMI was increased to 60 approximately 45 mg/day and was continued for a month; however, her thyroid function did not normalize and agranulocytosis developed."( [A case of thyroid storm associated with diabetic ketoacidosis (author's transl)].
Fukushima, H; Kato, N; Uzawa, H; Yamaguchi, K; Yano, T, 1980
)
0.26
" The clinical implications of our findings are discussed with relation to the dosage schedule commonly employed in the treatment of Graves' disease with antithyroid drugs."( Mechanism of action of thioureylene antithyroid drugs in the rat: possible inactivation of thyroid peroxidase by propylthiouracil.
Dorris, ML; Engler, H; Shiroozu, A; Taurog, A, 1983
)
0.27
" High pretreatment T3 values were comparatively common among patients in whom a fixed CMI dosage had a insufficient effect."( Studies of thyroid hormone and methimazole levels in patients with Graves' disease on a standardized anti-thyroid drug regimen.
Dahlberg, PA; Karlsson, FA; Lindström, B; Wide, L, 1981
)
0.55
" In one patient there was an initial response to single daily dose therapy, but subsequently split dosage was required for control."( Single daily dose methimazole treatment of hyperthyroidism.
Bouma, DJ; Kammer, H, 1980
)
0.59
" Further elevating O2 demand by increasing thyroid dosage did not enhance lung size beyond the level observed with the lowest dose used."( Lung growth in response to altered metabolic demand in hamsters: influence of thyroid function and cold exposure.
Thompson, ME, 1980
)
0.26
" The present studies were undertaken to determine the dose-response relationship for methimazole-induced olfactory mucosal damage and to determine whether or not similar damage occurs as a result of oral administration, mimicking the relevant route of human exposure."( Olfactory toxicity of methimazole: dose-response and structure-activity studies and characterization of flavin-containing monooxygenase activity in the Long-Evans rat olfactory mucosa.
Blake, BL; Deamer, NJ; Genter, MB; Levi, PE; Wesley, DS,
)
0.67
" Furthermore, the shrinkage of thyroid glands may further decrease the radioiodine dosage in patients with Graves' disease."( Therapeutic 131I dose in hyperthyroidism: role of pretreatment with thionamide.
Cech, R; Kabadi, U, 1994
)
0.29
"A bolus dose of methimazole (MMI) was administered IV over 1 minute to 5 healthy adult dogs at a dosage (40 mg/kg of body weight) known to impart protection against cisplatin-induced renal disease."( Pharmacokinetics and short-term clinicopathologic changes after intravenous administration of a high dose of methimazole in dogs.
Elfarra, AA; Hutson, PR; Panciera, DL; Vail, DM, 1994
)
0.85
" A dose-response relationship was observed, the minimal effective dose (i."( Studies on the goiter inhibiting action of iodolactones.
Bocanera, LV; Chester, HA; Juvenal, GJ; Krawiec, L; Pisarev, MA; Pregliasco, LB; Sartorio, G, 1994
)
0.29
" Male and female rats were dosed with 0, 5, 10, 25, or 75 mgPTI/kg/day for 13 weeks."( Subchronic toxicity study in rats with 1-methyl-3-propylimidazole-2-thione (PTI): effects on the thyroid.
Arduengo, AJ; Aschiero, M; Biegel, LB; Cook, JC; O'Connor, JC; Slone, TW, 1995
)
0.29
" As a positive control, another group received 300 mg/kg ip of 1-methyl-2-mercaptoimidazole (methimazole), a dosing regimen which destroys nearly all of the olfactory mucosa."( Characterization of olfactory deficits in the rat following administration of 2,6-dichlorobenzonitrile (dichlobenil), 3,3'-iminodipropionitrile, or methimazole.
Carlone, HB; Crofton, KM; Genter, MB; Owens, DM, 1996
)
0.71
" Possible adverse effects of this therapy include cardiovascular changes (shortening of systolic time intervals, increased frequency of atrial premature beats and, possibly, left ventricular hypertrophy) and bone changes (reduced bone density and bone mass), but the risk of these adverse effects can be minimised by carefully monitoring serum free thyroxine and free liothyronine (triiodothyronine) measurements and adjusting the dosage accordingly."( Adverse effects of thyroid hormone preparations and antithyroid drugs.
Bartalena, L; Bogazzi, F; Martino, E, 1996
)
0.29
" Methimazole treatment was initiated with a dosage of 40 mg/d, tapered to 20 mg/d after two weeks and maintained until complete remission in both groups."( [Effect of methimazole and dexamethasone on leucocyte glucocorticoid receptor, plasma ACTH, and cortisol levels in Graves' disease].
Gao, Y; Li, X; Zhang, C, 1996
)
1.59
" Preincubation with the antithyroid drug methimazole, at concentrations ranging from 0-25 microM, prevented superoxide-induced fibroblast proliferation in a dose-response pattern."( Superoxide radical production stimulates retroocular fibroblast proliferation in Graves' ophthalmopathy.
Bahn, RS; Barnes, S; Burch, HB; Lahiri, S, 1997
)
0.56
" These treatment regimens were continued for 24 weeks, and physicians were allowed to adjust MMI dosage during follow-up visits."( Effect of 1 alpha-hydroxyvitamin D3 on serum levels of thyroid hormones in hyperthyroid patients with untreated Graves' disease.
Abe, Y; Fukawa, E; Kawakami-Tani, T; Makino, I; Tanaka, H, 1997
)
0.3
" No differences between relapse rates were observed with the two different dosage regimens."( Treatment of hyperthyroidism with a small single daily dose of methimazole: a prospective long-term follow-up study.
Beniko, M; Ikota, A; Koizumi, S; Kunita, H; Mashio, Y; Matsuda, A; Matsuya, K; Mizumoto, H, 1997
)
0.54
"To explore the therapeutic effect and its mechanism mainly using traditional Chinese medicine (TCM) of replenishing Qi and nourishing Yin (RQNY) with a small dosage of Tapazol for treatment of Graves disease (GD)."( [Therapeutic effect and its mechanism exploration on mainly using traditional Chinese medicine of replenishing qi and nourishing yin in treating Graves disease].
Zha, LL, 1997
)
0.3
" As adjunctive COL treatment in hyperthyroidism allows reducing MMI dosage it may decrease the rate of dose dependent MMI side effects."( Role of colestipol in the treatment of hyperthyroidism.
Hagag, P; Nissenbaum, H; Weiss, M, 1998
)
0.3
" In examined cases the antithyroid dosage was medium high (mean 40 mg/die)."( [Methimazole-induced aplastic anemia].
Bolognesi, S; Castiglioni, MG; Mechelli, S; Siuti, E; Stefanelli, A, 1999
)
1.21
" There remains, however, significant variability among (131)I dosing regimens, and it is clear that most patients ultimately develop hypothyroidism after therapy."( High dose of (131)I therapy for the treatment of hyperthyroidism caused by Graves' disease.
Alexander, EK; Larsen, PR, 2002
)
0.31
" There were no significant differences in age, duration, or dosage between the MPO-ANCA positive and negative patients."( Prevalence of serum anti-myeloperoxidase antineutrophil cytoplasmic antibodies (MPO-ANCA) in patients with Graves' disease treated with propylthiouracil and thiamazole.
Ito, T; Kohno, M; Mukai, M; Notoya, A; Wada, N; Yoshioka, N, 2002
)
0.31
" In contrast, supplemental T(3) decreased IVL in euthyroid birds, regardless of the dosing interval, but had no effect on ME activity."( Methimazole and thyroid hormone replacement in broilers.
McMurtry, JP; Rosebrough, RW, 2003
)
1.76
" CPI was studied in relation to the cytologic parameters of the smears; clinical parameters, such as Wayne's Clinical Index (WCI) and time without treatment; laboratory parameters, such as 131I uptake and dosage of serum free thyroxin and thyroid-stimulating hormone; and thyroid ultrasound."( Thyroid cell proliferation in Graves' disease. Use of MIB-1 monoclonal antibody.
Aragon, FF; Mazeto, GM; Montenegro, MR; Oliveira, ML; Padovani, CR; Schmitt, FC,
)
0.13
" Serum TRAb levels were measured on the day of 131I dosing (D0), and at 1, 3, 6 and 12 months after 131I administration."( Serum thyrotropin-receptor autoantibodies levels after I therapy in Graves' patients: effect of pretreatment with methimazole evaluated by a prospective, randomized study.
Andrade, VA; Gross, JL; Maia, AL, 2004
)
0.53
" In contrast, supplemental T3 decreased IVL in euthyroid birds, regardless of the dosing interval, but had no effect on ME activity."( Methimazole, thyroid hormone replacement, and lipogenic enzyme gene expression in broilers.
Poch, SM; Richards, MP; Rosebrough, RW; Russell, BA, 2004
)
1.77
"Appropriate methimazole dosing for initial treatment of childhood Graves' disease is uncertain."( Effective methimazole dose for childhood Graves' disease and use of free triiodothyronine combined with concurrent thyroid-stimulating hormone level to identify mild hyperthyroidism and delayed pituitary recovery.
Boudreau, C; Slyper, AH; Wyatt, D, 2005
)
1.11
" Clinicians must be aware of the need for close anticoagulation monitoring and dosage adjustment in patients receiving concomitant warfarin and methimazole."( Effect of Graves' disease and methimazole on warfarin anticoagulation.
Busenbark, LA; Cushnie, SA, 2006
)
0.82
" Unfortunately, high dosage prednisone can be used for only a month, because of steroid toxicity."( An informative case of Graves' disease with implications for schizophrenia.
Adams, DD; Knight, JG; Manning, P; Smith, G,
)
0.13
" Using stepwise multivariate logistic regression, the authors could not identify any factors (including age, gender, family history of thyroid diseases, size of goiter, level of free T4, dosage and duration of antithyroid drugs) that would predict the remission of thyrotoxicosis with antithyroid drugs."( Thyrotoxicosis in children: treatment and outcome.
Jaruratanasirikul, S; Leethanaporn, K; Sriplung, H, 2006
)
0.33
" This study was performed to determine if the prevalence of agranulocytosis is different depending on the starting dosage of ATDs in patients with Graves' disease."( Methimazole-induced agranulocytosis in patients with Graves' disease is more frequent with an initial dose of 30 mg daily than with 15 mg daily.
Amino, N; Fukata, S; Ito, M; Kubota, S; Kudo, T; Miyauchi, A; Nishihara, E; Takata, K, 2009
)
1.8
"Until 1996, we had typically prescribed 30 mg/d of methimazole (MMI) as the initial dosage for the treatment of Graves' disease at our institution."( Methimazole-induced agranulocytosis in patients with Graves' disease is more frequent with an initial dose of 30 mg daily than with 15 mg daily.
Amino, N; Fukata, S; Ito, M; Kubota, S; Kudo, T; Miyauchi, A; Nishihara, E; Takata, K, 2009
)
2.05
"It is very likely that MMI-induced agranulocytosis occurs with a larger dosage of MMI and is dose related."( Methimazole-induced agranulocytosis in patients with Graves' disease is more frequent with an initial dose of 30 mg daily than with 15 mg daily.
Amino, N; Fukata, S; Ito, M; Kubota, S; Kudo, T; Miyauchi, A; Nishihara, E; Takata, K, 2009
)
1.8
" Linear regression analysis evaluated relationships of dosage (mg/kg), dosing interval (q24h versus q12h), and time after methimazole to all thyroid hormone concentrations."( Optimal testing for thyroid hormone concentration after treatment with methimazole in healthy and hyperthyroid cats.
Kruger, JM; Nachreiner, RF; Rutland, BE,
)
0.57
" In hyperthyroid cats, there were no significant relationships between thyroid hormone concentrations and time postpill or dosing interval."( Optimal testing for thyroid hormone concentration after treatment with methimazole in healthy and hyperthyroid cats.
Kruger, JM; Nachreiner, RF; Rutland, BE,
)
0.36
" KI was discontinued when patients showed normal free thyroxine (FT4) levels but MMI was continued with a tapering dosage until remission."( Benefit of short-term iodide supplementation to antithyroid drug treatment of thyrotoxicosis due to Graves' disease.
Amino, N; Fukata, S; Ito, M; Kubota, S; Kudo, T; Miyauchi, A; Nishihara, E; Sasaki, I; Takata, K, 2010
)
0.36
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" Coated buccal matrix tablets may represent a potential alternative dosage form for systemic delivery of MMI in hyperthyroidism management."( Buccal delivery of methimazole as an alternative means for improvement of drug bioavailability: permeation studies and matrix system design.
De Caro, V; Giandalia, G; Giannola, LI; Siragusa, MG, 2012
)
0.71
" The presence and details of birth defects, the dosage of CMZ, and the period of exposure during pregnancy were examined in these 29 pregnancies."( Carbimazole embryopathy in a Chinese population: case series and literature review.
Lao, TT; Ting, YH; Zhou, Y, 2013
)
0.39
" Amongst the 21 cases of CMZ embryopathy in the literature, 85% were exposed to a CMZ dosage of ≥20 mg/day, and the minimum duration of exposure being 7 weeks from last menstrual period."( Carbimazole embryopathy in a Chinese population: case series and literature review.
Lao, TT; Ting, YH; Zhou, Y, 2013
)
0.39
" Critical factors for its development are exposure to a CMZ dosage of ≥20 mg/day before 7 weeks of gestation."( Carbimazole embryopathy in a Chinese population: case series and literature review.
Lao, TT; Ting, YH; Zhou, Y, 2013
)
0.39
" Overall, suspensions were the most dispensed (47%), extemporaneously compounded dosage forms followed by solutions (28%), and capsules (10%)."( Evaluation of the Most Frequently Prescribed Extemporaneously Compounded Veterinary Medications at a Large Independent Community Pharmacy.
Demir, Z; Hines, R; Horsey, R; Karara, AH; Nnorom, B; Twigg, G,
)
0.13
" A quantitative model was constructed by contrasting in vitro and ex vivo AUR-TPO results and the in vivo time-course and dose-response analysis."( Extrapolating In Vitro Screening Assay Data for Thyroperoxidase Inhibition to Predict Serum Thyroid Hormones in the Rat.
Brennan, A; El-Masri, H; Ford, J; Gilbert, ME; Handa, S; Hassan, I; Paul Friedman, K, 2020
)
0.56
" Reduction of ATD dosage or replacement of thyroid hormone is suggested to relieve muscular symptoms."( Myopathy after rapid correction of hyperthyroidism: A case report and review of literature.
Gao, H; Hong, T; Lu, R; Wang, H, 2020
)
0.56
" Methimazole is usually the preferred thionamide for the treatment of hyperthyroidism if the patient is not planning to conceive or not in the first trimester of pregnancy, given the less frequent dosing and lower risk of hepatotoxicity."( Desensitization to Methimazole.
Emanuele, MA; Espiritu, B; Mazhari, A, 2021
)
1.86
" Thyroid ultrasound and serum thyroid function test were examined regularly after ablation and the MMI dosage was gradually reduced according to the results of the biochemical examination."( US-guided percutaneous microwave ablation for hyperthyroidism and immediate treatment response evaluation with contrast-enhanced ultrasound.
Xu, HX; Yu, SY; Zhang, HL; Zhu, JE, 2021
)
0.62
" We aimed to (a) develop a mathematical model capturing the dynamics of free thyroxine (FT4) during MMI treatment (b), validate this model by use of numerical simulation in comparison with real-life patient data (c), develop the software application Digital Thyroid (DigiThy) serving either as a practice tool for treating virtual patients or as a decision support system with dosing recommendations for MMI, and (d) validate this software framework by comparing the efficacy of its MMI dosing recommendations with that from clinical endocrinologists."( Mathematical Modeling of Free Thyroxine Concentrations During Methimazole Treatment for Graves' Disease: Development and Validation of a Computer-Aided Thyroid Treatment Method.
Benninger, T; Pilz, S; Reichhartinger, M; Theiler-Schwetz, V; Trummer, C, 2022
)
0.96
" It was subsequently used to create the web-based software application DigiThy as a simulation environment for treating virtual patients and an autonomous computer-aided thyroid treatment (CATT) method providing MMI dosing recommendations."( Mathematical Modeling of Free Thyroxine Concentrations During Methimazole Treatment for Graves' Disease: Development and Validation of a Computer-Aided Thyroid Treatment Method.
Benninger, T; Pilz, S; Reichhartinger, M; Theiler-Schwetz, V; Trummer, C, 2022
)
0.96
" Treatment success of MMI dosing recommendations in 41 virtually generated patients defined by achieved target FT4 concentrations preferably with low required MMI doses was similar between CATT and usual care."( Mathematical Modeling of Free Thyroxine Concentrations During Methimazole Treatment for Graves' Disease: Development and Validation of a Computer-Aided Thyroid Treatment Method.
Benninger, T; Pilz, S; Reichhartinger, M; Theiler-Schwetz, V; Trummer, C, 2022
)
0.96
" Clinical trial data are required to evaluate whether DigiThy can be approved as a decision support system with automatically generated MMI dosing recommendations."( Mathematical Modeling of Free Thyroxine Concentrations During Methimazole Treatment for Graves' Disease: Development and Validation of a Computer-Aided Thyroid Treatment Method.
Benninger, T; Pilz, S; Reichhartinger, M; Theiler-Schwetz, V; Trummer, C, 2022
)
0.96
" Her methimazole dosing had been stable at 15 mg daily for the month prior to presentation."( Concomitant methimazole-induced agranulocytosis and cholestatic jaundice in a young woman.
Alcorn, C; Anderson, J; Subarajan, P, 2022
)
1.61
" Group A and B were further subdivided depending on the reduction of dosage of thionamides."( The influence of thionamides on intra-thyroidal uptake of
Bockisch, B; Groener, D; Grünwald, F; Happel, C; Leonhäuser, B; Sabet, A, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antithyroid drugA drug used to treat hyperthyroidism by reducing the excessive production of thyroid hormones.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
1,3-dihydroimidazole-2-thionesA member of the class of imidazoles that is 1,3-dihydroimidazole-2-thione and its derivatives by substitution.
[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 (5)

PathwayProteinsCompounds
Metabolism14961108
Biological oxidations150276
Phase I - Functionalization of compounds69175
FMO oxidises nucleophiles313
thyroid hormone biosynthesis524

Protein Targets (34)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency31.62280.631035.7641100.0000AID504339
LuciferasePhotinus pyralis (common eastern firefly)Potency17.35980.007215.758889.3584AID624030
phosphopantetheinyl transferaseBacillus subtilisPotency19.95260.141337.9142100.0000AID1490
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency48.91233.189029.884159.4836AID1224846
TDP1 proteinHomo sapiens (human)Potency12.76220.000811.382244.6684AID686978
GLI family zinc finger 3Homo sapiens (human)Potency0.24340.000714.592883.7951AID1259369
AR proteinHomo sapiens (human)Potency41.19300.000221.22318,912.5098AID743035; AID743063
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency27.82980.011212.4002100.0000AID1030
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency43.23310.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency54.66730.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency27.27830.000417.946075.1148AID1346795
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency68.51990.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency16.64720.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency67.89320.001530.607315,848.9004AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency54.88050.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency68.51990.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency61.57690.000229.305416,493.5996AID743069
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency27.33420.035520.977089.1251AID504332
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency51.89640.057821.109761.2679AID1159526; AID1159528
Histone H2A.xCricetulus griseus (Chinese hamster)Potency79.90340.039147.5451146.8240AID1224896
heat shock protein beta-1Homo sapiens (human)Potency29.93120.042027.378961.6448AID743210; AID743228
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency35.25570.000627.21521,122.0200AID743202; AID743219
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.22020.00798.23321,122.0200AID2551
survival motor neuron protein isoform dHomo sapiens (human)Potency0.70790.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency0.00200.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Polyphenol oxidase 2Agaricus bisporusIC50 (µMol)1,430.00000.03403.987110.0000AID1139760
Polyphenol oxidase 2Agaricus bisporusKi470.00000.00063.28838.8900AID1139761
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)711.00000.11007.190310.0000AID1209455; AID1449628; AID1473738
Dopamine beta-hydroxylase Bos taurus (cattle)IC50 (µMol)754.00000.05001.49432.6000AID61955
Dopamine beta-hydroxylase Bos taurus (cattle)Ki380.50000.04100.13220.3440AID62121; AID62122
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50 (µMol)200.00000.05001.43904.0000AID322753
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyphenol oxidase 2Agaricus bisporusKis1,910.00002.90005.33008.8500AID1139762
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (54)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
dopamine catabolic processDopamine beta-hydroxylase Bos taurus (cattle)
norepinephrine biosynthetic processDopamine beta-hydroxylase Bos taurus (cattle)
detection of chemical stimulus involved in sensory perception of bitter tasteLactoperoxidaseHomo sapiens (human)
response to oxidative stressLactoperoxidaseHomo sapiens (human)
thiocyanate metabolic processLactoperoxidaseHomo sapiens (human)
defense response to bacteriumLactoperoxidaseHomo sapiens (human)
hydrogen peroxide catabolic processLactoperoxidaseHomo sapiens (human)
cellular oxidant detoxificationLactoperoxidaseHomo sapiens (human)
steroid biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
cholesterol biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol metabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein catabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein secretionLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of amyloid-beta clearanceLanosterol 14-alpha demethylaseHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (35)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
dopamine beta-monooxygenase activityDopamine beta-hydroxylase Bos taurus (cattle)
copper ion bindingDopamine beta-hydroxylase Bos taurus (cattle)
L-ascorbic acid bindingDopamine beta-hydroxylase Bos taurus (cattle)
heme bindingLactoperoxidaseHomo sapiens (human)
thiocyanate peroxidase activityLactoperoxidaseHomo sapiens (human)
metal ion bindingLactoperoxidaseHomo sapiens (human)
lactoperoxidase activityLactoperoxidaseHomo sapiens (human)
iron ion bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol 14-demethylase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
heme bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenLanosterol 14-alpha demethylaseHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular spaceDopamine beta-hydroxylase Bos taurus (cattle)
transport vesicle membraneDopamine beta-hydroxylase Bos taurus (cattle)
chromaffin granule lumenDopamine beta-hydroxylase Bos taurus (cattle)
secretory granule lumenDopamine beta-hydroxylase Bos taurus (cattle)
chromaffin granule membraneDopamine beta-hydroxylase Bos taurus (cattle)
extracellular regionLactoperoxidaseHomo sapiens (human)
extracellular spaceLactoperoxidaseHomo sapiens (human)
cytoplasmLactoperoxidaseHomo sapiens (human)
basolateral plasma membraneLactoperoxidaseHomo sapiens (human)
extracellular exosomeLactoperoxidaseHomo sapiens (human)
extracellular spaceLactoperoxidaseHomo sapiens (human)
endoplasmic reticulum membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (164)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary 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.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
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.
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.
AID1222071Toxicity in wild-type mouse olfactory mucosa assessed as detached epithelium from basement membrane, fractured and disorganized at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID339045Inhibition of dopamine beta-hydroxylase in Sprague-Dawley rat assessed as decrease in brain norepinephrine level at 50 mg/kg, ip after 2.5 hrs by liquid chromatography (RVb=0.216+/-0.025)
AID1222096AUC (infinity) in Cyp2a5-null B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID339044Inhibition of dopamine beta-hydroxylase in Sprague-Dawley rat assessed as decrease in brain norepinephrine level at 50 mg/kg, ip after 1 hr by liquid chromatography (RVb=0.222+/-0.069)
AID1139762Mixed-type inhibition of mushroom tyrosinase-mediated L-tyrosine oxidation assessed as enzyme-substrate-inhibitor complex after 10 mins by Lineweaver-Burk plot analysis2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Inhibitory effects of novel synthetic methimazole derivatives on mushroom tyrosinase and melanogenesis.
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]
AID1222073Toxicity in Cyp2a5-null B6 mouse olfactory mucosa assessed as abnormal nasal cavity and epithelium at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222087Clearance in liver-Cpr-null C57BL/6(B6) mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222075Toxicity in wild-type B6 mouse olfactory mucosa assessed as epithelium loss measured as intact olfactory epithelium at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222095Cmax in Cyp2a5-null B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222098Toxicity in liver-Cpr-null mouse C57BL/6(B6) olfactory mucosa assessed as epithelium loss measured as intact olfactory epithelium at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
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.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1222083Half life in liver-Cpr-null C57BL/6(B6) mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222076Drug metabolism in wild-type mouse olfactory mucosa microsomes assessed as rate of disappearance of compound at 5 uM after 15 mins2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
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
AID61955Inhibition of Dopamine beta hydroxylase.1986Journal of medicinal chemistry, Dec, Volume: 29, Issue:12
Multisubstrate inhibitors of dopamine beta-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione.
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).
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1222081AUC (infinity) in wild-type mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222099Toxicity in wild-type littermates mouse olfactory mucosa assessed as epithelium loss measured as intact olfactory epithelium at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID756686Activation of AMPKalpha in rat L6 cells assessed as phosphorylation at Thr172 after 40 mins to 24 hrs by Western blot analysis2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and mechanism of hypoglycemic activity of benzothiazole derivatives.
AID406949Antioxidant activity assessed as inhibition of lactoperoxidase-catalyzed oxidation of 2,2'-azinobis(3-ethylbenzthione 6-sulfonic acid)2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Interaction of methimazole with I2: X-ray crystal structure of the charge transfer complex methimazole-I2. implications for the mechanism of action of methimazole-based antithyroid drugs.
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).
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).
AID1222082Clearance in wild-type mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID589258Mechanism based inhibition of human cytochrome P450 2C92005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1222079Tmax in wild-type mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222092Clearance in wild-type B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222094Tmax in Cyp2a5-null B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222097Clearance in Cyp2a5-null B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1139767Antimelanogenic activity in mouse B16/F10 cells assessed as inhibition of alpha-MSH-induced melanin formation at 1 mM after 24 hrs by ELISA relative to control2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Inhibitory effects of novel synthetic methimazole derivatives on mushroom tyrosinase and melanogenesis.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1139760Inhibition of mushroom tyrosinase-mediated L-tyrosine hydroxylation after 30 mins by ELISA2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Inhibitory effects of novel synthetic methimazole derivatives on mushroom tyrosinase and melanogenesis.
AID1139766Cytotoxicity against mouse B16/F10 cells at 2 mM after 24 hrs by MTT assay2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Inhibitory effects of novel synthetic methimazole derivatives on mushroom tyrosinase and melanogenesis.
AID1222067Toxicity in Cyp2a5-null B6 mouse olfactory mucosa assessed as depletion of nonprotein sulfhydryl at 50 mg/kg, ip at 2 hrs relative to vehicle treated control2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID62121Compound was evaluated for the inhibition of Dopamine beta hydroxylase at pH 4.51986Journal of medicinal chemistry, Dec, Volume: 29, Issue:12
Multisubstrate inhibitors of dopamine beta-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione.
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.
AID756690Activation of AMPK in rat L6 cells assessed as increase of [3H]dGlc uptake at 100 uM after 5 hrs relative to control2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and mechanism of hypoglycemic activity of benzothiazole derivatives.
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).
AID1222086AUC (infinity) in liver-Cpr-null C57BL/6(B6) mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222078Half life in wild-type mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
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]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' 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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1222085Cmax in liver-Cpr-null C57BL/6(B6) mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID409956Inhibition of mouse brain 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.
AID589246Mechanism based inhibition of human cytochrome P450 2C192005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID459944Cytoprotective effect in rat cardiomyocytes under hypoxia-reoxygenation condition assessed as cell viability at 1 uM by trypan blue exclusion test2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Mitochondrial biotransformation of omega-(phenoxy)alkanoic acids, 3-(phenoxy)acrylic acids, and omega-(1-methyl-1H-imidazol-2-ylthio)alkanoic acids: a prodrug strategy for targeting cytoprotective antioxidants to mitochondria.
AID1222091AUC (infinity) in wild-type B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
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).
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.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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.
AID1222093Half life in Cyp2a5-null B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID589233Mechanism based inhibition of human cytochrome P450 2B62005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
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).
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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID756681Activation of AMPK in rat L6 cells assessed as increase of [3H]dGlc uptake at 100 uM after 5 hrs in presence of insulin2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Synthesis and mechanism of hypoglycemic activity of benzothiazole derivatives.
AID1222072Toxicity in Cyp2a5-null B6 mouse olfactory mucosa assessed as attached epithelium from basement membrane at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
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).
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.
AID1222089Tmax in wild-type B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID339040Inhibition of bovine adrenal dopamine beta-hydroxylase assessed as norepinephrine formation per mg of protein at 0.2 mM after 45 mins
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).
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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).
AID1222068Toxicity in wild-type B6 mouse olfactory mucosa assessed as depletion of nonprotein sulfhydryl at 50 mg/kg, ip at 2 hrs relative to vehicle treated control2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1222084Tmax in liver-Cpr-null C57BL/6(B6) mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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).
AID1222070Toxicity in wild-type mouse olfactory mucosa assessed as abnormal nasal cavity and epithelium at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID62122Compound was evaluated for the inhibition of Dopamine beta hydroxylase at pH 6.61986Journal of medicinal chemistry, Dec, Volume: 29, Issue:12
Multisubstrate inhibitors of dopamine beta-hydroxylase. 1. Some 1-phenyl and 1-phenyl-bridged derivatives of imidazole-2-thione.
AID1222069Toxicity in wild-type mouse olfactory mucosa assessed as epithelium loss at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
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).
AID1222088Half life in wild-type B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID345301Inhibition of lactoperoxidase-catalyzed iodination of L-tyrosine assessed as 3,5-diiodo-L-tyrosine formation by HPLC2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Antithyroid drug carbimazole and its analogues: synthesis and inhibition of peroxidase-catalyzed iodination of L-tyrosine.
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).
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1222090Cmax in wild-type B6 mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
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).
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID339046Inhibition of dopamine beta-hydroxylase in Sprague-Dawley rat assessed as decrease in brain norepinephrine level at 50 mg/kg, ip after 6 hrs by liquid chromatography (RVb=0.206+/-0.022)
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1222080Cmax in wild-type mouse plasma at 50 mg/kg, ip2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
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]
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID589110Mechanism based inhibition of human cytochrome P450 3A42005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1139761Mixed-type inhibition of mushroom tyrosinase-mediated L-tyrosine oxidation assessed as enzyme-inhibitor complex after 10 mins by Lineweaver-Burk plot analysis2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Inhibitory effects of novel synthetic methimazole derivatives on mushroom tyrosinase and melanogenesis.
AID1222100Toxicity in liver-Cpr-null C57BL/6(B6) mouse olfactory mucosa assessed as depletion of nonprotein sulfhydryl at 50 mg/kg, ip at 2 hrs relative to vehicle treated control2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
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).
AID1222077Drug metabolism in Cyp2a5-null B6 mouse olfactory mucosa microsomes assessed as rate of disappearance of compound at 5 uM after 15 mins2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1222074Toxicity in Cyp2a5-null B6 mouse olfactory mucosa assessed as epithelium loss measured as intact olfactory epithelium at 50 mg/kg, ip by hematoxylin/eosin staining2011Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6
The tissue-specific toxicity of methimazole in the mouse olfactory mucosa is partly mediated through target-tissue metabolic activation by CYP2A5.
AID322753Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 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]
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
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.
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.
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 (3,248)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901051 (32.36)18.7374
1990's677 (20.84)18.2507
2000's648 (19.95)29.6817
2010's661 (20.35)24.3611
2020's211 (6.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 96.45

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 Index96.45 (24.57)
Research Supply Index8.22 (2.92)
Research Growth Index4.50 (4.65)
Search Engine Demand Index191.43 (26.88)
Search Engine Supply Index2.13 (0.95)

This Compound (96.45)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials214 (6.12%)5.53%
Reviews185 (5.29%)6.00%
Case Studies722 (20.63%)4.05%
Observational3 (0.09%)0.25%
Other2,375 (67.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (25)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Characteristics of Islet β-cell Functions in Chinese Patients With Graves' Disease [NCT02376088]328 participants (Actual)Observational2011-06-30Completed
The Oral Microbiota in Autoimmune Thyroiditis is Distinctive And Predictive [NCT03447093]120 participants (Anticipated)Observational2017-12-23Recruiting
The Effect of Intestinal Microbiota on Treatment Sensitivity and Prognosis of Methimazole for GD [NCT03433352]90 participants (Anticipated)Observational2017-12-23Recruiting
[NCT01560299]150 participants (Actual)Interventional2010-02-28Completed
Effect of Hyperthyroidism and Its Treatment in Graves' Disease to Early Marker of Atherosclerosis: Review on the Pathway of Insulin Resistance, Lipid, Inflammation, and Endothelial Dysfunction to Pulse Wave Velocity and Carotid Intima-Media Thickness [NCT05118542]Phase 336 participants (Actual)Interventional2019-01-01Completed
A Single Arm Pilot Study to Evaluate the Safety and Feasibility of Inducing a Hypothyroxinemic State in Patients With Recurrent Glioblastoma [NCT05017610]Early Phase 10 participants (Actual)Interventional2021-10-20Withdrawn(stopped due to Per the PI-slow accrual)
Randomized Open Clinical Study to Evaluate the Efficacy of Selenium Plus Methimazole for Treatment of Graves' Hyperthyroidism [NCT02727738]30 participants (Actual)Interventional2014-01-31Completed
Prevention Relapse of Graves' Disease by Treatment With Intrathyroid Injection of Dexamethasone [NCT00917241]Phase 4218 participants (Actual)Interventional2004-06-30Completed
Phase II, Open-label, Prospective, Single-arm, Single-center Study of Induction of Hypothyroxinemia Adjunct to Conventional Therapies in GBM Patients [NCT02654041]Phase 23 participants (Actual)Interventional2016-03-31Terminated(stopped due to Drug manufacturer no longer could supply for study)
Serum Betatrophin Levels and Its Influencing Factors in Patients With Hyperthyroidism [NCT02812888]240 participants (Anticipated)Observational [Patient Registry]2016-07-31Recruiting
A Phase III, Randomized, Controlled, Open Label, no Profit, Single-center Intervention Study to Compare the Effect of a Conservative (Antithyroid Drugs) and an Ablative Approach (Radioiodine or Total Thyroidectomy) for the Treatment of Hyperthyroidism in [NCT04776993]Phase 352 participants (Anticipated)Interventional2023-03-02Recruiting
The Influence of Continuous Treatment With Antithyroid Drugs on the Effect of Radioiodine in Patients With Hyperthyroidism [NCT00150137]Phase 480 participants Interventional2003-01-31Completed
The Efficacy of Cook County Health's Methimazole Dosing Algorithm in the Setting of ne Onset Graves' Hyperthyroidism [NCT05964452]60 participants (Anticipated)Observational2022-02-14Recruiting
B Cell Depletion With the Anti-CD20 Monoclonal Antibody Rituximab in the Treatment of Graves' Disease [NCT00150111]Phase 1/Phase 220 participants Interventional2003-06-30Completed
Cardiopulmonary Capacity In Different Quartiles Ranges Of Reference For Serum Thyroid Stimulating Hormone (TSH): Sectional Evaluation And Effect Of The Use Of Methimazole In Elderly Population [NCT01849861]Phase 4200 participants (Anticipated)Interventional2011-09-30Recruiting
Targeting Transsulfuration Via Suppression of Thyroid Hormone Signaling in Progressive Glioblastoma: Phase 2 and Pharmacodynamic Trial of Methimazole in Patients With Progressive Glioblastoma [NCT05607407]Phase 219 participants (Anticipated)Interventional2023-01-30Recruiting
Comparative Study of mMASI Before and After Hyperthyroid Therapy in Hyperthyroid Subjects With Melasma [NCT04346901]Phase 123 participants (Actual)Interventional2019-08-01Completed
he Efficacy and Safety of Combining Mycophenolate Mofetil With Methimazole on Remission of Newly Diagnosis Graves' Disease (3M-RGD Trial): an Open-label, Randomized Trial [NCT06068179]Phase 2/Phase 3205 participants (Anticipated)Interventional2023-10-08Not yet recruiting
A Pilot Study of the Role of Methimazole in Patients With Polymyositis and Dermatomyositis [NCT00001421]Phase 220 participants Interventional1995-06-30Completed
The Influence of Continuous Block-replacement Therapy on the Effect of Radioiodine in Patients With Hyperthyroidism [NCT00150124]Phase 4100 participants (Actual)Interventional2003-01-31Completed
Clinical Study on the Effect of Routine Treatment and Intensive Treatment on the Regulation of Graves' Disease and the Cumulative Recurrence Two Years After Drug Withdrawal [NCT05461820]Phase 4240 participants (Anticipated)Interventional2018-05-01Recruiting
Comparison of the Effect of Bromocriptine and Pentoxifylline in Mild to Moderate Autoimmune Ophthalmopathy. A Randomized, Controlled, Single Blind, Clinical Trial. [NCT01893450]31 participants (Actual)Interventional2008-06-30Terminated(stopped due to Efficacy demonstrated on a preliminary analysis)
Adjuvant Treatment of Graves´ Ophthalmopathy With NSAID (aGO Study) [NCT01458600]Phase 465 participants (Actual)Interventional2006-09-30Completed
Gut Microbiota is Associated With Autoimmune Thyroid Disease(GD and HT) [NCT03390582]200 participants (Anticipated)Observational2017-04-20Recruiting
The Observation Study of Graves' Disease Cohort [NCT05043233]1,000 participants (Anticipated)Observational [Patient Registry]2020-10-01Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]