thiamazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
1745 60-56-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • methimazole
  • methylimidazolethiol
  • thyrozol
  • thymidazole
  • thymidazol
  • thycapzol
  • thiamazole
  • tapazole
  • methymazol
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.
  • Molecular weight: 114.17
  • Formula: C4H6N2S
  • CLOGP: -0.34
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 15.27
  • ALOGS: -1
  • ROTB: 0
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 8.76 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
BA (Bioavailability) 95 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.86 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.70 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.40 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 200 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.094 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.728 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 17.824 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 2.286 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 91.430 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 85.570 % High 1
herg hERG pIC50 3.689 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 1.585 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.090 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 84.540 % High 1
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MARK4,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 44
kinase-selectivity-class ACVR2B,AXL,BRAF,CDK9,DDR1,ERBB2,GRK2,MAPK7,MARK4,PRKDC,SIK2,STK33,SYK,TEK,TTK 15
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.255 High 1
mh-clint Mouse hepatocyte intrinsic clearance 1.811 High 1
mppb Mouse plasma protein binding (% unbound) 95.680 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.423 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 83.140 % High 1
rh-clint Rat hepatocyte intrinsic clearance 0.617 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 97.810 % High 1
rppb Rat plasma protein binding (% unbound) 86.540 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 519.996 uM High 1

Approvals:

DateAgencyCompanyOrphan
June 21, 1950 FDA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Agranulocytosis 547.75 12.81 205 13748 34797 90579697
Thyrotoxic crisis 350.11 12.81 71 13882 1160 90613334
Hyperthyroidism 325.94 12.81 118 13835 18192 90596302
Hypothyroidism 113.09 12.81 81 13872 53046 90561448
Endocrine ophthalmopathy 90.69 12.81 23 13930 1051 90613443
Antithyroid arthritis syndrome 82.16 12.81 11 13942 4 90614490
Thyrotoxic myopathy 64.29 12.81 9 13944 8 90614486
Choanal atresia 60.47 12.81 9 13944 17 90614477
Exophthalmos 49.16 12.81 16 13937 1786 90612708
Neutropenia 46.29 12.81 105 13848 224799 90389695
Thyroid stimulating immunoglobulin increased 45.27 12.81 9 13944 132 90614362
Anti-neutrophil cytoplasmic antibody positive vasculitis 43.41 12.81 18 13935 3975 90610519
Blood thyroid stimulating hormone decreased 43.28 12.81 20 13933 5720 90608774
Goitre 43.13 12.81 21 13932 6746 90607748
Arthropathy 41.90 12.81 4 13949 366238 90248256
Drug-induced liver injury 41.71 12.81 60 13893 90258 90524236
Drug intolerance 39.73 12.81 10 13943 447581 90166913
Systemic lupus erythematosus 38.76 12.81 5 13948 361891 90252603
Jaundice cholestatic 37.98 12.81 22 13931 10021 90604473
Toxic goitre 37.65 12.81 6 13947 21 90614473
Thyroxine free increased 35.83 12.81 11 13942 1016 90613478
Synovitis 34.25 12.81 5 13948 329747 90284747
Deafness neurosensory 34.16 12.81 18 13935 6823 90607671
Physical disability 33.58 12.81 15 13938 3966 90610528
Joint swelling 33.34 12.81 18 13935 503282 90111212
Economic problem 33.02 12.81 14 13939 3267 90611227
Contraindicated product administered 32.92 12.81 5 13948 320134 90294360
Deafness permanent 32.91 12.81 9 13944 552 90613942
Eosinophilic pleural effusion 32.57 12.81 7 13946 153 90614341
Treatment noncompliance 32.56 12.81 40 13913 51687 90562807
Cardiac arrest 32.35 12.81 58 13895 104877 90509617
Insulin autoimmune syndrome 32.15 12.81 7 13946 163 90614331
Toxic nodular goitre 31.95 12.81 6 13947 64 90614430
Pericarditis 30.76 12.81 3 13950 270148 90344346
Infusion related reaction 30.51 12.81 13 13940 416767 90197727
Stevens-Johnson syndrome 29.43 12.81 29 13924 29347 90585147
Dysmorphism 29.35 12.81 12 13941 2556 90611938
Lower respiratory tract infection 27.97 12.81 3 13950 250656 90363838
Concomitant disease aggravated 27.84 12.81 19 13934 11499 90602995
Therapeutic product effect decreased 27.06 12.81 5 13948 277566 90336928
Oropharyngeal pain 26.18 12.81 56 13897 115131 90499363
Mucocutaneous candidiasis 25.83 12.81 4 13949 11 90614483
Cardiac failure 25.77 12.81 54 13899 109442 90505052
Impaired healing 25.64 12.81 3 13950 234196 90380298
Thyroidectomy 25.33 12.81 9 13944 1310 90613184
Aplasia cutis congenita 25.04 12.81 5 13948 75 90614419
Tinnitus 25.00 12.81 32 13921 43070 90571424
Pulmonary alveolar haemorrhage 24.99 12.81 14 13939 5984 90608510
Wound 24.60 12.81 8 13945 302972 90311522
Emotional distress 24.13 12.81 29 13924 36633 90577861
Drug interaction 23.14 12.81 94 13859 276359 90338135
Tonsillitis 23.04 12.81 14 13939 6955 90607539
Premature delivery 22.83 12.81 29 13924 38733 90575761
Neuroendocrine tumour of the lung metastatic 22.82 12.81 5 13948 120 90614374
Septic shock 22.78 12.81 44 13909 84116 90530378
Anaemia 22.76 12.81 111 13842 352691 90261803
Abdominal discomfort 22.72 12.81 24 13929 477304 90137190
Thyroid dermatopathy 22.68 12.81 4 13949 29 90614465
Thyroid disorder 22.52 12.81 20 13933 17765 90596729
Sopor 22.25 12.81 23 13930 24621 90589873
Hypoglycaemia 22.03 12.81 39 13914 69809 90544685
Bleeding varicose vein 21.99 12.81 6 13947 365 90614129
Irritable bowel syndrome 21.87 12.81 3 13950 207445 90407049
Autophony 21.81 12.81 4 13949 37 90614457
Acquired epidermolysis bullosa 21.62 12.81 4 13949 39 90614455
Myxoedema 21.41 12.81 5 13948 161 90614333
Atrial fibrillation 20.70 12.81 56 13897 133555 90480939
Epiphysiolysis 20.29 12.81 4 13949 56 90614438
Pancytopenia 20.25 12.81 52 13901 120211 90494283
Respiratory syncytial virus infection 20.07 12.81 15 13938 10465 90604029
Polyarthritis 20.05 12.81 19 13934 18331 90596163
Neonatal thyrotoxicosis 20.04 12.81 3 13950 6 90614488
Rheumatoid arthritis 19.89 12.81 16 13937 362598 90251896
Mobility decreased 19.69 12.81 7 13946 250727 90363767
Thyrotoxic cardiomyopathy 19.44 12.81 3 13950 8 90614486
Tri-iodothyronine increased 19.30 12.81 5 13948 249 90614245
Folliculitis 19.24 12.81 4 13949 204349 90410145
Type 2 diabetes mellitus 19.09 12.81 4 13949 203240 90411254
Thyroid haemorrhage 19.05 12.81 4 13949 78 90614416
Disease recurrence 18.83 12.81 26 13927 37627 90576867
Multiple organ dysfunction syndrome 18.83 12.81 36 13917 68300 90546194
Left-to-right cardiac shunt 18.78 12.81 5 13948 277 90614217
Tinea faciei 18.51 12.81 3 13950 12 90614482
Functional residual capacity increased 18.30 12.81 4 13949 95 90614399
Hypersensitivity vasculitis 18.13 12.81 10 13943 4149 90610345
Hepatitis cholestatic 18.08 12.81 13 13940 8548 90605946
Serratia bacteraemia 17.65 12.81 3 13950 17 90614477
Foetal exposure during pregnancy 17.60 12.81 27 13926 42948 90571546
Exposure during pregnancy 17.56 12.81 78 13875 238332 90376162
Leukopenia 17.43 12.81 44 13909 100666 90513828
Thyroxine free abnormal 17.23 12.81 3 13950 20 90614474
Plasmacytosis 17.15 12.81 4 13949 128 90614366
Thyroxine free decreased 17.10 12.81 6 13947 842 90613652
Product administered to patient of inappropriate age 17.08 12.81 10 13943 4643 90609851
Ecthyma 16.88 12.81 5 13948 409 90614085
Swelling 16.84 12.81 24 13929 419034 90195460
Thyroiditis 16.56 12.81 9 13944 3628 90610866
Clinodactyly 16.51 12.81 4 13949 151 90614343
Systemic candida 16.49 12.81 10 13943 4949 90609545
Pleural effusion 16.41 12.81 46 13907 111945 90502549
Palpitations 16.11 12.81 52 13901 136676 90477818
Skin sensitisation 16.05 12.81 6 13947 1009 90613485
Symptom masked 16.01 12.81 6 13947 1015 90613479
Blood cholesterol increased 16.00 12.81 6 13947 208006 90406488
Spigelian hernia 15.97 12.81 3 13950 32 90614462
Bradycardia 15.96 12.81 38 13915 83809 90530685
Febrile neutropenia 15.83 12.81 57 13896 158292 90456202
Jaundice 15.58 12.81 22 13931 32495 90581999
Psoriatic arthropathy 15.34 12.81 8 13945 228327 90386167
Stomatitis 15.21 12.81 12 13941 274686 90339808
Premature baby 15.15 12.81 19 13934 25058 90589436
Product use in unapproved indication 15.13 12.81 96 13857 336140 90278354
Tri-iodothyronine free increased 14.94 12.81 4 13949 226 90614268
Microscopic polyangiitis 14.93 12.81 4 13949 227 90614267
Choluria 14.47 12.81 4 13949 255 90614239
Neonatal respiratory distress 14.37 12.81 5 13948 684 90613810
Pancreatitis acute 14.33 12.81 21 13932 32094 90582400
Eosinophil percentage decreased 14.32 12.81 4 13949 265 90614229
Autoimmune neutropenia 14.31 12.81 4 13949 266 90614228
Fibromyalgia 14.19 12.81 7 13946 206262 90408232
Hepatic enzyme increased 14.16 12.81 21 13932 360715 90253779
Kidney transplant rejection 14.14 12.81 9 13944 4848 90609646
Ear discomfort 13.98 12.81 12 13941 10188 90604306
Drug ineffective 13.94 12.81 294 13659 1384004 89230490
Antineutrophil cytoplasmic antibody positive 13.94 12.81 5 13948 748 90613746
Treatment failure 13.66 12.81 16 13937 303912 90310582
Acute phase reaction 13.49 12.81 4 13949 328 90614166
Renal infarct 13.35 12.81 6 13947 1609 90612885
Thyroid function test abnormal 13.15 12.81 8 13945 3981 90610513
Impaired quality of life 13.13 12.81 17 13936 23127 90591367
Off label use 13.07 12.81 240 13713 1102012 89512482
Failure to suspend medication 13.05 12.81 3 13950 90 90614404
Bladder transitional cell carcinoma 13.05 12.81 5 13948 899 90613595
Hypersensitivity 13.00 12.81 32 13921 454645 90159849

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hyperthyroidism 202.69 16.89 76 5886 14265 42601108
Thyrotoxic crisis 176.33 16.89 37 5925 797 42614576
Thyrotoxic periodic paralysis 146.24 16.89 25 5937 165 42615208
Agranulocytosis 95.07 16.89 57 5905 30555 42584818
Hypothyroidism 58.78 16.89 43 5919 32041 42583332
Cardiac arrest 44.56 16.89 65 5897 109255 42506118
Polymerase chain reaction 43.31 16.89 8 5954 86 42615287
Goitre 42.30 16.89 14 5948 1816 42613557
Deafness permanent 41.18 16.89 9 5953 236 42615137
Kounis syndrome 37.40 16.89 15 5947 3353 42612020
Endocrine ophthalmopathy 37.28 16.89 8 5954 192 42615181
Product administered to patient of inappropriate age 35.55 16.89 16 5946 4745 42610628
Cardiogenic shock 34.42 16.89 33 5929 35607 42579766
Drug ineffective 33.80 16.89 175 5787 630022 41985351
Albumin urine present 31.68 16.89 8 5954 396 42614977
Exomphalos 31.12 16.89 7 5955 210 42615163
Urine leukocyte esterase positive 30.76 16.89 8 5954 446 42614927
Pulseless electrical activity 29.55 16.89 17 5945 8420 42606953
Product use in unapproved indication 27.87 16.89 72 5890 184384 42430989
Haemoglobinuria 27.49 16.89 8 5954 678 42614695
Drug-induced liver injury 27.11 16.89 30 5932 38243 42577130
Atrial fibrillation 27.02 16.89 60 5902 139533 42475840
Physical disability 26.69 16.89 10 5952 1863 42613510
Cholestatic liver injury 26.22 16.89 12 5950 3697 42611676
Pericarditis fungal 25.28 16.89 6 5956 229 42615144
Mouth swelling 24.93 16.89 10 5952 2236 42613137
Urinary bladder rupture 24.22 16.89 5 5957 99 42615274
Economic problem 23.47 16.89 9 5953 1786 42613587
Jaundice cholestatic 22.26 16.89 12 5950 5241 42610132
Glycosuria 22.05 16.89 8 5954 1362 42614011
Urine ketone body present 21.91 16.89 8 5954 1386 42613987
Respiratory tract haemorrhage 21.83 16.89 8 5954 1401 42613972
Blood sodium decreased 21.79 16.89 19 5943 18143 42597230
Blood cyanide increased 21.57 16.89 4 5958 44 42615329
Antithyroid arthritis syndrome 21.55 16.89 3 5959 3 42615370
Thyroiditis 21.41 16.89 10 5952 3226 42612147
Loss of proprioception 21.38 16.89 6 5956 446 42614927
Autoimmune thyroiditis 20.93 16.89 8 5954 1574 42613799
Treatment noncompliance 20.81 16.89 26 5936 37646 42577727
Cardiac failure 20.74 16.89 46 5916 106810 42508563
Coagulation time shortened 20.53 16.89 5 5957 213 42615160
Axial spondyloarthritis 20.27 16.89 6 5956 539 42614834
Tracheo-oesophageal fistula 20.16 16.89 6 5956 550 42614823
Product use issue 19.57 16.89 37 5925 76714 42538659
Toxic goitre 19.01 16.89 3 5959 11 42615362
Off label use 18.49 16.89 152 5810 638183 41977190
Ischaemic hepatitis 18.46 16.89 8 5954 2169 42613204
Thyroid operation 18.25 16.89 3 5959 15 42615358
Exophthalmos 17.59 16.89 6 5956 852 42614521

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Agranulocytosis 562.02 13.01 250 17979 61510 110509560
Thyrotoxic crisis 492.99 13.01 104 18125 1936 110569134
Hyperthyroidism 409.28 13.01 161 18068 29100 110541970
Hypothyroidism 154.80 13.01 114 18115 72785 110498285
Thyrotoxic periodic paralysis 146.71 13.01 26 18203 180 110570890
Endocrine ophthalmopathy 107.15 13.01 28 18201 1345 110569725
Antithyroid arthritis syndrome 101.63 13.01 14 18215 8 110571062
Deafness permanent 67.93 13.01 18 18211 913 110570157
Cardiac arrest 65.74 13.01 117 18112 196636 110374434
Thyrotoxic myopathy 63.68 13.01 9 18220 8 110571062
Physical disability 60.64 13.01 25 18204 5081 110565989
Drug-induced liver injury 60.26 13.01 86 18143 119981 110451089
Exophthalmos 59.93 13.01 20 18209 2253 110568817
Goitre 59.17 13.01 26 18203 6178 110564892
Economic problem 58.65 13.01 23 18206 4108 110566962
Anti-neutrophil cytoplasmic antibody positive vasculitis 55.90 13.01 24 18205 5393 110565677
Drug ineffective 55.30 13.01 433 17796 1520107 109050963
Jaundice cholestatic 53.22 13.01 32 18197 14576 110556494
Toxic goitre 53.12 13.01 9 18220 46 110571024
Treatment noncompliance 50.12 13.01 61 18168 72929 110498141
Cardiac failure 43.78 13.01 96 18133 187530 110383540
Deafness neurosensory 42.81 13.01 24 18205 9595 110561475
Concomitant disease aggravated 42.59 13.01 29 18200 16335 110554735
Thyroid stimulating immunoglobulin increased 42.52 13.01 9 18220 170 110570900
Polymerase chain reaction 39.85 13.01 8 18221 115 110570955
Thyroxine free increased 39.13 13.01 13 18216 1444 110569626
Product administered to patient of inappropriate age 38.37 13.01 21 18208 8015 110563055
Atrial fibrillation 38.08 13.01 103 18126 229539 110341531
Pulseless electrical activity 37.33 13.01 27 18202 16730 110554340
Cardiogenic shock 36.28 13.01 46 18183 57292 110513778
Drug intolerance 34.45 13.01 12 18217 406500 110164570
Synovitis 34.09 13.01 3 18226 274089 110296981
Arthropathy 33.56 13.01 4 18225 287518 110283552
Blood thyroid stimulating hormone decreased 32.05 13.01 18 18211 7221 110563849
Emotional distress 30.00 13.01 37 18192 44810 110526260
Kounis syndrome 29.72 13.01 16 18213 5909 110565161
Albumin urine present 29.68 13.01 9 18220 744 110570326
Lower respiratory tract infection 29.33 13.01 3 18226 243103 110327967
Systemic lupus erythematosus 28.57 13.01 4 18225 254334 110316736
Joint swelling 28.50 13.01 19 18210 442826 110128244
Autoimmune thyroiditis 28.49 13.01 16 18213 6418 110564652
Product use in unapproved indication 28.30 13.01 147 18082 447230 110123840
Thyroiditis 28.17 13.01 16 18213 6557 110564513
Hepatitis cholestatic 27.57 13.01 23 18206 17543 110553527
Tonsillitis 27.38 13.01 17 18212 8196 110562874
Premature delivery 26.76 13.01 29 18200 30603 110540467
Infusion related reaction 26.41 13.01 15 18214 381147 110189923
Thyrotoxic cardiomyopathy 26.13 13.01 4 18225 9 110571061
Pericarditis 25.68 13.01 3 18226 219111 110351959
Neutropenia 25.01 13.01 125 18104 374495 110196575
Therapeutic product effect decreased 24.88 13.01 5 18224 244311 110326759
Jaundice 24.80 13.01 39 18190 59197 110511873
Toxic nodular goitre 24.46 13.01 5 18224 79 110570991
Haemoglobinuria 24.25 13.01 8 18221 869 110570201
Tinnitus 24.16 13.01 39 18190 60501 110510569
Eosinophilic pleural effusion 23.80 13.01 7 18222 521 110570549
Pericarditis fungal 22.57 13.01 6 18223 308 110570762
Drug interaction 22.34 13.01 150 18079 500033 110071037
Impaired healing 22.31 13.01 3 18226 196714 110374356
Polyarthritis 22.14 13.01 21 18208 18942 110552128
Tri-iodothyronine increased 21.55 13.01 6 18223 367 110570703
Autophony 21.54 13.01 4 18225 37 110571033
Insulin autoimmune syndrome 21.45 13.01 7 18222 735 110570335
Cholestatic liver injury 21.43 13.01 14 18215 7362 110563708
Off label use 21.34 13.01 356 17873 1499829 109071241
Stomatitis 21.19 13.01 9 18220 270233 110300837
Urinary bladder rupture 20.95 13.01 5 18224 165 110570905
Blood cyanide increased 20.67 13.01 4 18225 47 110571023
Rheumatoid arthritis 20.45 13.01 12 18217 299601 110271469
Bradycardia 20.23 13.01 64 18165 155453 110415617
Sopor 19.54 13.01 27 18202 36519 110534551
Leukopenia 19.14 13.01 61 18168 148730 110422340
Myxoedema 18.86 13.01 5 18224 254 110570816
Oropharyngeal pain 18.83 13.01 57 18172 135219 110435851
Thyroidectomy 18.62 13.01 7 18222 1115 110569955
Blood sodium decreased 18.55 13.01 27 18202 38292 110532778
Palpitations 18.45 13.01 63 18166 159149 110411921
Urine leukocyte esterase positive 18.37 13.01 10 18219 3776 110567294
Blood cholesterol increased 18.36 13.01 4 18225 184781 110386289
Tinea faciei 18.31 13.01 3 18226 12 110571058
Abdominal discomfort 18.10 13.01 23 18206 393835 110177235
Mucocutaneous candidiasis 17.98 13.01 4 18225 96 110570974
Respiratory tract haemorrhage 17.79 13.01 8 18221 2006 110569064
Functional residual capacity increased 17.79 13.01 4 18225 101 110570969
Acquired epidermolysis bullosa 17.75 13.01 4 18225 102 110570968
Bleeding varicose vein 17.72 13.01 6 18223 707 110570363
Thyroid haemorrhage 17.71 13.01 4 18225 103 110570967
Multiple organ dysfunction syndrome 17.55 13.01 60 18169 151650 110419420
Impaired quality of life 17.30 13.01 23 18206 29994 110541076
Stevens-Johnson syndrome 17.08 13.01 29 18200 46872 110524198
Coagulation time shortened 16.60 13.01 5 18224 404 110570666
Ischaemic hepatitis 16.46 13.01 10 18219 4638 110566432
Ill-defined disorder 16.41 13.01 3 18226 156850 110414220
Epiphysiolysis 15.87 13.01 4 18225 166 110570904
Acute phase reaction 15.82 13.01 5 18224 474 110570596
Glycosuria 15.76 13.01 8 18221 2622 110568448
Anaemia 15.59 13.01 148 18081 546938 110024132
Contraindicated product administered 15.50 13.01 11 18218 248256 110322814
Thyroid dermatopathy 15.44 13.01 3 18226 36 110571034
Irritable bowel syndrome 15.44 13.01 4 18225 164211 110406859
Hyperbilirubinaemia 15.42 13.01 22 18207 30649 110540421
Disease recurrence 15.19 13.01 32 18197 60752 110510318
Plasmacytosis 15.05 13.01 4 18225 205 110570865
Hypersensitivity vasculitis 15.05 13.01 11 18218 6926 110564144
Exposure during pregnancy 15.01 13.01 61 18168 167363 110403707
Respiratory syncytial virus infection 14.96 13.01 15 18214 14469 110556601
Psoriatic arthropathy 14.72 13.01 7 18222 196754 110374316
Hypertransaminasaemia 14.62 13.01 19 18210 24236 110546834
Thyroxine free decreased 14.58 13.01 6 18223 1214 110569856
Fibromyalgia 14.54 13.01 5 18224 170904 110400166
Tonsillitis bacterial 14.39 13.01 4 18225 243 110570827
Disability 14.20 13.01 21 18208 30202 110540868
Tri-iodothyronine free increased 14.10 13.01 4 18225 262 110570808
Pulmonary alveolar haemorrhage 14.08 13.01 17 18212 20133 110550937
Drug ineffective for unapproved indication 14.00 13.01 43 18186 102795 110468275
Cholestasis 13.90 13.01 32 18197 64486 110506584
Ventricular septal defect 13.83 13.01 5 18224 714 110570356
Pleural effusion 13.81 13.01 62 18167 177647 110393423
Hypoaesthesia 13.77 13.01 19 18210 314204 110256866
Respiratory failure 13.75 13.01 71 18158 215261 110355809
Auditory disorder 13.68 13.01 6 18223 1418 110569652
Gastrointestinal disorder 13.49 13.01 12 18217 241940 110329130
Serratia bacteraemia 13.26 13.01 3 18226 78 110570992
Musculoskeletal stiffness 13.21 13.01 16 18213 279806 110291264
Immune-mediated hepatitis 13.13 13.01 10 18219 6701 110564369

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H03BB02 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
THYROID THERAPY
ANTITHYROID PREPARATIONS
Sulfur-containing imidazole derivatives
ATC H03BB52 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
THYROID THERAPY
ANTITHYROID PREPARATIONS
Sulfur-containing imidazole derivatives
MeSH PA D006727 Hormone Antagonists
MeSH PA D013956 Antithyroid Agents
FDA MoA N0000175917 Thyroid Hormone Synthesis Inhibitors
FDA EPC N0000175918 Thyroid Hormone Synthesis Inhibitor
CHEBI has role CHEBI:50671 antithyroid drug

Related Drugs by ATC class:

H03BB Sulfur-containing imidazole derivatives 1 drug
carbimazole

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hyperthyroidism indication 34486009 DOID:7998
Thyrotoxic crisis off-label use 29028009 DOID:12837
Agranulocytosis contraindication 17182001 DOID:12987
Hypothyroidism contraindication 40930008 DOID:1459
Factor II deficiency contraindication 73975000
Leukopenia contraindication 84828003 DOID:615
Pancytopenia contraindication 127034005 DOID:12450
Liver function tests abnormal contraindication 166603001
Drug-induced hepatitis contraindication 235876009
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Bone marrow depression contraindication 307762000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

ProductApplicantIngredients
Felimazole Dechra, Ltd. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.7 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Thyroid peroxidase Enzyme INHIBITOR IC50 5.57 WOMBAT-PK CHEMBL
Lactoperoxidase Enzyme IC50 4.93 CHEMBL
Taste receptor type 2 member 38 GPCR AGONIST EC50 4.01 IUPHAR
Lactoperoxidase Enzyme IC50 5.08 CHEMBL
Dopamine beta-hydroxylase Enzyme Ki 4.35 CHEMBL

External reference:

IDSource
4017434 VUID
N0000145822 NUI
D00401 KEGG_DRUG
4017434 VANDF
C0025644 UMLSCUI
CHEBI:50673 CHEBI
MMZ PDB_CHEM_ID
CHEMBL1515 ChEMBL_ID
DB00763 DRUGBANK_ID
1349907 PUBCHEM_CID
224936 RXNORM
2293 MMSL
31962 MMSL
5073 MMSL
d00290 MMSL
002139 NDDF
37656002 SNOMEDCT_US
404864000 SNOMEDCT_US
D008713 MESH_DESCRIPTOR_UI
4198 INN_ID
6649 IUPHAR_LIGAND_ID
554Z48XN5E UNII
554Z48XN5E INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 0832-6072 TABLET 5 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 0832-6073 TABLET 10 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 11788-011 TABLET 5 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 11788-012 TABLET 10 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 23155-070 TABLET 5 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 23155-071 TABLET 10 mg ORAL ANDA 19 sections
Methimazole Human Prescription Drug Label 1 33342-335 TABLET 5 mg ORAL ANDA 19 sections
Methimazole Human Prescription Drug Label 1 33342-336 TABLET 10 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 42254-008 TABLET 5 mg ORAL ANDA 18 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 42254-009 TABLET 10 mg ORAL ANDA 18 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 50090-2366 TABLET 5 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 50090-3334 TABLET 5 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 50090-6536 TABLET 5 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 50268-495 TABLET 5 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 50268-496 TABLET 10 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 53808-0850 TABLET 10 mg ORAL ANDA 18 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 53808-0949 TABLET 10 mg ORAL ANDA 18 sections
METHIMAZOLE HUMAN PRESCRIPTION DRUG LABEL 1 53808-1044 TABLET 10 mg ORAL ANDA 18 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 54868-5135 TABLET 10 mg ORAL ANDA 18 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 54868-6071 TABLET 5 mg ORAL ANDA 18 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 60429-380 TABLET 5 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 60429-381 TABLET 10 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 60687-669 TABLET 5 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 60687-680 TABLET 10 mg ORAL ANDA 20 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 62135-205 TABLET 5 mg ORAL ANDA 12 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 62135-206 TABLET 10 mg ORAL ANDA 12 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 63629-8347 TABLET 5 mg ORAL ANDA 19 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 63629-9249 TABLET 5 mg ORAL ANDA 17 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 63629-9250 TABLET 5 mg ORAL ANDA 17 sections
Methimazole HUMAN PRESCRIPTION DRUG LABEL 1 63629-9251 TABLET 10 mg ORAL ANDA 17 sections