pioglitazone ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peroxisome proliferator activating receptor-gamma (PPAR-gamma) agonists, thiazolidinedione derivatives 2179 111025-46-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pioglitazone
  • glustin
  • sepioglin
  • pioglitazone hydrochloride
  • pioglitazone HCl
Pioglitazone is a thiazolidinedione that depends on the presence of insulin for its mechanism of action. Pioglitazone decreases insulin resistance in the periphery and in the liver resulting in increased insulin-dependent glucose disposal and decreased hepatic glucose output. Pioglitazone is not an insulin secretagogue. Pioglitazone is an agonist for peroxisome proliferator-activated receptor-gamma (PPAR-gamma). PPAR receptors are found in tissues important for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma nuclear receptors modulates the transcription of a number of insulin responsive genes involved in the control of glucose and lipid metabolism.
  • Molecular weight: 356.44
  • Formula: C19H20N2O3S
  • CLOGP: 3.53
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 68.29
  • ALOGS: -4.91
  • ROTB: 7

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
30 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.80 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 83 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
July 15, 1999 FDA TAKEDA PHARMS USA

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
Bladder cancer 581.36 11.97 157 21744 3175 50580048
Hypoglycaemia 414.90 11.97 269 21632 53312 50529911
Blood glucose increased 392.06 11.97 290 21611 71034 50512189
Cardiac failure congestive 173.82 11.97 198 21703 84184 50499039
Diabetes mellitus inadequate control 132.03 11.97 78 21823 13067 50570156
Blood glucose decreased 120.42 11.97 83 21818 18128 50565095
Glycosylated haemoglobin increased 119.98 11.97 68 21833 10538 50572685
Oedema peripheral 106.03 11.97 220 21681 157741 50425482
Diabetic ketoacidosis 92.02 11.97 70 21831 17802 50565421
Diabetic metabolic decompensation 78.43 11.97 28 21873 1452 50581771
Cardiac failure 72.26 11.97 123 21778 75917 50507306
Lactic acidosis 66.43 11.97 77 21824 33278 50549945
Pancreatitis 64.96 11.97 86 21815 42528 50540695
Drug ineffective 60.40 11.97 170 21731 819163 49764060
Weight increased 58.38 11.97 206 21695 201685 50381538
Bladder neoplasm 56.69 11.97 17 21884 505 50582718
Myocardial infarction 56.15 11.97 121 21780 88906 50494317
Oedema 55.74 11.97 105 21796 70076 50513147
Bladder transitional cell carcinoma 53.49 11.97 16 21885 471 50582752
Off label use 49.34 11.97 81 21820 474345 50108878
Systemic lupus erythematosus 48.91 11.97 3 21898 140619 50442604
Drug intolerance 48.74 11.97 17 21884 219087 50364136
Hyperglycaemia 48.73 11.97 69 21832 36336 50546887
Macular oedema 48.39 11.97 26 21875 3628 50579595
Pancreatitis acute 42.51 11.97 52 21849 23760 50559463
Maternal exposure during pregnancy 41.88 11.97 9 21892 159769 50423454
Infusion related reaction 41.60 11.97 11 21890 169546 50413677
Weight decreased 40.39 11.97 196 21705 221049 50362174
Pancreatic carcinoma 40.31 11.97 28 21873 6186 50577037
Coronary artery disease 39.28 11.97 56 21845 29670 50553553
Glossodynia 38.63 11.97 3 21898 115566 50467657
Acute kidney injury 38.07 11.97 197 21704 227861 50355362
Treatment failure 37.64 11.97 7 21894 137630 50445593
Diabetes mellitus 36.02 11.97 71 21830 48962 50534261
Contraindicated product administered 35.90 11.97 10 21891 148948 50434275
Rheumatoid arthritis 35.35 11.97 22 21879 202528 50380695
Diabetic retinopathy 32.88 11.97 17 21884 2193 50581030
Ureteric cancer 30.93 11.97 7 21894 65 50583158
Product use issue 29.32 11.97 14 21887 149461 50433762
Hypoglycaemic coma 29.22 11.97 16 21885 2317 50580906
Product complaint 28.96 11.97 30 21871 11436 50571787
Lower respiratory tract infection 27.90 11.97 4 21897 95197 50488026
Arthropathy 27.75 11.97 17 21884 157889 50425334
Wound 27.63 11.97 6 21895 105788 50477435
Alopecia 27.15 11.97 40 21861 245007 50338216
Bladder trabeculation 26.68 11.97 6 21895 54 50583169
Bladder adenocarcinoma stage unspecified 26.56 11.97 5 21896 16 50583207
Chest pain 26.24 11.97 148 21753 176734 50406489
Blood glucose fluctuation 25.30 11.97 18 21883 4128 50579095
Joint swelling 24.39 11.97 43 21858 245243 50337980
Biopsy skin abnormal 23.70 11.97 6 21895 93 50583130
Renal failure 23.55 11.97 100 21801 106533 50476690
Angina unstable 23.47 11.97 21 21880 6685 50576538
Therapeutic product effect decreased 23.41 11.97 15 21886 136035 50447188
Discomfort 23.08 11.97 9 21892 108371 50474852
Asthenia 22.63 11.97 224 21677 318818 50264405
Pancreatitis chronic 21.83 11.97 13 21888 2207 50581016
Myalgia 21.83 11.97 109 21792 124210 50459013
Portal fibrosis 21.77 11.97 7 21894 263 50582960
Cholelithiasis 20.99 11.97 49 21852 37924 50545299
Diabetic neuropathy 20.57 11.97 15 21886 3576 50579647
Therapeutic product effect incomplete 20.50 11.97 7 21894 91508 50491715
Fall 20.38 11.97 228 21673 334704 50248519
Fasting 20.00 11.97 4 21897 19 50583204
Exposure during pregnancy 19.94 11.97 14 21887 121001 50462222
Radius fracture 19.74 11.97 14 21887 3195 50580028
Ketoacidosis 19.48 11.97 15 21886 3880 50579343
Fluid retention 19.42 11.97 57 21844 50592 50532631
Blood triglycerides increased 19.06 11.97 24 21877 11288 50571935
Dehydration 19.04 11.97 122 21779 152327 50430896
Haematuria 18.70 11.97 37 21864 25576 50557647
Nasopharyngitis 18.12 11.97 35 21866 192892 50390331
General physical health deterioration 18.07 11.97 21 21880 142413 50440810
Abdominal discomfort 17.71 11.97 47 21854 231594 50351629
Tibia fracture 17.65 11.97 15 21886 4460 50578763
Pancreatic carcinoma metastatic 17.62 11.97 11 21890 2031 50581192
Dyspnoea 17.46 11.97 333 21568 547275 50035948
Incorrect dose administered 17.16 11.97 53 21848 48361 50534862
High density lipoprotein decreased 16.83 11.97 10 21891 1690 50581533
Nicotinic acid deficiency 16.59 11.97 4 21897 50 50583173
Acute myocardial infarction 16.42 11.97 38 21863 29235 50553988
Transitional cell carcinoma 16.30 11.97 7 21894 595 50582628
Musculoskeletal stiffness 16.23 11.97 19 21882 128462 50454761
Varicose vein ruptured 16.18 11.97 4 21897 56 50583167
Pericarditis 16.00 11.97 7 21894 78682 50504541
Arteriosclerosis coronary artery 15.82 11.97 18 21883 7618 50575605
IIIrd nerve paralysis 15.81 11.97 7 21894 640 50582583
Decreased appetite 15.16 11.97 143 21758 200780 50382443
Retinal aneurysm 15.11 11.97 5 21896 206 50583017
Infection 14.87 11.97 33 21868 172921 50410302
Inflammatory bowel disease 14.50 11.97 12 21889 3438 50579785
Contraindicated product prescribed 14.42 11.97 7 21894 790 50582433
Ankle fracture 14.35 11.97 25 21876 15697 50567526
Blood glucose abnormal 14.29 11.97 16 21885 6656 50576567
Rash 14.27 11.97 121 21780 437350 50145873
Rhabdomyolysis 14.09 11.97 43 21858 38984 50544239
Shock 14.08 11.97 29 21872 20621 50562602
Vomiting 13.92 11.97 278 21623 460480 50122743
Ketosis 13.89 11.97 6 21895 517 50582706
Renal impairment 13.74 11.97 67 21834 75594 50507629
Adult failure to thrive 13.70 11.97 4 21897 108 50583115
Nausea 13.58 11.97 400 21501 704998 49878225
Visual acuity reduced 13.40 11.97 28 21873 20111 50563112
Upper airway obstruction 13.37 11.97 6 21895 567 50582656
Arteriosclerosis 13.33 11.97 18 21883 9059 50574164
Postmortem blood drug level increased 13.28 11.97 6 21895 576 50582647
Unresponsive to stimuli 13.25 11.97 36 21865 30573 50552650
Medication error 13.24 11.97 40 21861 36064 50547159
Acute coronary syndrome 12.88 11.97 18 21883 9356 50573867
Left ventricular dysfunction 12.72 11.97 19 21882 10487 50572736
Salpingo-oophorectomy bilateral 12.55 11.97 4 21897 146 50583077
Death 12.48 11.97 86 21815 325293 50257930
Pyrexia 12.46 11.97 105 21796 380098 50203125
Insulin resistance 12.16 11.97 6 21895 702 50582521
Neutrophilia 12.13 11.97 11 21890 3564 50579659
Face oedema 12.10 11.97 25 21876 17814 50565409

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
Bladder cancer 2566.23 12.13 733 23655 9394 29540745
Bladder transitional cell carcinoma 384.18 12.13 123 24265 2338 29547801
Blood glucose increased 252.83 12.13 276 24112 58708 29491431
Hypoglycaemia 222.55 12.13 235 24153 48111 29502028
Pancreatitis 131.43 12.13 152 24236 34362 29515777
Cardiac failure congestive 124.57 12.13 225 24163 76356 29473783
Diabetes mellitus inadequate control 124.48 12.13 93 24295 12041 29538098
Glycosylated haemoglobin increased 123.83 12.13 84 24304 9342 29540797
Oedema peripheral 99.14 12.13 245 24143 103312 29446827
Haematuria 97.66 12.13 149 24239 43990 29506149
Pancreatic carcinoma 94.58 12.13 64 24324 7086 29543053
Bladder neoplasm 82.08 12.13 33 24355 1231 29548908
Diabetic ketoacidosis 80.79 12.13 82 24306 15991 29534148
Blood glucose decreased 65.12 12.13 64 24324 12005 29538134
Transitional cell carcinoma 59.63 12.13 30 24358 1905 29548234
Myocardial infarction 59.51 12.13 213 24175 110083 29440056
Macular oedema 55.60 12.13 31 24357 2427 29547712
Weight increased 52.91 12.13 161 24227 76506 29473633
Off label use 52.35 12.13 106 24282 300694 29249445
Ureteric cancer 49.28 12.13 14 24374 173 29549966
Toxicity to various agents 47.48 12.13 44 24344 173617 29376522
Product use in unapproved indication 42.03 12.13 10 24378 86865 29463274
Drug ineffective 41.51 12.13 157 24231 363013 29187126
Pancreatitis acute 40.00 12.13 72 24316 24313 29525826
Bladder cancer recurrent 37.85 12.13 13 24375 309 29549830
Oedema 36.77 12.13 94 24294 40389 29509750
Genital infection fungal 36.76 12.13 11 24377 165 29549974
Coronary artery disease 36.47 12.13 99 24289 44091 29506048
Bladder cancer stage 0, with cancer in situ 35.96 12.13 8 24380 32 29550107
Hyperglycaemia 34.72 12.13 83 24305 34204 29515935
Diabetic nephropathy 30.03 12.13 19 24369 1876 29548263
Death 29.98 12.13 163 24225 341921 29208218
Meningitis eosinophilic 28.56 12.13 6 24382 17 29550122
Prostate cancer 28.25 12.13 64 24324 25463 29524676
Pemphigoid 28.17 12.13 33 24355 7548 29542591
Product complaint 27.92 12.13 28 24360 5377 29544762
Acute myocardial infarction 27.32 12.13 95 24293 48343 29501796
Gallbladder neoplasm 26.78 12.13 6 24382 25 29550114
Urethral cancer 25.41 12.13 6 24382 33 29550106
Hypoglycaemic coma 25.40 12.13 18 24370 2145 29547994
Diabetic retinopathy 25.23 12.13 16 24372 1586 29548553
Diabetic metabolic decompensation 24.47 12.13 15 24373 1401 29548738
Bladder transitional cell carcinoma stage III 21.91 12.13 5 24383 23 29550116
General physical health deterioration 21.68 12.13 32 24356 102825 29447314
Bladder papilloma 21.25 12.13 5 24383 27 29550112
Hepatic cancer 20.57 12.13 26 24362 6430 29543709
Treatment failure 20.52 12.13 3 24385 36936 29513203
Pollakiuria 20.51 12.13 44 24344 16872 29533267
Cardiac failure 20.18 12.13 123 24265 79164 29470975
Euglycaemic diabetic ketoacidosis 20.18 12.13 17 24371 2613 29547526
Weight decreased 19.94 12.13 201 24187 150704 29399435
Neutropenia 19.90 12.13 50 24338 131661 29418478
Overdose 19.75 12.13 22 24366 79797 29470342
Anti-insulin antibody positive 19.54 12.13 7 24381 189 29549950
Bladder cancer stage II 19.44 12.13 7 24381 192 29549947
Malignant neoplasm of renal pelvis 19.34 12.13 5 24383 42 29550097
Renal cyst 19.33 12.13 28 24360 7879 29542260
Thrombocytopenia 18.98 12.13 53 24335 134770 29415369
Diabetic neuropathy 18.58 12.13 19 24369 3734 29546405
Infectious mononucleosis 18.47 12.13 9 24379 533 29549606
Urine cytology abnormal 18.30 12.13 3 24385 0 29550139
Cerebral infarction 18.11 12.13 53 24335 24622 29525517
Pyrexia 17.70 12.13 152 24236 287470 29262669
Bladder transitional cell carcinoma stage II 17.66 12.13 5 24383 61 29550078
Metastatic carcinoma of the bladder 17.22 12.13 6 24382 149 29549990
Pulmonary oedema 16.92 12.13 75 24313 42660 29507479
Cerebrovascular accident 16.92 12.13 115 24273 76796 29473343
Intentional product use issue 16.79 12.13 7 24381 42491 29507648
Abnormal weight gain 16.68 12.13 10 24378 897 29549242
Blood creatine phosphokinase increased 15.84 12.13 71 24317 40573 29509566
Insulin resistance 15.64 12.13 8 24380 526 29549613
Product use issue 15.29 12.13 12 24376 51432 29498707
Post-thoracotomy pain syndrome 15.23 12.13 4 24384 36 29550103
Bladder adenocarcinoma stage unspecified 15.01 12.13 3 24385 6 29550133
Drug intolerance 14.74 12.13 11 24377 48368 29501771
Retinal aneurysm 14.47 12.13 5 24383 121 29550018
Pleural effusion 14.34 12.13 105 24283 71803 29478336
Angina pectoris 14.31 12.13 53 24335 27797 29522342
Loss of consciousness 14.12 12.13 107 24281 73949 29476190
Sleep talking 14.05 12.13 7 24381 435 29549704
Rectal cancer 14.04 12.13 12 24376 1880 29548259
Blood glucose abnormal 13.91 12.13 19 24369 5064 29545075
Metastases to liver 13.42 12.13 30 24358 11826 29538313
Hypoglycaemic unconsciousness 12.97 12.13 8 24380 755 29549384
Urogenital infection fungal 12.94 12.13 3 24385 15 29550124
Diabetes mellitus 12.93 12.13 66 24322 39765 29510374
Aortic stenosis 12.91 12.13 16 24372 3878 29546261
Angina unstable 12.87 12.13 28 24360 10837 29539302
Renal cancer 12.76 12.13 17 24371 4424 29545715
Intentional overdose 12.75 12.13 8 24380 38520 29511619
Blood urine present 12.55 12.13 26 24362 9729 29540410
Interstitial lung disease 12.50 12.13 86 24302 57632 29492507
Diabetic retinal oedema 12.47 12.13 5 24383 185 29549954
Febrile neutropenia 12.43 12.13 49 24339 112191 29437948
Hyperlipidaemia 12.22 12.13 30 24358 12560 29537579

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
Bladder cancer 2534.36 11.20 682 35858 10292 64451900
Hypoglycaemia 557.50 11.20 438 36102 89454 64372738
Blood glucose increased 474.80 11.20 414 36126 97659 64364533
Bladder transitional cell carcinoma 463.65 11.20 129 36411 2201 64459991
Diabetes mellitus inadequate control 230.18 11.20 146 36394 21175 64441017
Cardiac failure congestive 222.00 11.20 319 36221 130261 64331931
Diabetic ketoacidosis 177.31 11.20 142 36398 29703 64432489
Oedema peripheral 175.01 11.20 375 36165 209942 64252250
Glycosylated haemoglobin increased 151.56 11.20 101 36439 15918 64446274
Haematuria 135.23 11.20 169 36371 60302 64401890
Bladder neoplasm 134.33 11.20 45 36495 1461 64460731
Blood glucose decreased 128.85 11.20 106 36434 23017 64439175
Pancreatic carcinoma 114.35 11.20 72 36468 10301 64451891
Myocardial infarction 107.31 11.20 268 36272 165553 64296639
Pancreatitis 106.13 11.20 149 36391 59458 64402734
Diabetic metabolic decompensation 98.27 11.20 42 36498 2686 64459506
Drug ineffective 90.28 11.20 216 36324 840031 63622161
Weight increased 85.07 11.20 290 36250 213058 64249134
Off label use 83.79 11.20 144 36396 632662 63829530
Macular oedema 83.44 11.20 45 36495 4822 64457370
Ureteric cancer 82.83 11.20 21 36519 245 64461947
Cardiac failure 76.38 11.20 205 36335 132168 64330024
Transitional cell carcinoma 72.44 11.20 32 36508 2217 64459975
Oedema 71.82 11.20 160 36380 91775 64370417
Hyperglycaemia 70.43 11.20 125 36415 60843 64401349
Coronary artery disease 62.35 11.20 118 36422 60315 64401877
Diabetic retinopathy 56.49 11.20 29 36511 2810 64459382
Acute myocardial infarction 51.83 11.20 119 36421 69599 64392593
Drug intolerance 51.51 11.20 21 36519 187971 64274221
Drug abuse 51.46 11.20 7 36533 132367 64329825
Pancreatitis acute 50.95 11.20 89 36451 42766 64419426
Hypoglycaemic coma 50.47 11.20 31 36509 4243 64457949
Rheumatoid arthritis 48.98 11.20 16 36524 164278 64297914
Bladder cancer stage 0, with cancer in situ 46.88 11.20 10 36530 50 64462142
Bladder cancer recurrent 42.77 11.20 14 36526 422 64461770
Infusion related reaction 42.47 11.20 20 36520 164447 64297745
Pemphigoid 42.07 11.20 44 36496 12942 64449250
Lactic acidosis 41.50 11.20 101 36439 61309 64400883
Treatment failure 41.32 11.20 8 36532 116808 64345384
Genital infection fungal 41.03 11.20 11 36529 162 64462030
Bladder adenocarcinoma stage unspecified 39.37 11.20 8 36532 30 64462162
Product use in unapproved indication 37.76 11.20 27 36513 176591 64285601
Diabetes mellitus 36.36 11.20 101 36439 66373 64395819
Toxicity to various agents 34.58 11.20 99 36441 363414 64098778
Prostate cancer 34.49 11.20 49 36491 19746 64442446
Diabetic neuropathy 33.99 11.20 27 36513 5574 64456618
Diabetic nephropathy 33.27 11.20 20 36520 2634 64459558
Product use issue 32.68 11.20 23 36517 151692 64310500
Angina unstable 32.60 11.20 42 36498 15425 64446767
General physical health deterioration 32.31 11.20 41 36499 204384 64257808
Bladder papilloma 31.07 11.20 6 36534 16 64462176
Maternal exposure during pregnancy 31.03 11.20 8 36532 95876 64366316
Rhabdomyolysis 30.80 11.20 118 36422 91608 64370584
Euglycaemic diabetic ketoacidosis 30.54 11.20 25 36515 5385 64456807
Urine cytology abnormal 30.04 11.20 5 36535 3 64462189
Weight decreased 29.65 11.20 269 36271 285470 64176722
Pulmonary oedema 29.59 11.20 105 36435 78569 64383623
Chest pain 29.15 11.20 231 36309 235749 64226443
Retinal aneurysm 28.58 11.20 9 36531 239 64461953
Lower respiratory tract infection 28.57 11.20 9 36531 94605 64367587
Cerebral infarction 28.25 11.20 68 36472 40976 64421216
Cerebrovascular accident 28.21 11.20 153 36387 137430 64324762
Contraindicated product administered 26.49 11.20 14 36526 107815 64354377
Blood creatine phosphokinase increased 26.33 11.20 83 36457 58475 64403717
Urethral cancer 25.70 11.20 6 36534 48 64462144
Hepatic cancer 25.50 11.20 26 36514 7422 64454770
Meningitis eosinophilic 25.46 11.20 5 36535 15 64462177
Bladder trabeculation 24.69 11.20 6 36534 58 64462134
Product complaint 24.47 11.20 32 36508 11922 64450270
Exposure during pregnancy 24.16 11.20 7 36533 77668 64384524
Dehydration 23.98 11.20 207 36333 216556 64245636
Retinal haemorrhage 23.85 11.20 25 36515 7373 64454819
Gallbladder neoplasm 23.59 11.20 6 36534 71 64462121
Pleural effusion 23.47 11.20 137 36403 126422 64335770
Bladder transitional cell carcinoma stage III 23.28 11.20 5 36535 26 64462166
Fluid retention 21.94 11.20 79 36461 59527 64402665
Glossodynia 21.71 11.20 5 36535 64691 64397501
Insulin resistance 21.20 11.20 11 36529 1089 64461103
Visual acuity reduced 20.91 11.20 47 36493 27094 64435098
Blood triglycerides increased 20.90 11.20 38 36502 18828 64443364
Blood glucose fluctuation 20.78 11.20 21 36519 5934 64456258
Death 20.48 11.20 175 36365 482530 63979662
Ketoacidosis 20.02 11.20 22 36518 6841 64455351
Hypersensitivity 19.77 11.20 52 36488 196400 64265792
Pyrexia 19.69 11.20 212 36328 558432 63903760
Anti-insulin antibody positive 19.50 11.20 7 36533 280 64461912
Cholelithiasis 19.09 11.20 63 36477 45443 64416749
Alopecia 18.95 11.20 41 36499 165649 64296543
Pericarditis 18.78 11.20 6 36534 62510 64399682
Febrile neutropenia 18.64 11.20 50 36490 187607 64274585
IIIrd nerve paralysis 18.60 11.20 10 36530 1064 64461128
Intentional product use issue 18.58 11.20 16 36524 95348 64366844
Angina pectoris 18.55 11.20 62 36478 45019 64417173
Lacunar infarction 18.38 11.20 19 36521 5513 64456679
Bladder transitional cell carcinoma stage II 18.32 11.20 5 36535 79 64462113
Cardiomegaly 18.23 11.20 41 36499 23643 64438549
Diabetic retinal oedema 18.21 11.20 7 36533 340 64461852
Biopsy skin abnormal 18.14 11.20 6 36534 187 64462005
Coronary artery occlusion 18.02 11.20 30 36510 13861 64448331
Retinal exudates 17.96 11.20 10 36530 1140 64461052
Hepatic function abnormal 17.83 11.20 78 36462 64235 64397957
High density lipoprotein decreased 17.73 11.20 16 36524 3930 64458262
Renal cyst 17.46 11.20 28 36512 12542 64449650
Pancreatic carcinoma metastatic 17.42 11.20 15 36525 3463 64458729
Fatigue 17.15 11.20 310 36230 748420 63713772
Therapeutic product effect incomplete 17.14 11.20 20 36520 103462 64358730
Blood glucose abnormal 16.93 11.20 23 36517 8890 64453302
Renal cell carcinoma 16.83 11.20 19 36521 6085 64456107
Pain 16.82 11.20 217 36323 553294 63908898
Fasting 16.82 11.20 4 36536 35 64462157
Renal failure 16.81 11.20 167 36373 181521 64280671
Renal cancer 16.62 11.20 20 36520 6855 64455337
Acute kidney injury 16.47 11.20 351 36189 448889 64013303
Peripheral swelling 16.38 11.20 62 36478 209091 64253101
Malignant neoplasm of renal pelvis 16.28 11.20 5 36535 122 64462070
Aortic stenosis 16.19 11.20 19 36521 6346 64455846
Joint swelling 16.13 11.20 65 36475 215317 64246875
Nasopharyngitis 16.09 11.20 57 36483 196016 64266176
Fall 15.70 11.20 327 36213 416499 64045693
Diabetic complication 15.25 11.20 9 36531 1146 64461046
Discomfort 15.23 11.20 14 36526 80864 64381328
Neutropenia 15.14 11.20 77 36463 239547 64222645
Pancreatitis chronic 15.06 11.20 14 36526 3572 64458620
Blood urea increased 14.98 11.20 57 36483 44096 64418096
Transient ischaemic attack 14.95 11.20 57 36483 44125 64418067
Microalbuminuria 14.83 11.20 8 36532 857 64461335
Low density lipoprotein increased 14.74 11.20 20 36520 7720 64454472
Wound 14.69 11.20 13 36527 76464 64385728
Portal fibrosis 14.63 11.20 7 36533 583 64461609
Rash 14.58 11.20 178 36362 458371 64003821
Radius fracture 14.48 11.20 13 36527 3171 64459021
Metastatic carcinoma of the bladder 14.40 11.20 5 36535 181 64462011
Stomatitis 14.37 11.20 25 36515 109580 64352612
Chronic gastritis 14.29 11.20 13 36527 3227 64458965
Cardiac disorder 14.20 11.20 66 36474 55750 64406442
Infectious mononucleosis 14.19 11.20 10 36530 1723 64460469
Decreased appetite 14.19 11.20 231 36309 281058 64181134
Peripheral vascular disorder 14.19 11.20 19 36521 7242 64454950
Mucosal inflammation 14.13 11.20 9 36531 62575 64399617
Ketosis 14.11 11.20 8 36532 945 64461247
Multiple injuries 14.09 11.20 13 36527 3286 64458906
Urogenital infection fungal 14.06 11.20 3 36537 15 64462177
Face oedema 13.91 11.20 38 36502 24723 64437469
Blood pressure fluctuation 13.86 11.20 6 36534 51865 64410327
Rectal cancer 13.85 11.20 12 36528 2794 64459398
Arthropathy 13.77 11.20 30 36510 120937 64341255
Varicose vein ruptured 13.73 11.20 4 36536 81 64462111
Musculoskeletal stiffness 13.66 11.20 31 36509 123175 64339017
Ill-defined disorder 13.64 11.20 4 36536 44048 64418144
Arthralgia 13.56 11.20 173 36367 442087 64020105
Pollakiuria 13.54 11.20 44 36496 31486 64430706
Adenocarcinoma pancreas 13.50 11.20 10 36530 1863 64460329
Coma 13.39 11.20 18 36522 87597 64374595
Psoriatic arthropathy 13.27 11.20 4 36536 43277 64418915
Treatment noncompliance 13.03 11.20 54 36486 43428 64418764
Nocturia 13.02 11.20 23 36517 11142 64451050
Bladder cancer stage II 12.98 11.20 5 36535 244 64461948
Hypoglycaemic unconsciousness 12.90 11.20 8 36532 1113 64461079
Arteriosclerosis 12.80 11.20 28 36512 15849 64446343
Salpingo-oophorectomy bilateral 12.74 11.20 3 36537 25 64462167
Medication error 12.65 11.20 59 36481 49907 64412285
Polydipsia 12.57 11.20 16 36524 5805 64456387
Cardiac failure acute 12.25 11.20 28 36512 16316 64445876
Cytomegalovirus infection 12.23 11.20 3 36537 37196 64424996
Urine ketone body present 12.16 11.20 12 36528 3295 64458897
Loss of control of legs 12.08 11.20 9 36531 1690 64460502
Abnormal weight gain 12.02 11.20 10 36530 2203 64459989
Dilatation atrial 11.73 11.20 12 36528 3438 64458754
Multiple organ dysfunction syndrome 11.67 11.20 25 36515 101388 64360804
Nicotinic acid deficiency 11.65 11.20 4 36536 140 64462052
Neuropathic arthropathy 11.65 11.20 5 36535 323 64461869
Humerus fracture 11.56 11.20 18 36522 7867 64454325
Hypoglycaemic encephalopathy 11.45 11.20 6 36534 606 64461586
Thrombocytopenia 11.42 11.20 77 36463 223724 64238468
Cough 11.29 11.20 113 36427 302035 64160157
Blood ketone body increased 11.27 11.20 6 36534 626 64461566
Adult failure to thrive 11.24 11.20 4 36536 156 64462036
Gastric cancer 11.20 11.20 16 36524 6477 64455715

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A10BD05 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD06 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD09 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD12 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BG03 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Thiazolidinediones
FDA CS M0199111 PPAR alpha
FDA CS M0199114 PPAR gamma
FDA CS M0447306 Thiazolidinediones
FDA MoA N0000175374 Peroxisome Proliferator-activated Receptor Activity
FDA EPC N0000175596 Peroxisome Proliferator Receptor alpha Agonist
MeSH PA D007004 Hypoglycemic Agents
CHEBI has role CHEBI:35469 antidepressants
CHEBI has role CHEBI:35526 antidiabetic
CHEBI has role CHEBI:35703 Xenobiotic
CHEBI has role CHEBI:50864 insulin sensitizers
CHEBI has role CHEBI:71554 PPARgamma agonist
CHEBI has role CHEBI:77194 ATP:pantothenate 4-phosphotransferase inhibitor
CHEBI has role CHEBI:77307 cardioprotective agents
CHEBI has role CHEBI:83157 EC 6.2.1.3 inhibitors
CHEBI has role CHEBI:173084 ferroptosis inhibitors
CHEBI has role CHEBI:176497 geroprotectors
FDA EPC N0000180186 Peroxisome Proliferator Receptor gamma Agonist
FDA EPC N0000180190 Thiazolidinedione

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

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Alcoholism contraindication 7200002
Asthenia contraindication 13791008
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
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
Decompensated cardiac failure contraindication 195111005
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Sepsis syndrome contraindication 238150007
Edema contraindication 267038008
Primary adrenocortical insufficiency contraindication 373662000
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Fever contraindication 386661006
Surgical procedure contraindication 387713003
Malignant tumor of urinary bladder contraindication 399326009 DOID:11054
Severe diarrhea contraindication 409587002
Breastfeeding (mother) contraindication 413712001
Traumatic injury contraindication 417746004
Fever greater than 100.4 Fahrenheit contraindication 426000000
Radiography with IV Iodinated Contrast Agent contraindication
Severe Hypoxemia contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.33 acidic
pKa2 7.15 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 12.5MG BASE;EQ 15MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 DISCN TABLET ORAL 8173663 March 15, 2025 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING A COMPOUND SUCH AS ALOGLIPTIN
EQ 12.5MG BASE;EQ 30MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 8173663 March 15, 2025 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING A COMPOUND SUCH AS ALOGLIPTIN
EQ 12.5MG BASE;EQ 45MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 DISCN TABLET ORAL 8173663 March 15, 2025 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING A COMPOUND SUCH AS ALOGLIPTIN
EQ 25MG BASE;EQ 15MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 8173663 March 15, 2025 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING A COMPOUND SUCH AS ALOGLIPTIN
EQ 25MG BASE;EQ 30MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 8173663 March 15, 2025 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING A COMPOUND SUCH AS ALOGLIPTIN
EQ 25MG BASE;EQ 45MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 8173663 March 15, 2025 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING A COMPOUND SUCH AS ALOGLIPTIN
EQ 12.5MG BASE;EQ 15MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 DISCN TABLET ORAL 7807689 June 27, 2028 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING ALOGLIPTIN
EQ 12.5MG BASE;EQ 30MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 7807689 June 27, 2028 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING ALOGLIPTIN
EQ 12.5MG BASE;EQ 45MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 DISCN TABLET ORAL 7807689 June 27, 2028 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING ALOGLIPTIN
EQ 25MG BASE;EQ 15MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 7807689 June 27, 2028 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING ALOGLIPTIN
EQ 25MG BASE;EQ 30MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 7807689 June 27, 2028 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING ALOGLIPTIN
EQ 25MG BASE;EQ 45MG BASE OSENI TAKEDA PHARMS USA N022426 Jan. 25, 2013 RX TABLET ORAL 7807689 June 27, 2028 METHOD OF TREATING DIABETES COMPRISING ADMINISTERING ALOGLIPTIN

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 6.23 WOMBAT-PK CHEMBL
Bile salt export pump Transporter IC50 6.52 CHEMBL
Amine oxidase [flavin-containing] B Enzyme Ki 6.30 CHEMBL
Amine oxidase [flavin-containing] A Enzyme IC50 4.46 DRUG MATRIX
Peroxisome proliferator-activated receptor alpha Nuclear hormone receptor EC50 5.18 CHEMBL
CDGSH iron-sulfur domain-containing protein 1 Unclassified Ki 6.43 CHEMBL
Carbonic anhydrase 2 Enzyme IC50 6.94 DRUG MATRIX
CDGSH iron-sulfur domain-containing protein 2 Unclassified IC50 5.32 CHEMBL
Aldose reductase Enzyme IC50 4.88 DRUG MATRIX
Amine oxidase [flavin-containing] B Enzyme Ki 5.68 CHEMBL
Peroxisome proliferator-activated receptor alpha Transcription factor IC50 5.94 CHEMBL
Peroxisome proliferator-activated receptor gamma Transcription factor IC50 6.15 CHEMBL
Peroxisome proliferator-activated receptor gamma Transcription factor IC50 6.15 CHEMBL
Enoyl-[acyl-carrier-protein] reductase [NADH] Enzyme IC50 4.10 CHEMBL
Bile salt export pump Transporter IC50 5.70 CHEMBL
CDGSH iron-sulfur domain-containing protein 1 Unclassified IC50 6 CHEMBL

External reference:

IDSource
4021165 VUID
N0000148616 NUI
D00945 KEGG_DRUG
112529-15-4 SECONDARY_CAS_RN
4021165 VANDF
4021166 VANDF
4029214 VANDF
C0071097 UMLSCUI
CHEBI:8228 CHEBI
8N6 PDB_CHEM_ID
CHEMBL595 ChEMBL_ID
DB01132 DRUGBANK_ID
CHEMBL1715 ChEMBL_ID
D000077205 MESH_DESCRIPTOR_UI
4829 PUBCHEM_CID
2694 IUPHAR_LIGAND_ID
6343 INN_ID
X4OV71U42S UNII
259319 RXNORM
178611 MMSL
29092 MMSL
35713 MMSL
8258 MMSL
d04442 MMSL
007823 NDDF
007824 NDDF
116097005 SNOMEDCT_US
326058001 SNOMEDCT_US
395828009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0093-7271 TABLET 15 mg ORAL ANDA 29 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0093-7272 TABLET 30 mg ORAL ANDA 29 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0093-7273 TABLET 45 mg ORAL ANDA 29 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5420 TABLET 15 mg ORAL ANDA 28 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5421 TABLET 30 mg ORAL ANDA 28 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0781-5422 TABLET 45 mg ORAL ANDA 28 sections
Pioglitazone and metformin HUMAN PRESCRIPTION DRUG LABEL 2 0781-5626 TABLET, FILM COATED 15 mg ORAL ANDA 29 sections
Pioglitazone and metformin HUMAN PRESCRIPTION DRUG LABEL 2 0781-5627 TABLET, FILM COATED 15 mg ORAL ANDA 29 sections
Pioglitazone hydrochloride and glimepiride HUMAN PRESCRIPTION DRUG LABEL 2 0781-5634 TABLET 30 mg ORAL ANDA 28 sections
Pioglitazone hydrochloride and glimepiride HUMAN PRESCRIPTION DRUG LABEL 2 0781-5635 TABLET 30 mg ORAL ANDA 28 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0904-7090 TABLET 15 mg ORAL ANDA 30 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 0904-7096 TABLET 30 mg ORAL ANDA 30 sections
PIOGLITAZONEHYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 13668-119 TABLET 30 mg ORAL ANDA 26 sections
PIOGLITAZONEHYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 13668-120 TABLET 45 mg ORAL ANDA 26 sections
PIOGLITAZONEHYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 13668-140 TABLET 15 mg ORAL ANDA 26 sections
Pioglitazone HCL and Metformin HCL HUMAN PRESCRIPTION DRUG LABEL 2 13668-280 TABLET 15 mg ORAL ANDA 28 sections
Pioglitazone HCL and Metformin HCL HUMAN PRESCRIPTION DRUG LABEL 2 13668-281 TABLET 15 mg ORAL ANDA 28 sections
PIOGLITAZONE HUMAN PRESCRIPTION DRUG LABEL 1 16729-020 TABLET 15 mg ORAL ANDA 29 sections
PIOGLITAZONE HUMAN PRESCRIPTION DRUG LABEL 1 16729-021 TABLET 30 mg ORAL ANDA 29 sections
PIOGLITAZONE HUMAN PRESCRIPTION DRUG LABEL 1 16729-022 TABLET 45 mg ORAL ANDA 29 sections
Actos HUMAN PRESCRIPTION DRUG LABEL 1 21695-147 TABLET 15 mg ORAL NDA 31 sections
Actos HUMAN PRESCRIPTION DRUG LABEL 1 21695-148 TABLET 30 mg ORAL NDA 31 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 33342-054 TABLET 15 mg ORAL ANDA 30 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 33342-055 TABLET 30 mg ORAL ANDA 30 sections
Pioglitazone HUMAN PRESCRIPTION DRUG LABEL 1 33342-056 TABLET 45 mg ORAL ANDA 30 sections
Pioglitazole and metformin hydrochloride Human Prescription Drug Label 2 33342-176 TABLET 15 mg ORAL ANDA 30 sections
Pioglitazole and metformin hydrochloride Human Prescription Drug Label 2 33342-177 TABLET 15 mg ORAL ANDA 30 sections
Pioglitazone Hydrochloride Human Prescription Drug Label 1 43353-326 TABLET 45 mg ORAL ANDA 28 sections
PIOGLITAZONE HUMAN PRESCRIPTION DRUG LABEL 1 43547-426 TABLET 15 mg ORAL ANDA 21 sections
PIOGLITAZONE HUMAN PRESCRIPTION DRUG LABEL 1 43547-427 TABLET 30 mg ORAL ANDA 21 sections