rosiglitazone Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peroxisome proliferator activating receptor-gamma (PPAR-gamma) agonists, thiazolidinedione derivatives 2405 122320-73-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rosiglitazone
  • rosiglitazone maleate
  • rosiglizole
  • rosiglitazone hydrochloride
  • rosiglitazone HCl
A thiazolidinedione that functions as a selective agonist for PPAR GAMMA. It improves INSULIN SENSITIVITY in adipose tissue, skeletal muscle, and the liver of patients with TYPE 2 DIABETES MELLITUS.
  • Molecular weight: 357.43
  • Formula: C18H19N3O3S
  • CLOGP: 3.02
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 71.53
  • ALOGS: -3.97
  • ROTB: 7

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
6 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.04 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.37 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 99 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.65 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.00 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
May 25, 1999 FDA SB PHARMCO

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
Cardiac failure congestive 22445.87 23.62 6565 37456 85185 46556856
Myocardial infarction 19382.97 23.62 5955 38066 91573 46550468
Coronary artery disease 8286.92 23.62 2449 41572 31303 46610738
Cerebrovascular accident 7793.10 23.62 3071 40950 97968 46544073
Acute myocardial infarction 2689.44 23.62 1041 42980 30883 46611158
Coronary arterial stent insertion 1555.26 23.62 390 43631 2463 46639578
Coronary artery bypass 1477.25 23.62 363 43658 2082 46639959
Myocardial ischaemia 1363.76 23.62 496 43525 12253 46629788
Angina unstable 1359.17 23.62 434 43587 7114 46634927
Cardiac disorder 1241.89 23.62 670 43351 43188 46598853
Transient ischaemic attack 1103.22 23.62 574 43447 34329 46607712
Cardiovascular disorder 973.03 23.62 383 43638 11804 46630237
Angina pectoris 748.63 23.62 406 43615 26369 46615672
Ischaemic cardiomyopathy 695.68 23.62 203 43818 2407 46639634
Heart injury 633.53 23.62 161 43860 1078 46640963
Acute coronary syndrome 620.71 23.62 264 43757 9940 46632101
Atrial fibrillation 557.12 23.62 582 43439 103008 46539033
Arteriosclerosis 530.34 23.62 233 43788 9500 46632541
Vascular graft 521.09 23.62 126 43895 666 46641375
Cardiomyopathy 517.75 23.62 268 43753 15805 46626236
Chest pain 502.12 23.62 718 43303 175606 46466435
Drug ineffective 470.89 23.62 48 43973 677790 45964251
Arteriosclerosis coronary artery 433.84 23.62 192 43829 7964 46634077
Stent placement 423.71 23.62 150 43871 3406 46638635
Cardio-respiratory arrest 357.07 23.62 356 43665 59513 46582528
Diarrhoea 335.38 23.62 62 43959 559540 46082501
Off label use 317.40 23.62 9 44012 379832 46262209
Sudden cardiac death 301.64 23.62 103 43918 2092 46639949
Cardiac arrest 287.84 23.62 389 43632 90010 46552031
Nausea 241.40 23.62 179 43842 687275 45954766
Fatigue 219.37 23.62 154 43867 608543 46033498
Pyrexia 216.46 23.62 35 43986 348767 46293274
Headache 197.32 23.62 103 43918 478249 46163792
Rheumatoid arthritis 195.71 23.62 7 44014 240208 46401833
Rash 193.74 23.62 49 43972 356463 46285578
Arthralgia 192.66 23.62 53 43968 364550 46277491
Congestive cardiomyopathy 177.40 23.62 93 43928 5620 46636421
Malaise 175.23 23.62 48 43973 331184 46310857
Arrhythmia 167.86 23.62 185 43836 34656 46607385
Vomiting 166.21 23.62 112 43909 452682 46189359
Hypertensive heart disease 157.68 23.62 67 43954 2511 46639530
Hypertension 152.05 23.62 468 43553 195888 46446153
Drug hypersensitivity 143.42 23.62 28 43993 243797 46398244
Pulmonary oedema 141.74 23.62 206 43815 50899 46591142
Coronary artery occlusion 139.70 23.62 90 43931 8012 46634029
Product dose omission issue 124.32 23.62 9 44012 168511 46473530
Drug intolerance 120.68 23.62 4 44017 147045 46494996
Pneumonia 117.87 23.62 109 43912 376211 46265830
Cough 109.80 23.62 40 43981 230209 46411832
Toxicity to various agents 107.59 23.62 33 43988 211733 46430308
Peripheral swelling 107.03 23.62 12 44009 158059 46483982
Supraventricular tachycardia 104.13 23.62 92 43929 13178 46628863
Nasopharyngitis 103.49 23.62 12 44009 153986 46488055
Cardiac failure 103.34 23.62 231 43790 79717 46562324
Macular oedema 102.96 23.62 58 43963 4043 46637998
Infection 101.86 23.62 6 44015 133586 46508455
Abdominal pain 101.46 23.62 45 43976 229986 46412055
Pruritus 101.39 23.62 51 43970 242301 46399740
Catheterisation cardiac 100.97 23.62 57 43964 3990 46638051
Sinus node dysfunction 97.89 23.62 57 43964 4232 46637809
Mitral valve incompetence 97.58 23.62 104 43917 18748 46623293
Ischaemia 96.25 23.62 57 43964 4367 46637674
Cerebral infarction 95.51 23.62 114 43907 23252 46618789
Cardiac pacemaker insertion 94.73 23.62 53 43968 3646 46638395
Somnolence 94.04 23.62 17 44004 156504 46485537
Drug interaction 93.95 23.62 37 43984 203057 46438984
Lacunar infarction 92.16 23.62 51 43970 3434 46638607
Implantable defibrillator insertion 91.91 23.62 28 43993 388 46641653
Back pain 91.19 23.62 42 43979 209997 46432044
Urinary tract infection 91.15 23.62 47 43974 220219 46421822
Silent myocardial infarction 90.48 23.62 28 43993 410 46641631
Cardiomegaly 89.70 23.62 96 43925 17386 46624655
Abdominal discomfort 89.57 23.62 17 44004 151148 46490893
Constipation 88.64 23.62 27 43994 174070 46467971
Cardiogenic shock 87.67 23.62 92 43929 16292 46625749
Neutropenia 87.23 23.62 15 44006 143189 46498852
Aortic stenosis 86.39 23.62 53 43968 4329 46637712
Fall 85.65 23.62 111 43910 328986 46313055
Alopecia 83.02 23.62 25 43996 162389 46479652
Pleural effusion 80.83 23.62 215 43806 82737 46559304
Hypotension 79.27 23.62 62 43959 232527 46409514
Carotid artery stenosis 78.84 23.62 53 43968 5067 46636974
Cardiac assistance device user 78.44 23.62 17 44004 49 46641992
Febrile neutropenia 76.13 23.62 3 44018 94624 46547417
Sinusitis 73.94 23.62 16 44005 129752 46512289
Pain 73.03 23.62 220 43801 476728 46165313
Cardiac valve disease 73.01 23.62 46 43975 3938 46638103
Ventricular tachycardia 71.35 23.62 84 43937 16883 46625158
Erythema 71.16 23.62 23 43998 142797 46499244
Injury 70.60 23.62 139 43882 43888 46598153
Injection site pain 70.37 23.62 9 44012 107143 46534898
Dizziness 69.45 23.62 135 43886 340279 46301762
Hypersensitivity 68.48 23.62 28 43993 150293 46491748
Pain in extremity 67.51 23.62 87 43934 258593 46383448
Condition aggravated 66.47 23.62 80 43941 244972 46397069
Insomnia 65.55 23.62 37 43984 164887 46477154
Coronary angioplasty 63.48 23.62 16 44005 103 46641938
Exposure during pregnancy 62.34 23.62 13 44008 108199 46533842
Decreased appetite 61.91 23.62 55 43966 193781 46448260
Disease progression 61.59 23.62 7 44014 91293 46550748
Hyponatraemia 60.85 23.62 11 44010 101321 46540720
Feeling abnormal 60.79 23.62 21 44000 125039 46517002
Thrombocytopenia 60.26 23.62 22 43999 126559 46515482
Atrioventricular block complete 60.08 23.62 53 43968 7574 46634467
White blood cell count decreased 59.69 23.62 16 44005 112215 46529826
Joint swelling 59.47 23.62 42 43979 166031 46476010
Confusional state 59.17 23.62 39 43982 159853 46482188
Pericardial effusion 58.14 23.62 94 43927 25449 46616592
Musculoskeletal stiffness 58.06 23.62 11 44010 97982 46544059
Oropharyngeal pain 57.54 23.62 3 44018 74165 46567876
Influenza 57.41 23.62 8 44013 89262 46552779
Platelet count decreased 55.63 23.62 13 44008 100011 46542030
Urticaria 55.26 23.62 21 44000 117871 46524170
Dehydration 54.98 23.62 42 43979 159498 46482543
Brain stem infarction 54.88 23.62 23 43998 832 46641209
Abdominal pain upper 54.36 23.62 35 43986 145270 46496771
Therapeutic product effect decreased 54.08 23.62 7 44014 82594 46559447
Intracardiac thrombus 53.53 23.62 31 43990 2277 46639764
Cardiac operation 51.93 23.62 32 43989 2634 46639407
Overdose 51.54 23.62 16 44005 101963 46540078
Psoriasis 50.65 23.62 7 44014 78597 46563444
Ischaemic stroke 50.14 23.62 70 43951 16652 46625389
Cerebrovascular disorder 49.52 23.62 32 43989 2862 46639179
Inappropriate schedule of product administration 49.29 23.62 3 44018 65010 46577031
Angioplasty 49.21 23.62 24 43997 1243 46640798
Herpes zoster 48.95 23.62 4 44017 67868 46574173
Chills 48.65 23.62 15 44006 96017 46546024
Bronchitis 47.83 23.62 20 44001 105959 46536082
Oxygen saturation decreased 47.42 23.62 5 44016 69159 46572882
Stomatitis 46.66 23.62 5 44016 68292 46573749
Diastolic dysfunction 46.19 23.62 39 43982 5253 46636788
General physical health deterioration 45.94 23.62 26 43995 115743 46526298
Coronary artery stenosis 45.87 23.62 37 43984 4676 46637365
Asthenia 45.71 23.62 146 43875 310929 46331112
Cardiopulmonary failure 44.90 23.62 33 43988 3636 46638405
Injection site erythema 44.85 23.62 8 44013 74419 46567622
Hyperlipidaemia 44.63 23.62 70 43951 18469 46623572
Arthropathy 43.32 23.62 13 44008 84687 46557354
Thalamic infarction 43.00 23.62 17 44004 528 46641513
Haemoglobin decreased 41.86 23.62 36 43985 128913 46513128
Arterial occlusive disease 41.10 23.62 35 43986 4769 46637272
Paraesthesia 40.34 23.62 31 43990 117406 46524635
Acute kidney injury 40.27 23.62 103 43918 235752 46406289
Hepatic enzyme increased 39.28 23.62 14 44007 81773 46560268
Weight decreased 39.23 23.62 88 43933 210761 46431280
Hypokalaemia 39.09 23.62 17 44004 88007 46554034
Pulmonary hypertension 38.85 23.62 97 43924 35896 46606145
Cardiac death 38.49 23.62 16 44005 567 46641474
Pancytopenia 38.46 23.62 16 44005 85042 46556999
Heart rate irregular 37.74 23.62 65 43956 18526 46623515
Memory impairment 37.55 23.62 13 44008 77324 46564717
Arthritis 37.53 23.62 13 44008 77303 46564738
Ventricular fibrillation 37.30 23.62 50 43971 11446 46630595
Blindness 37.20 23.62 62 43959 17207 46624834
Flushing 36.72 23.62 8 44013 64606 46577435
Peripheral vascular disorder 36.40 23.62 36 43985 5941 46636100
Oedema 36.17 23.62 142 43879 66929 46575112
Musculoskeletal pain 35.43 23.62 11 44010 70117 46571924
Migraine 35.35 23.62 11 44010 70015 46572026
Lower respiratory tract infection 35.27 23.62 5 44016 55084 46586957
Tricuspid valve incompetence 34.71 23.62 53 43968 13664 46628377
Gastrointestinal disorder 34.63 23.62 7 44014 59569 46582472
Carotid artery disease 34.62 23.62 21 44000 1680 46640361
Cor pulmonale 34.52 23.62 22 43999 1921 46640120
Rhinorrhoea 33.84 23.62 3 44018 47662 46594379
Intentional overdose 33.15 23.62 10 44011 64934 46577107
Contusion 32.80 23.62 21 44000 87466 46554575
Blood pressure increased 32.57 23.62 43 43978 126623 46515418
Neuropathy peripheral 32.50 23.62 23 43998 90870 46551171
Myalgia 32.46 23.62 41 43980 123047 46518994
Wrong technique in product usage process 32.46 23.62 6 44015 54416 46587625
Interstitial lung disease 32.07 23.62 6 44015 53943 46588098
Diabetes mellitus inadequate control 31.95 23.62 50 43971 13164 46628877
Atrial flutter 31.55 23.62 41 43980 9107 46632934
Agitation 31.20 23.62 7 44014 55408 46586633
Intentional product misuse 30.83 23.62 4 44017 47124 46594917
Haemorrhage 30.76 23.62 7 44014 54862 46587179
Asthma 30.38 23.62 25 43996 91517 46550524
Abortion spontaneous 30.32 23.62 3 44018 43643 46598398
Upper respiratory tract infection 30.31 23.62 11 44010 63545 46578496
Neutrophil count decreased 30.12 23.62 3 44018 43423 46598618
Tremor 30.00 23.62 39 43982 115600 46526441
Anaphylactic reaction 29.33 23.62 7 44014 53105 46588936
Leukopenia 29.10 23.62 14 44007 68329 46573712
Atrioventricular block 29.10 23.62 34 43987 6777 46635264
Multiple sclerosis relapse 28.99 23.62 3 44018 42122 46599919
Dysphagia 28.38 23.62 19 44002 77293 46564748
Alanine aminotransferase increased 28.32 23.62 25 43996 88426 46553615
Renal failure 27.84 23.62 193 43828 113401 46528640
Dyspepsia 27.70 23.62 15 44006 68457 46573584
Seizure 27.53 23.62 46 43975 123008 46519033
Injection site swelling 27.42 23.62 3 44018 40324 46601717
Therapeutic response decreased 27.42 23.62 4 44017 43141 46598900
Influenza like illness 27.39 23.62 10 44011 57560 46584481
Productive cough 27.39 23.62 7 44014 50708 46591333
Mitral valve disease 27.30 23.62 20 44001 2192 46639849
Nasal congestion 27.25 23.62 6 44015 48107 46593934
Injection site reaction 27.03 23.62 6 44015 47843 46594198
Bone pain 26.25 23.62 6 44015 46884 46595157
Epistaxis 26.14 23.62 14 44007 64291 46577750
Dry skin 25.61 23.62 4 44017 41012 46601029
Dry mouth 25.36 23.62 10 44011 54916 46587125
Suicidal ideation 24.85 23.62 11 44010 56371 46585670
Delirium 24.74 23.62 3 44018 37225 46604816
Cognitive disorder 24.44 23.62 3 44018 36880 46605161
Gait disturbance 24.34 23.62 64 43957 145199 46496842
Multiple fractures 24.13 23.62 28 43993 5539 46636502
Muscle spasms 24.02 23.62 50 43971 123063 46518978
Gastrooesophageal reflux disease 23.81 23.62 21 44000 74323 46567718

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
Myocardial infarction 27543.87 25.61 9959 51268 115666 29775585
Cardiac failure congestive 20478.07 25.61 7257 53970 77150 29814101
Coronary artery disease 12821.55 25.61 4500 56727 45212 29846039
Cerebrovascular accident 7845.16 25.61 3664 57563 79813 29811438
Acute myocardial infarction 3457.87 25.61 1823 59404 51116 29840135
Coronary artery bypass 3342.95 25.61 950 60277 4212 29887039
Coronary arterial stent insertion 2363.35 25.61 693 60534 3501 29887750
Cardiac disorder 1789.57 25.61 1076 60151 38817 29852434
Myocardial ischaemia 1769.07 25.61 811 60416 16506 29874745
Ischaemic cardiomyopathy 1560.58 25.61 558 60669 5739 29885512
Angina unstable 1514.76 25.61 657 60570 11653 29879598
Cardiovascular disorder 1427.93 25.61 609 60618 10343 29880908
Transient ischaemic attack 1024.40 25.61 639 60588 24561 29866690
Vascular graft 821.59 25.61 241 60986 1214 29890037
Angina pectoris 790.58 25.61 578 60649 28940 29862311
Stent placement 766.56 25.61 305 60922 4291 29886960
Arteriosclerosis 743.38 25.61 387 60840 10446 29880805
Heart injury 737.14 25.61 222 61005 1244 29890007
Arteriosclerosis coronary artery 729.18 25.61 386 60841 10790 29880461
Cardiomyopathy 712.68 25.61 422 60805 14721 29876530
Acute coronary syndrome 704.28 25.61 403 60824 13170 29878081
Atrial fibrillation 585.71 25.61 898 60329 107226 29784025
Drug ineffective 472.91 25.61 68 61159 340319 29550932
Off label use 447.28 25.61 14 61213 249276 29641975
Pyrexia 445.43 25.61 44 61183 294445 29596806
Diarrhoea 415.49 25.61 89 61138 334014 29557237
Sudden cardiac death 370.85 25.61 172 61055 3580 29887671
Cardiac arrest 361.71 25.61 666 60561 92184 29799067
Chest pain 324.24 25.61 731 60496 116896 29774355
Cardio-respiratory arrest 322.32 25.61 485 60742 56821 29834430
Pneumonia 320.67 25.61 142 61085 334164 29557087
Toxicity to various agents 291.13 25.61 18 61209 177165 29714086
Coronary artery occlusion 286.00 25.61 213 61014 10944 29880307
Nausea 244.86 25.61 153 61074 296804 29594447
Rash 244.39 25.61 48 61179 191841 29699410
Vomiting 234.14 25.61 79 61148 219739 29671512
Fatigue 227.05 25.61 194 61033 320479 29570772
Macular oedema 220.32 25.61 109 61118 2629 29888622
Implantable defibrillator insertion 220.13 25.61 75 61152 657 29890594
Arrhythmia 212.91 25.61 299 60928 32870 29858381
Neutropenia 202.47 25.61 16 61211 128524 29762727
Catheterisation cardiac 198.09 25.61 95 61132 2136 29889115
Hypotension 195.29 25.61 83 61144 200482 29690769
Drug interaction 188.91 25.61 86 61141 199482 29691769
Febrile neutropenia 184.01 25.61 8 61219 106685 29784566
Acute kidney injury 177.88 25.61 179 61048 273663 29617588
Congestive cardiomyopathy 177.64 25.61 130 61097 6497 29884754
Silent myocardial infarction 173.38 25.61 54 61173 344 29890907
Malaise 172.48 25.61 63 61164 166899 29724352
Decreased appetite 171.87 25.61 47 61180 149863 29741388
Platelet count decreased 164.91 25.61 14 61213 106115 29785136
Thrombocytopenia 160.82 25.61 41 61186 137003 29754248
Fall 159.08 25.61 87 61140 181785 29709466
Pruritus 155.83 25.61 27 61200 118177 29773074
Arthralgia 151.14 25.61 45 61182 135746 29755505
Confusional state 147.69 25.61 46 61181 134788 29756463
Ischaemia 147.46 25.61 100 61127 4421 29886830
Headache 144.38 25.61 98 61129 182208 29709043
White blood cell count decreased 139.29 25.61 8 61219 83939 29807312
Sepsis 138.55 25.61 63 61164 146332 29744919
Constipation 133.93 25.61 33 61194 112873 29778378
Abdominal pain 130.52 25.61 57 61170 135597 29755654
Lacunar infarction 127.94 25.61 80 61147 3075 29888176
Pancytopenia 127.36 25.61 13 61214 85039 29806212
Cardiac pacemaker insertion 125.06 25.61 73 61154 2472 29888779
Completed suicide 124.15 25.61 26 61201 99466 29791785
Cardiac assistance device user 123.72 25.61 25 61202 7 29891244
Injury 123.51 25.61 185 61042 21546 29869705
Hypertensive heart disease 123.12 25.61 71 61156 2349 29888902
Disease progression 122.79 25.61 11 61216 79863 29811388
Cardiac operation 119.62 25.61 71 61156 2481 29888770
Cough 118.96 25.61 54 61173 125588 29765663
Carotid artery stenosis 117.33 25.61 88 61139 4566 29886685
Malignant neoplasm progression 116.60 25.61 8 61219 72279 29818972
Dehydration 115.56 25.61 54 61173 123485 29767766
General physical health deterioration 111.38 25.61 33 61194 99911 29791340
Somnolence 109.57 25.61 31 61196 96732 29794519
Dizziness 109.43 25.61 143 61084 194766 29696485
Anaemia 109.37 25.61 160 61067 207832 29683419
Erythema 108.14 25.61 15 61212 77436 29813815
Hypertension 107.65 25.61 512 60715 120842 29770409
Aortic stenosis 107.56 25.61 79 61148 3969 29887282
Peripheral swelling 107.20 25.61 4 61223 61070 29830181
Haemoglobin decreased 106.51 25.61 50 61177 114048 29777203
Sinus node dysfunction 104.38 25.61 76 61151 3767 29887484
Interstitial lung disease 102.15 25.61 5 61222 60192 29831059
Back pain 102.03 25.61 41 61186 102555 29788696
Overdose 101.26 25.61 24 61203 84313 29806938
Infection 100.32 25.61 19 61208 78055 29813196
Asthenia 96.37 25.61 192 61035 221098 29670153
Insomnia 93.30 25.61 37 61190 93299 29797952
Plasma cell myeloma 92.14 25.61 4 61223 53458 29837793
Chills 90.02 25.61 19 61208 72319 29818932
Peripheral vascular disorder 89.88 25.61 79 61148 5140 29886111
Weight decreased 87.48 25.61 108 61119 150813 29740438
Urinary tract infection 84.49 25.61 23 61204 73636 29817615
Tremor 83.73 25.61 25 61202 75338 29815913
Arterial occlusive disease 83.65 25.61 68 61159 3972 29887279
Hyponatraemia 80.90 25.61 19 61208 67183 29824068
Drug hypersensitivity 79.33 25.61 21 61206 68498 29822753
Gastrointestinal haemorrhage 78.72 25.61 36 61191 83410 29807841
Condition aggravated 78.48 25.61 100 61127 137766 29753485
Leukopenia 78.09 25.61 11 61216 56148 29835103
Hallucination 77.46 25.61 6 61221 49053 29842198
Hospitalisation 77.43 25.61 3 61224 44316 29846935
Hyperlipidaemia 77.02 25.61 117 61110 13790 29877461
Neuropathy peripheral 75.39 25.61 25 61202 70450 29820801
Pulmonary oedema 75.19 25.61 229 60998 43746 29847505
C-reactive protein increased 72.52 25.61 4 61223 43469 29847782
Supraventricular tachycardia 72.49 25.61 97 61130 10175 29881076
Epistaxis 72.22 25.61 11 61216 52970 29838281
Nasopharyngitis 72.11 25.61 16 61211 58833 29832418
Coronary angioplasty 72.10 25.61 28 61199 367 29890884
Agitation 71.97 25.61 12 61215 54061 29837190
Ventricular tachycardia 71.92 25.61 154 61073 23708 29867543
Psoriasis 70.63 25.61 4 61223 42502 29848749
Cardiogenic shock 70.58 25.61 125 61102 16736 29874515
Blood pressure increased 69.46 25.61 30 61197 71898 29819353
Cerebrovascular disorder 69.24 25.61 46 61181 1964 29889287
Myalgia 67.88 25.61 36 61191 76631 29814620
Atrial flutter 67.84 25.61 112 61115 14169 29877082
Hypokalaemia 67.11 25.61 11 61216 50181 29841070
Hepatic function abnormal 66.59 25.61 5 61222 41940 29849311
Cerebral infarction 65.89 25.61 158 61069 26215 29865036
Mitral valve incompetence 65.86 25.61 106 61121 13128 29878123
Intentional overdose 65.69 25.61 5 61222 41476 29849775
Intracardiac thrombus 65.55 25.61 48 61179 2400 29888851
Rheumatoid arthritis 65.14 25.61 5 61222 41192 29850059
Cardiomegaly 63.89 25.61 110 61117 14399 29876852
Septic shock 63.89 25.61 25 61202 63582 29827669
Urticaria 62.70 25.61 17 61210 54589 29836662
Angioplasty 62.57 25.61 34 61193 1000 29890251
Ventricular fibrillation 61.78 25.61 111 61116 15027 29876224
Hypersensitivity 61.70 25.61 17 61210 54011 29837240
Renal impairment 61.66 25.61 49 61178 84135 29807116
Oxygen saturation decreased 61.60 25.61 8 61219 43432 29847819
Influenza 61.52 25.61 8 61219 43390 29847861
Blood pressure decreased 61.43 25.61 11 61216 47064 29844187
Atrioventricular block 61.20 25.61 75 61152 7207 29884044
Feeling abnormal 60.93 25.61 20 61207 56736 29834515
High density lipoprotein decreased 60.16 25.61 51 61176 3159 29888092
White blood cell count increased 59.52 25.61 6 61221 39667 29851584
Suicide attempt 59.33 25.61 4 61223 36693 29854558
Alanine aminotransferase increased 58.58 25.61 40 61187 74236 29817015
Intentional product misuse 58.42 25.61 3 61224 34664 29856587
Muscle spasms 58.05 25.61 30 61197 64808 29826443
Electrocardiogram QT prolonged 57.66 25.61 4 61223 35831 29855420
Pain in extremity 56.64 25.61 86 61141 110135 29781116
Seizure 56.45 25.61 71 61156 98404 29792847
Rhabdomyolysis 56.07 25.61 30 61197 63550 29827701
Cardiac valve disease 55.57 25.61 47 61180 2902 29888349
Coronary artery stenosis 55.54 25.61 80 61147 8990 29882261
Atrioventricular block complete 55.20 25.61 77 61150 8400 29882851
Blindness 55.09 25.61 94 61133 12215 29879036
Tachycardia 52.65 25.61 44 61183 73695 29817556
Dyspnoea 52.55 25.61 433 60794 332862 29558389
Hypoxic-ischaemic encephalopathy 52.47 25.61 56 61171 4631 29886620
Basal ganglia infarction 52.37 25.61 17 61210 126 29891125
Paraesthesia 51.90 25.61 23 61204 54304 29836947
Pneumonia aspiration 51.13 25.61 8 61219 37772 29853479
Dysphagia 51.11 25.61 26 61201 56672 29834579
Mucosal inflammation 50.26 25.61 3 61224 30491 29860760
Blood creatinine increased 50.19 25.61 68 61159 91307 29799944
Pleural effusion 50.04 25.61 290 60937 73776 29817475
Cor pulmonale 49.30 25.61 26 61201 719 29890532
Asthma 48.19 25.61 8 61219 36166 29855085
Angiogram 47.83 25.61 15 61212 98 29891153
Abdominal discomfort 47.65 25.61 20 61207 48771 29842480
Hyperkalaemia 47.60 25.61 39 61188 65971 29825280
Ischaemic stroke 46.71 25.61 103 61124 16172 29875079
Delirium 45.99 25.61 13 61214 40618 29850633
Suicidal ideation 45.92 25.61 9 61218 36105 29855146
Colitis 45.36 25.61 5 61222 30815 29860436
Injection site pain 44.40 25.61 5 61222 30305 29860946
Diabetic retinopathy 43.91 25.61 33 61194 1717 29889534
Abdominal pain upper 43.82 25.61 38 61189 62513 29828738
Cardiac failure 43.60 25.61 306 60921 83112 29808139
Musculoskeletal stiffness 43.45 25.61 10 61217 35871 29855380
Bone marrow failure 43.41 25.61 5 61222 29780 29861471
Haemorrhage 43.25 25.61 20 61207 46059 29845192
Angioedema 42.82 25.61 9 61218 34375 29856876
Lethargy 42.28 25.61 14 61213 39505 29851746
Loss of consciousness 41.66 25.61 61 61166 79314 29811937
Thalamic infarction 41.05 25.61 22 61205 629 29890622
Encephalopathy 41.00 25.61 8 61219 32197 29859054
Hyperhidrosis 40.96 25.61 46 61181 67044 29824207
Muscular weakness 40.68 25.61 42 61185 63603 29827648
Respiratory distress 40.31 25.61 9 61218 32963 29858288
Urinary retention 40.21 25.61 9 61218 32908 29858343
Joint swelling 40.15 25.61 23 61204 46923 29844328
International normalised ratio increased 39.97 25.61 24 61203 47715 29843536
Pneumonitis 39.05 25.61 5 61222 27449 29863802
Cardiac death 38.90 25.61 25 61202 1008 29890243
Oropharyngeal pain 38.63 25.61 6 61221 28490 29862761
Therapeutic response decreased 38.36 25.61 3 61224 24346 29866905
Flushing 38.24 25.61 7 61220 29485 29861766
Aspartate aminotransferase increased 38.16 25.61 44 61183 63378 29827873
Brain stem infarction 38.15 25.61 27 61200 1279 29889972
Carotid artery disease 38.04 25.61 24 61203 937 29890314
Anaphylactic reaction 37.69 25.61 6 61221 27976 29863275
Haemoptysis 36.96 25.61 9 61218 31069 29860182
Depressed level of consciousness 36.79 25.61 16 61211 38206 29853045
Therapy non-responder 36.08 25.61 8 61219 29445 29861806
Cerebellar infarction 35.93 25.61 30 61197 1819 29889432
Hepatocellular injury 35.37 25.61 5 61222 25466 29865785
Multiple organ dysfunction syndrome 35.10 25.61 47 61180 63440 29827811
Restlessness 35.01 25.61 3 61224 22596 29868655
Wheezing 34.82 25.61 10 61217 30928 29860323
Aggression 34.66 25.61 16 61211 36891 29854360
Cholestasis 34.41 25.61 5 61222 24945 29866306
Incorrect dose administered 34.29 25.61 11 61216 31675 29859576
Aortic valve replacement 34.10 25.61 20 61207 683 29890568
Cardiopulmonary failure 34.03 25.61 41 61186 3870 29887381
Metabolic acidosis 34.02 25.61 17 61210 37444 29853807
Disorientation 33.84 25.61 11 61216 31407 29859844
Gastrointestinal disorder 33.76 25.61 8 61219 28129 29863122
Hypoxia 33.60 25.61 29 61198 47825 29843426
Adverse drug reaction 33.45 25.61 4 61223 23141 29868110
Influenza like illness 33.36 25.61 6 61221 25599 29865652
Cellulitis 33.28 25.61 28 61199 46756 29844495
Productive cough 33.13 25.61 10 61217 29943 29861308
Death 33.05 25.61 523 60704 356760 29534491
Rash maculo-papular 33.02 25.61 6 61221 25412 29865839
Haematuria 32.93 25.61 26 61201 44808 29846443
Leukocytosis 32.91 25.61 3 61224 21499 29869752
Peritonitis 32.67 25.61 3 61224 21372 29869879
Brain stem stroke 32.55 25.61 12 61215 135 29891116
Rash erythematous 32.15 25.61 4 61223 22448 29868803
Melaena 32.15 25.61 13 61214 32424 29858827
Left ventricular dysfunction 32.03 25.61 61 61166 8630 29882621
Syncope 31.67 25.61 80 61147 84823 29806428
Rectal haemorrhage 31.51 25.61 16 61211 34923 29856328
Lower respiratory tract infection 31.26 25.61 8 61219 26706 29864545
Memory impairment 30.68 25.61 19 61208 37155 29854096
Sinusitis 30.48 25.61 15 61212 33330 29857921
Hypertensive cardiomyopathy 30.45 25.61 12 61215 164 29891087
Haematochezia 30.37 25.61 16 61211 34206 29857045
Therapeutic product effect decreased 29.90 25.61 11 61216 29065 29862186
Transaminases increased 29.49 25.61 6 61221 23451 29867800
Deep vein thrombosis 29.35 25.61 49 61178 60452 29830799
Disseminated intravascular coagulation 29.31 25.61 5 61222 22166 29869085
Eosinophilia 29.29 25.61 5 61222 22155 29869096
Rhinorrhoea 28.99 25.61 4 61223 20750 29870501
Dyskinesia 28.70 25.61 5 61222 21829 29869422
Bronchitis 28.34 25.61 23 61204 39102 29852149
Heart rate irregular 28.02 25.61 71 61156 12188 29879063
Blood creatine phosphokinase increased 27.94 25.61 29 61198 43819 29847432
Swelling face 27.56 25.61 5 61222 21199 29870052
Acute respiratory distress syndrome 27.52 25.61 7 61220 23465 29867786
Altered state of consciousness 27.45 25.61 4 61223 19915 29871336
Osteonecrosis of jaw 27.45 25.61 3 61224 18615 29872636
Ascites 27.44 25.61 20 61207 35901 29855350
Skin lesion 27.21 25.61 3 61224 18491 29872760
Contusion 27.21 25.61 15 61212 31265 29859986
Disturbance in attention 27.13 25.61 6 61221 22123 29869128
Coronary artery insufficiency 27.08 25.61 10 61217 113 29891138
Staphylococcal infection 27.02 25.61 14 61213 30210 29861041
Inflammation 26.94 25.61 6 61221 22020 29869231
Nephrolithiasis 26.17 25.61 9 61218 24801 29866450
Gait disturbance 25.96 25.61 73 61154 74704 29816547
Aortic valve stenosis 25.87 25.61 24 61203 1675 29889576
Abnormal behaviour 25.83 25.61 10 61217 25613 29865638
Hypocalcaemia 25.79 25.61 6 61221 21370 29869881

Pharmacologic Action:

SourceCodeDescription
ATC A10BD03 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD04 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BG02 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Thiazolidinediones
FDA CS M0199114 PPAR gamma
FDA CS M0447306 Thiazolidinediones
FDA MoA N0000175374 Peroxisome Proliferator-activated Receptor Activity
FDA EPC N0000180186 Peroxisome Proliferator Receptor gamma Agonist
FDA EPC N0000180190 Thiazolidinedione
MeSH PA D007004 Hypoglycemic Agents
CHEBI has role CHEBI:50864 glitazone drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Treatment Refractory Type 2 Diabetes Mellitus indication
Alcoholism contraindication 7200002
Weight gain finding contraindication 8943002
Asthenia contraindication 13791008
Pulmonary edema contraindication 19242006 DOID:11396
Myocardial infarction contraindication 22298006 DOID:5844
Acute vomiting contraindication 23971007
Alcohol intoxication contraindication 25702006
Shock contraindication 27942005
Dehydration contraindication 34095006
Macular retinal edema contraindication 37231002 DOID:4449
Infectious disease contraindication 40733004
Body fluid retention contraindication 43498006
Chronic heart failure contraindication 48447003
Hepatic porphyria contraindication 55056006 DOID:3133
Ketoacidosis contraindication 56051008
Metabolic acidosis contraindication 59455009
Hemolytic anemia contraindication 61261009 DOID:583
Glucose-6-phosphate dehydrogenase deficiency anemia contraindication 62403005
Osteoporosis contraindication 64859006 DOID:11476
Hypopituitarism contraindication 74728003 DOID:9406
Cardiogenic shock contraindication 89138009
Kidney disease contraindication 90708001 DOID:557
Lactic acidosis contraindication 91273001 DOID:3650
Fracture of bone contraindication 125605004
Autonomic dysreflexia contraindication 129618003
Liver function tests abnormal contraindication 166603001
Cobalamin deficiency contraindication 190634004
Angina pectoris contraindication 194828000
Decompensated cardiac failure contraindication 195111005
Cerebrovascular accident contraindication 230690007
Disease of liver contraindication 235856003 DOID:409
Drug-induced hepatitis contraindication 235876009
Hypoglycemic disorder contraindication 237630007
Sepsis syndrome contraindication 238150007
Osteopenia contraindication 312894000
Primary adrenocortical insufficiency contraindication 373662000
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Fever contraindication 386661006
Surgical procedure contraindication 387713003
Severe diarrhea contraindication 409587002
Breastfeeding (mother) contraindication 413712001
Disorder of coronary artery contraindication 414024009
Myocardial ischemia contraindication 414795007 DOID:3393
Traumatic injury contraindication 417746004
Fever greater than 100.4 Fahrenheit contraindication 426000000
Radiography with IV Iodinated Contrast Agent contraindication
Severe Hypoxemia contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.5 acidic
pKa2 5.84 Basic

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
Peroxisome proliferator-activated receptor gamma Nuclear hormone receptor AGONIST EC50 7.04 WOMBAT-PK CHEMBL
Free fatty acid receptor 1 GPCR AGONIST EC50 5.60 IUPHAR
Carbonic anhydrase 2 Enzyme IC50 5.39 DRUG MATRIX
Thromboxane-A synthase Enzyme IC50 5.45 DRUG MATRIX
Amine oxidase [flavin-containing] B Enzyme Ki 5.38 CHEMBL
Amine oxidase [flavin-containing] A Enzyme Ki 4.56 CHEMBL
Peroxisome proliferator-activated receptor delta Nuclear hormone receptor EC50 5.44 CHEMBL
Peroxisome proliferator-activated receptor alpha Nuclear hormone receptor EC50 7.41 CHEMBL
Retinoic acid receptor gamma Nuclear hormone receptor Ki 5 CHEMBL
Short transient receptor potential channel 5 Ion channel ACTIVATOR EC50 4.51 IUPHAR
Bile salt export pump Transporter IC50 5.19 CHEMBL
Type-1A angiotensin II receptor GPCR Ki 9.64 CHEMBL
Amine oxidase [flavin-containing] B Enzyme Ki 5.24 CHEMBL
Amine oxidase [flavin-containing] A Enzyme Ki 4.49 CHEMBL
Bile salt export pump Unclassified IC50 4.40 CHEMBL
Peroxisome proliferator-activated receptor gamma Transcription factor EC50 7.52 CHEMBL

External reference:

IDSource
4021162 VUID
N0000148613 NUI
D00596 KEGG_DRUG
302543-62-0 SECONDARY_CAS_RN
4021162 VANDF
4021163 VANDF
C0289313 UMLSCUI
CHEBI:50122 CHEBI
BRL PDB_CHEM_ID
CHEMBL121 ChEMBL_ID
CHEMBL843 ChEMBL_ID
D000077154 MESH_DESCRIPTOR_UI
1056 IUPHAR_LIGAND_ID
7662 INN_ID
DB00412 DRUGBANK_ID
05V02F2KDG UNII
77999 PUBCHEM_CID
253198 RXNORM
8221 MMSL
d04434 MMSL
007789 NDDF
007790 NDDF
116096001 SNOMEDCT_US
326053005 SNOMEDCT_US
395869000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
AVANDIA2MG HUMAN PRESCRIPTION DRUG LABEL 1 0173-0861 TABLET, FILM COATED 2 mg ORAL NDA 29 sections
AVANDIA4MG HUMAN PRESCRIPTION DRUG LABEL 1 0173-0863 TABLET, FILM COATED 4 mg ORAL NDA 29 sections
Avandia HUMAN PRESCRIPTION DRUG LABEL 1 54868-4198 TABLET, FILM COATED 4 mg ORAL NDA 19 sections
Avandia HUMAN PRESCRIPTION DRUG LABEL 1 54868-4221 TABLET, FILM COATED 8 mg ORAL NDA 19 sections
AVANDAMET HUMAN PRESCRIPTION DRUG LABEL 2 54868-4965 TABLET, FILM COATED 2 mg ORAL NDA 30 sections
AVANDAMET HUMAN PRESCRIPTION DRUG LABEL 2 54868-5157 TABLET, FILM COATED 4 mg ORAL NDA 30 sections
Avandia HUMAN PRESCRIPTION DRUG LABEL 1 54868-5249 TABLET, FILM COATED 2 mg ORAL NDA 19 sections
AVANDAMET HUMAN PRESCRIPTION DRUG LABEL 2 54868-5262 TABLET, FILM COATED 4 mg ORAL NDA 30 sections
AVANDAMET HUMAN PRESCRIPTION DRUG LABEL 2 54868-5376 TABLET, FILM COATED 2 mg ORAL NDA 30 sections