dapagliflozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives 4304 461432-26-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dapagliflozin propanediol monohydrate
  • dapagliflozin propanediol
  • BMS 512148
  • forxiga
  • dapaglifozin
  • dapagliflozin
  • farxiga
  • dapagliflozin propylene glycolate hydrate
an Sodium-glucose cotransporter 2 (SGLT2) inhibitor, SGLT2 expressed in the proximal renal tubules, is responsible for the majority of the reabsorption of filtered glucose from the tubular lumen, by inhibiting SGLT2, dapagliflozin reduces reabsorption of filtered glucose and lowers the renal threshold for glucose, and thereby increases urinary glucose excretion
  • Molecular weight: 408.88
  • Formula: C21H25ClO6
  • CLOGP: 3.37
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 99.38
  • ALOGS: -3.37
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.70 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.09 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 12.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 24, 2014 PMDA BRISTOL-MYERS
Jan. 8, 2014 FDA ASTRAZENECA AB
Nov. 12, 2012 EMA

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
Diabetic ketoacidosis 3100.88 18.82 719 9724 17153 50577528
Ketoacidosis 1369.35 18.82 281 10162 3614 50591067
Euglycaemic diabetic ketoacidosis 935.45 18.82 194 10249 2625 50592056
Fungal infection 354.82 18.82 156 10287 29809 50564872
Ketosis 179.15 18.82 37 10406 486 50594195
Diabetes mellitus inadequate control 147.56 18.82 66 10377 13079 50581602
Glycosylated haemoglobin increased 137.70 18.82 59 10384 10547 50584134
Ketonuria 130.65 18.82 28 10415 444 50594237
Urinary tract infection 127.21 18.82 191 10252 223829 50370852
Blood glucose increased 102.85 18.82 98 10345 71226 50523455
Hypoglycaemia 91.59 18.82 81 10362 53500 50541181
Lactic acidosis 90.25 18.82 66 10377 33289 50561392
Blood ketone body increased 86.07 18.82 18 10425 252 50594429
Diabetic metabolic decompensation 81.07 18.82 24 10419 1456 50593225
Acute kidney injury 76.18 18.82 154 10289 227904 50366777
Glomerular filtration rate decreased 74.93 18.82 40 10403 11612 50583069
Urine ketone body present 74.26 18.82 25 10418 2308 50592373
Weight decreased 71.04 18.82 147 10296 221098 50373583
Dehydration 69.81 18.82 118 10325 152331 50442350
Metabolic acidosis 68.95 18.82 60 10383 38765 50555916
Diabetic ketosis 68.12 18.82 14 10429 179 50594502
Hyperglycaemia 58.16 18.82 53 10390 36352 50558329
Vulvovaginal pruritus 53.72 18.82 20 10423 2476 50592205
Pyelonephritis 53.06 18.82 35 10408 14954 50579727
Necrotising fasciitis 52.89 18.82 20 10423 2584 50592097
Genital infection female 51.76 18.82 10 10433 91 50594590
Pruritus genital 51.74 18.82 14 10429 612 50594069
Temperature perception test abnormal 50.78 18.82 8 10435 17 50594664
Glucose urine present 45.83 18.82 13 10430 677 50594004
Left ventricular dysfunction 43.29 18.82 27 10416 10479 50584202
Candida infection 43.05 18.82 37 10406 23486 50571195
Pollakiuria 40.60 18.82 36 10407 23815 50570866
Urosepsis 40.45 18.82 30 10413 15435 50579246
Cerebral infarction 39.58 18.82 34 10409 21570 50573111
Polyuria 39.02 18.82 22 10421 7099 50587582
Genital infection 37.61 18.82 7 10436 51 50594630
Genital infection fungal 34.98 18.82 8 10435 173 50594508
Decreased vibratory sense 32.60 18.82 8 10435 236 50594445
Drug ineffective 31.93 18.82 77 10366 819256 49775425
Acidosis 31.70 18.82 22 10421 10205 50584476
Bladder trabeculation 31.11 18.82 6 10437 54 50594627
Haematuria 30.94 18.82 32 10411 25581 50569100
Pancreatitis 29.43 18.82 40 10403 42574 50552107
Cardiac failure 28.50 18.82 54 10389 75986 50518695
Vulvovaginal mycotic infection 27.58 18.82 15 10428 4514 50590167
Blood glucose abnormal 27.12 18.82 17 10426 6655 50588026
Dysuria 26.44 18.82 31 10412 28473 50566208
Peripartum cardiomyopathy 26.22 18.82 6 10437 130 50594551
Toe amputation 26.20 18.82 11 10432 1866 50592815
Urinary tract infection fungal 25.69 18.82 8 10435 576 50594105
Compartment syndrome 25.63 18.82 11 10432 1971 50592710
Blood ketone body 25.54 18.82 5 10438 49 50594632
Suspected COVID-19 25.32 18.82 10 10433 1451 50593230
Pain 25.28 18.82 51 10392 578852 50015829
Hyperglycaemic hyperosmolar nonketotic syndrome 25.22 18.82 8 10435 612 50594069
Vomiting 24.72 18.82 171 10272 460587 50134094
Arteriosclerosis 24.62 18.82 18 10425 9059 50585622
Capillary leak syndrome 22.84 18.82 10 10433 1880 50592801
Dizziness 22.52 18.82 135 10308 346234 50248447
Perineal pain 22.43 18.82 6 10437 251 50594430
Latent autoimmune diabetes in adults 22.31 18.82 4 10439 23 50594658
Portal fibrosis 22.13 18.82 6 10437 264 50594417
Thirst 22.06 18.82 18 10425 10632 50584049
Upper airway obstruction 21.69 18.82 7 10436 566 50594115
Food refusal 21.09 18.82 6 10437 316 50594365
Atrioventricular block complete 21.07 18.82 15 10428 7240 50587441
Contraindicated product administered 20.80 18.82 3 10440 148955 50445726
Glycosuria 20.77 18.82 8 10435 1086 50593595
Pyelonephritis acute 20.72 18.82 12 10431 4071 50590610
Toxicity to various agents 20.66 18.82 9 10434 212490 50382191
Rheumatoid arthritis 20.63 18.82 8 10435 202542 50392139
Aortic valve calcification 19.70 18.82 6 10437 401 50594280
Vulvovaginal candidiasis 19.46 18.82 10 10433 2682 50591999
Orthopnoea 19.44 18.82 13 10430 5676 50589005
Diabetic ketoacidotic hyperglycaemic coma 19.33 18.82 4 10439 53 50594628
Metabolic alkalosis 19.33 18.82 10 10433 2721 50591960
Hyperkalaemia 19.07 18.82 35 10408 48054 50546627

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
Diabetic ketoacidosis 2177.06 17.82 601 10676 15472 29547778
Ketoacidosis 782.36 17.82 197 11080 3442 29559808
Euglycaemic diabetic ketoacidosis 618.26 17.82 153 11124 2477 29560773
Glycosylated haemoglobin increased 207.00 17.82 91 11186 9335 29553915
Ketosis 175.26 17.82 39 11238 384 29562866
Ketonuria 147.60 17.82 36 11241 544 29562706
Phimosis 136.64 17.82 35 11242 652 29562598
Balanoposthitis 128.08 17.82 36 11241 966 29562284
Blood glucose increased 107.22 17.82 122 11155 58862 29504388
Fungal infection 104.32 17.82 65 11212 13620 29549630
Diabetic ketosis 99.26 17.82 19 11258 80 29563170
Glomerular filtration rate abnormal 91.78 17.82 26 11251 718 29562532
Metabolic acidosis 89.79 17.82 90 11187 37572 29525678
Glomerular filtration rate decreased 89.64 17.82 55 11222 11211 29552039
Lactic acidosis 88.63 17.82 81 11196 30166 29533084
Diabetes mellitus inadequate control 88.38 17.82 56 11221 12078 29551172
Polyuria 82.74 17.82 45 11232 7317 29555933
N-terminal prohormone brain natriuretic peptide increased 81.98 17.82 30 11247 1902 29561348
Toe amputation 78.79 17.82 30 11247 2125 29561125
Hypoglycaemia 74.57 17.82 92 11185 48254 29514996
Bladder cancer 74.40 17.82 47 11230 10080 29553170
Weight decreased 73.36 17.82 171 11106 150734 29412516
Blood ketone body increased 68.86 17.82 18 11259 364 29562886
Urinary tract infection 67.27 17.82 108 11169 72246 29491004
Type V hyperlipidaemia 66.70 17.82 20 11257 677 29562573
Necrotising fasciitis 65.88 17.82 30 11247 3335 29559915
Pollakiuria 65.17 17.82 53 11224 16863 29546387
Dehydration 61.23 17.82 135 11142 114613 29448637
Epididymitis 60.57 17.82 25 11252 2190 29561060
Acquired phimosis 60.19 17.82 12 11265 65 29563185
Urine ketone body present 54.79 17.82 19 11258 1029 29562221
Blood pressure decreased 52.32 17.82 75 11202 45402 29517848
Cerebral infarction 49.85 17.82 54 11223 24621 29538629
Hyperglycaemia 47.68 17.82 62 11215 34225 29529025
Glucose urine present 44.61 17.82 16 11261 957 29562293
Urosepsis 44.21 17.82 35 11242 10711 29552539
Hyperglycaemic hyperosmolar nonketotic syndrome 43.12 17.82 16 11261 1054 29562196
Cardiac failure 43.05 17.82 94 11183 79193 29484057
Acute kidney injury 42.17 17.82 206 11071 265061 29298189
Thirst 40.02 17.82 27 11250 6464 29556786
Mitral valve thickening 36.98 17.82 11 11266 362 29562888
Toxicity to various agents 35.61 17.82 11 11266 173650 29389600
Glycosuria 34.79 17.82 14 11263 1148 29562102
Thrombotic cerebral infarction 34.07 17.82 10 11267 314 29562936
Mitral valve calcification 33.05 17.82 11 11266 525 29562725
Ejection fraction decreased 32.32 17.82 35 11242 15943 29547307
Neutropenia 31.56 17.82 6 11271 131705 29431545
Blood glucose abnormal 30.99 17.82 21 11256 5062 29558188
Thrombocytopenia 30.54 17.82 7 11270 134816 29428434
Genital rash 30.34 17.82 10 11267 463 29562787
N-terminal prohormone brain natriuretic peptide abnormal 29.34 17.82 8 11269 191 29563059
Foot amputation 29.33 17.82 10 11267 514 29562736
Acute myocardial infarction 29.24 17.82 60 11217 48378 29514872
Perineal abscess 28.55 17.82 8 11269 212 29563038
Body mass index increased 28.33 17.82 11 11266 821 29562429
Gangrene 27.09 17.82 18 11259 4200 29559050
Microalbuminuria 26.96 17.82 10 11267 658 29562592
Obesity 26.14 17.82 25 11252 9838 29553412
Total cholesterol/HDL ratio increased 25.80 17.82 7 11270 164 29563086
Genital infection fungal 25.60 17.82 7 11270 169 29563081
Febrile neutropenia 25.07 17.82 6 11271 112234 29451016
Mitral valve incompetence 24.95 17.82 28 11249 13265 29549985
Pancreatitis 24.77 17.82 46 11231 34468 29528782
Cardiac failure chronic 24.34 17.82 20 11257 6447 29556803
Pancreatitis acute 23.43 17.82 37 11240 24348 29538902
Hyperuricaemia 23.24 17.82 20 11257 6869 29556381
Hypertrophy 22.89 17.82 8 11269 443 29562807
Genital infection male 22.78 17.82 4 11273 9 29563241
Peripheral circulatory failure 22.47 17.82 6 11271 132 29563118
Urine output increased 22.44 17.82 10 11267 1056 29562194
Renal atrophy 22.25 17.82 10 11267 1077 29562173
Acetonaemia 22.10 17.82 6 11271 141 29563109
Immune-mediated hepatitis 21.91 17.82 11 11266 1516 29561734
Brain stem infarction 21.88 17.82 10 11267 1120 29562130
Vaccination failure 21.69 17.82 8 11269 518 29562732
Bladder cancer recurrent 21.43 17.82 7 11270 315 29562935
Diabetes mellitus 21.33 17.82 47 11230 39784 29523466
Haematuria 21.32 17.82 50 11227 44089 29519161
Disease progression 21.24 17.82 3 11274 81913 29481337
Hypoglycaemic coma 20.96 17.82 12 11265 2151 29561099
Polycythaemia 20.53 17.82 11 11266 1733 29561517
Drug ineffective 20.25 17.82 71 11206 363099 29200151
Type 2 diabetes mellitus 19.56 17.82 25 11252 13556 29549694
Pancytopenia 19.47 17.82 4 11273 83164 29480086
Pyrexia 19.02 17.82 52 11225 287570 29275680
Pyelonephritis 18.89 17.82 16 11261 5377 29557873
Dysuria 18.79 17.82 32 11245 22408 29540842
Anaemia 18.59 17.82 30 11247 200921 29362329
Malignant neoplasm progression 18.47 17.82 3 11274 73856 29489394
Concomitant disease aggravated 17.91 17.82 15 11262 4963 29558287

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
Diabetic ketoacidosis 4112.57 16.15 1065 17416 28780 64451471
Ketoacidosis 1605.04 16.15 376 18105 6487 64473764
Euglycaemic diabetic ketoacidosis 1352.55 16.15 313 18168 5097 64475154
Ketosis 291.10 16.15 65 18416 888 64479363
Glycosylated haemoglobin increased 253.91 16.15 113 18368 15906 64464345
Ketonuria 223.32 16.15 54 18427 1063 64479188
Diabetes mellitus inadequate control 205.73 16.15 107 18374 21214 64459037
Lactic acidosis 166.28 16.15 139 18342 61271 64418980
Metabolic acidosis 160.61 16.15 145 18336 70813 64409438
Hypoglycaemia 151.20 16.15 156 18325 89736 64390515
Diabetic ketosis 145.74 16.15 31 18450 332 64479919
Fungal infection 142.17 16.15 100 18381 34151 64446100
Blood glucose increased 138.22 16.15 155 18326 97918 64382333
Dehydration 119.76 16.15 219 18262 216544 64263707
Acute kidney injury 115.31 16.15 335 18146 448905 64031346
Glomerular filtration rate decreased 112.42 16.15 70 18411 19502 64460749
Cerebral infarction 105.08 16.15 90 18391 40954 64439297
Polyuria 103.78 16.15 57 18424 12586 64467665
Hyperglycaemia 102.80 16.15 106 18375 60862 64419389
Weight decreased 99.58 16.15 239 18242 285500 64194751
Urine ketone body present 99.58 16.15 37 18444 3270 64476981
Blood ketone body increased 98.39 16.15 25 18456 607 64479644
Balanoposthitis 97.13 16.15 26 18455 778 64479473
Urinary tract infection 96.54 16.15 208 18273 231388 64248863
Toe amputation 93.94 16.15 36 18445 3464 64476787
Necrotising fasciitis 92.21 16.15 40 18441 5286 64474965
Glomerular filtration rate abnormal 85.60 16.15 26 18455 1233 64479018
Glucose urine present 78.96 16.15 26 18455 1606 64478645
Pollakiuria 78.39 16.15 68 18413 31462 64448789
Diabetic metabolic decompensation 73.00 16.15 28 18453 2700 64477551
Phimosis 71.81 16.15 18 18463 413 64479838
Type V hyperlipidaemia 71.16 16.15 21 18460 901 64479350
N-terminal prohormone brain natriuretic peptide increased 69.13 16.15 29 18452 3530 64476721
Cardiac failure 65.84 16.15 128 18353 132245 64348006
Hyperglycaemic hyperosmolar nonketotic syndrome 62.09 16.15 22 18459 1697 64478554
Epididymitis 61.65 16.15 22 18459 1732 64478519
Urosepsis 57.65 16.15 49 18432 22045 64458206
Pyelonephritis 54.97 16.15 43 18438 17223 64463028
Pruritus genital 52.18 16.15 17 18464 1015 64479236
Toxicity to various agents 51.35 16.15 20 18461 363493 64116758
Thrombotic cerebral infarction 50.81 16.15 14 18467 468 64479783
Temperature perception test abnormal 48.16 16.15 8 18473 17 64480234
Bladder cancer 47.75 16.15 33 18448 10941 64469310
Drug ineffective 46.66 16.15 108 18373 840139 63640112
Genital infection female 45.60 16.15 9 18472 64 64480187
Blood pressure decreased 44.85 16.15 85 18396 86114 64394137
Thirst 44.55 16.15 35 18446 14102 64466149
Blood glucose abnormal 44.03 16.15 29 18452 8884 64471367
Left ventricular dysfunction 43.01 16.15 37 18444 16917 64463334
Acute myocardial infarction 42.96 16.15 74 18407 69644 64410607
Acquired phimosis 42.62 16.15 8 18473 42 64480209
Haematuria 42.37 16.15 68 18413 60403 64419848
Vulvovaginal pruritus 42.18 16.15 17 18464 1869 64478382
Genital infection 41.16 16.15 8 18473 52 64480199
Dysuria 40.60 16.15 55 18426 42002 64438249
Mitral valve thickening 39.30 16.15 11 18470 390 64479861
Acetonaemia 38.59 16.15 10 18471 263 64479988
Pancreatitis acute 38.30 16.15 54 18427 42801 64437450
Congenital hydrocephalus 37.92 16.15 7 18474 33 64480218
Suspected COVID-19 37.63 16.15 15 18466 1602 64478649
Glycosuria 37.29 16.15 16 18465 2058 64478193
Hypoglycaemic coma 37.10 16.15 20 18461 4254 64475997
Body mass index increased 34.51 16.15 14 18467 1565 64478686
Infusion related reaction 33.31 16.15 4 18477 164463 64315788
Pancreatitis 32.52 16.15 60 18421 59547 64420704
Neutropenia 32.48 16.15 14 18467 239610 64240641
N-terminal prohormone brain natriuretic peptide abnormal 29.67 16.15 8 18473 246 64480005
Pancreatic carcinoma 29.11 16.15 24 18457 10349 64469902
Perineal abscess 28.96 16.15 9 18472 461 64479790
Bladder trabeculation 28.76 16.15 6 18475 58 64480193
Mitral valve incompetence 28.70 16.15 36 18445 25502 64454749
Joint swelling 28.53 16.15 13 18468 215369 64264882
Microalbuminuria 27.23 16.15 10 18471 855 64479396
Brain stem infarction 26.14 16.15 12 18469 1811 64478440
Thrombocytopenia 25.98 16.15 16 18465 223785 64256466
Total cholesterol/HDL ratio increased 25.88 16.15 7 18474 218 64480033
Mitral valve calcification 25.86 16.15 11 18470 1385 64478866
Hypersensitivity 25.80 16.15 12 18469 196440 64283811
Diabetes mellitus 25.67 16.15 58 18423 66416 64413835
Disease progression 25.16 16.15 5 18476 141675 64338576
Drug abuse 24.96 16.15 4 18477 132370 64347881
Acidosis 24.80 16.15 28 18453 17767 64462484
Obesity 24.74 16.15 30 18451 20532 64459719
Peripartum cardiomyopathy 24.48 16.15 6 18475 125 64480126
Vomiting 24.41 16.15 253 18228 550864 63929387
Arthropathy 24.35 16.15 3 18478 120964 64359287
Shock 24.09 16.15 41 18440 38199 64442052
White blood cell count decreased 23.41 16.15 8 18473 157829 64322422
Hyperuricaemia 23.36 16.15 21 18460 10170 64470081
Pain 23.34 16.15 81 18400 553430 63926821
Treatment failure 23.26 16.15 3 18478 116813 64363438
Decreased vibratory sense 22.97 16.15 8 18473 586 64479665
Genital infection fungal 22.83 16.15 6 18475 167 64480084
Gangrene 22.76 16.15 18 18463 7320 64472931
Musculoskeletal stiffness 22.62 16.15 4 18477 123202 64357049
Immune-mediated hepatitis 22.59 16.15 12 18469 2477 64477774
Hyperkalaemia 22.56 16.15 72 18409 101057 64379194
Perineal pain 22.29 16.15 9 18472 994 64479257
Low density lipoprotein increased 21.91 16.15 18 18463 7722 64472529
Foot amputation 21.68 16.15 8 18473 693 64479558
Cardiac failure chronic 21.46 16.15 19 18462 9022 64471229
Urinary retention 21.35 16.15 45 18436 49156 64431095
Condition aggravated 21.27 16.15 47 18434 372379 64107872
Ejection fraction decreased 21.09 16.15 33 18448 28674 64451577
Hypertrophy 21.05 16.15 8 18473 752 64479499
Renal atrophy 20.91 16.15 10 18471 1654 64478597
Pyrexia 20.79 16.15 86 18395 558558 63921693
Hypernatraemia 20.17 16.15 21 18460 12168 64468083
High density lipoprotein decreased 19.88 16.15 13 18468 3933 64476318
Vaccination failure 19.82 16.15 8 18473 883 64479368
Urinary tract infection fungal 19.78 16.15 8 18473 887 64479364
COVID-19 pneumonia 19.72 16.15 24 18457 16480 64463771
Polydipsia 19.62 16.15 15 18466 5806 64474445
Polycythaemia 19.23 16.15 10 18471 1977 64478274
Renal impairment 19.10 16.15 83 18398 134934 64345317
Vulvovaginal candidiasis 18.58 16.15 10 18471 2120 64478131
Diabetic retinopathy 18.46 16.15 11 18470 2828 64477423
Pancytopenia 18.43 16.15 9 18472 143300 64336951
Febrile neutropenia 18.42 16.15 16 18465 187641 64292610
Heat illness 18.12 16.15 6 18475 377 64479874
Malignant neoplasm progression 18.03 16.15 5 18476 112866 64367385
Coronary artery stenosis 17.94 16.15 19 18462 11229 64469022
Bladder transitional cell carcinoma 17.74 16.15 10 18471 2320 64477931
Urine ketone body 17.60 16.15 5 18476 187 64480064
Depression 17.54 16.15 16 18465 183275 64296976
Food refusal 17.11 16.15 6 18475 449 64479802
Urine output increased 16.97 16.15 9 18472 1852 64478399
Aortic valve incompetence 16.88 16.15 16 18465 8285 64471966
Insulin C-peptide decreased 16.88 16.15 4 18477 72 64480179
Diabetic ketoacidotic hyperglycaemic coma 16.82 16.15 5 18476 220 64480031
Contraindicated product administered 16.81 16.15 5 18476 107824 64372427
Pneumonia 16.81 16.15 93 18388 559483 63920768
Pyelonephritis acute 16.80 16.15 13 18468 5121 64475130
Abnormal loss of weight 16.47 16.15 15 18466 7385 64472866
Candida infection 16.35 16.15 31 18450 31388 64448863

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A10BD15 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD21 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BD25 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BK01 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Sodium-glucose co-transporter 2 (SGLT2) inhibitors
MeSH PA D007004 Hypoglycemic Agents
MeSH PA D000077203 Sodium-Glucose Transporter 2 Inhibitors
FDA MoA N0000187058 Sodium-Glucose Transporter 2 Inhibitors
FDA EPC N0000187059 Sodium-Glucose Cotransporter 2 Inhibitor
CHEBI has role CHEBI:35526 antidiabetic
CHEBI has role CHEBI:73273 sodium-glucose transport protein subtype 2 inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Diabetes mellitus type 1 indication 46635009 DOID:9744
Chronic heart failure indication 48447003
Chronic kidney disease indication 709044004




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.62 acidic
pKa2 13.26 acidic
pKa3 13.7 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL RE44186 July 31, 2023 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9238076 April 15, 2024 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 9238076 April 15, 2024 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8431685 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8461105 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8431685 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8461105 April 13, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 7456254 June 30, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 7456254 June 30, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 6515117 Oct. 4, 2025 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING FASTING PLASMA GLUCOSE IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING HBA1C IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8906851 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING FASTING PLASMA GLUCOSE IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 REDUCING HBA1C IN A HUMAN IN NEED THEREOF IN COMBINATION WITH A SUSTAINED-RELEASE COMPOSITION CONTAINING EXENDIN-4
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8329648 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8906851 Aug. 18, 2026 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8501698 June 20, 2027 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO ARE ALREADY TREATED WITH DAPAGLIFLOZIN AND SAXAGLIPTIN
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8501698 June 20, 2027 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO HAVE INADEQUATE CONTROL WITH DAPAGLIFLOZIN
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
2.5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL 8501698 June 20, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS IN COMBINATION WITH EXENATIDE
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8361972 March 21, 2028 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO ARE ALREADY TREATED WITH DAPAGLIFLOZIN AND SAXAGLIPTIN
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8361972 March 21, 2028 METHOD FOR TREATING TYPE 2 DIABETES MELLITUS (T2DM) IN PATIENTS WHO HAVE INADEQUATE CONTROL WITH DAPAGLIFLOZIN
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL 8361972 March 21, 2028 TREATMENT OF TYPE 2 DIABETES MELLITUS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
10MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
10MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
2.5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
5MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL 8685934 May 26, 2030 TREATMENT OF TYPE 2 DIABETES MELLITUS IN A PATIENT, WHEREIN GLYCEMIC CONTROL (HBA1C < 7.0%) IS NOT ACHIEVABLE USING ONE OR MORE OF INSULIN, METFORMIN, PIOGLITAZONE, OR ROSIGLITAZONE
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL 10973836 March 9, 2040 REDUCTION OF THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH HEART FAILURE WITH REDUCED EJECTION FRACTION AND WITHOUT TYPE II DIABETES

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Feb. 22, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO REFLECT THAT NO DOSE ADJUSTMENT IS NEEDED FOR PATIENTS WITH AN ESTIMATED GLOMERULAR FILTRATION RATE (EGFR) OF 45 ML/MIN/1.73 M2 OR GREATER AS SUPPORTED BY CLINICAL STUDY REPORT
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Feb. 22, 2022 INFORMATION ADDED TO THE PRESCRIBING INFORMATION TO REFLECT THAT NO DOSE ADJUSTMENT IS NEEDED FOR PATIENTS WITH AN ESTIMATED GLOMERULAR FILTRATION RATE (EGFR) OF 45 ML/MIN/1.73 M2 OR GREATER AS SUPPORTED BY CLINICAL STUDY REPORT
10MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 Feb. 27, 2017 RX TABLET ORAL May 2, 2022 EXPANDED INDICATION FOR USE AS AN ADJUNCT TO DIET AND EXERCISE TO IMPROVE GLYCEMIC CONTROL IN ADULTS WITH TYPE 2 DIABETES MELLITUS
5MG;EQ 5MG BASE QTERN ASTRAZENECA AB N209091 May 2, 2019 RX TABLET ORAL May 2, 2022 NEW STRENGTH
10MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT
2.5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT
5MG;1GM;EQ 2.5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT
5MG;1GM;EQ 5MG BASE QTERNMET XR ASTRAZENECA AB N210874 May 2, 2019 DISCN TABLET, EXTENDED RELEASE ORAL May 2, 2022 NEW PRODUCT
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
10MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
10MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
2.5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 July 28, 2017 RX TABLET, EXTENDED RELEASE ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
5MG;1GM XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
5MG;500MG XIGDUO XR ASTRAZENECA AB N205649 Oct. 29, 2014 RX TABLET, EXTENDED RELEASE ORAL Oct. 18, 2022 TO REDUCE THE RISK OF HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH TYPE 2 DIABETES MELLITUS AND ESTABLISHED CARDIOVASCULAR DISEASE OR MULTIPLE CARDIOVASCULAR RISK FACTORS
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL May 5, 2023 TO REDUCE THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH HEART FAILURE (NYHA CLASS II-IV) WITH REDUCED EJECTION FRACTION
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL May 5, 2023 TO REDUCE THE RISK OF CARDIOVASCULAR DEATH AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH HEART FAILURE (NYHA CLASS II-IV) WITH REDUCED EJECTION FRACTION
10MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL April 30, 2024 TO REDUCE THE RISK OF SUSTAINED EGFR DECLINE, END-STAGE KIDNEY DISEASE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH CHRONIC KIDNEY DISEASE AT RISK OF PROGRESSION
5MG FARXIGA ASTRAZENECA AB N202293 Jan. 8, 2014 RX TABLET ORAL April 30, 2024 TO REDUCE THE RISK OF SUSTAINED EGFR DECLINE, END-STAGE KIDNEY DISEASE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN ADULTS WITH CHRONIC KIDNEY DISEASE AT RISK OF PROGRESSION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium/glucose cotransporter 2 Transporter INHIBITOR IC50 9.30 IUPHAR IUPHAR
Sodium/glucose cotransporter 1 Transporter IC50 8.49 CHEMBL
Sodium/myo-inositol cotransporter 2 Transporter IC50 6.42 CHEMBL
Low affinity sodium-glucose cotransporter Transporter IC50 8.87 CHEMBL
Sodium/glucose cotransporter 2 Transporter EC50 8.52 CHEMBL

External reference:

IDSource
D08897 KEGG_DRUG
960404-48-2 SECONDARY_CAS_RN
4033035 VANDF
CHEBI:85078 CHEBI
CHEMBL429910 ChEMBL_ID
CHEMBL2103802 ChEMBL_ID
C529054 MESH_SUPPLEMENTAL_RECORD_UI
4594 IUPHAR_LIGAND_ID
8886 INN_ID
DB06292 DRUGBANK_ID
1ULL0QJ8UC UNII
9887712 PUBCHEM_CID
1486966 RXNORM
210769 MMSL
28989 MMSL
29986 MMSL
d07928 MMSL
014949 NDDF
014950 NDDF
703674001 SNOMEDCT_US
703675000 SNOMEDCT_US
703678003 SNOMEDCT_US
783086004 SNOMEDCT_US
C2353951 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 0310-6205 TABLET, FILM COATED 5 mg ORAL NDA 27 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 0310-6210 TABLET, FILM COATED 10 mg ORAL NDA 27 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6225 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6225 TABLET, FILM COATED, EXTENDED RELEASE 2.50 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6250 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6250 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6260 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6260 TABLET, FILM COATED, EXTENDED RELEASE 5 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6270 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6270 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6280 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 30 sections
XIGDUOXR HUMAN PRESCRIPTION DRUG LABEL 2 0310-6280 TABLET, FILM COATED, EXTENDED RELEASE 10 mg ORAL NDA 30 sections
QTERN HUMAN PRESCRIPTION DRUG LABEL 2 0310-6770 TABLET, FILM COATED 5 mg ORAL NDA 28 sections
QTERN HUMAN PRESCRIPTION DRUG LABEL 2 0310-6770 TABLET, FILM COATED 5 mg ORAL NDA 28 sections
QTERN HUMAN PRESCRIPTION DRUG LABEL 2 0310-6780 TABLET, FILM COATED 10 mg ORAL NDA 28 sections
QTERN HUMAN PRESCRIPTION DRUG LABEL 2 0310-6780 TABLET, FILM COATED 10 mg ORAL NDA 28 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 50090-3481 TABLET, FILM COATED 10 mg ORAL NDA 27 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 50090-3482 TABLET, FILM COATED 5 mg ORAL NDA 27 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 55154-6932 TABLET, FILM COATED 5 mg ORAL NDA 27 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 55154-6932 TABLET, FILM COATED 5 mg ORAL NDA 27 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 55154-6933 TABLET, FILM COATED 10 mg ORAL NDA 27 sections
FARXIGA HUMAN PRESCRIPTION DRUG LABEL 1 55154-6933 TABLET, FILM COATED 10 mg ORAL NDA 27 sections