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

Stem definitionDrug idCAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives 4758 842133-18-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • invokana
  • canagliflozin hemihydrate
  • canagliflozin anhydrous
  • canagliflozin
  • canagliflozin hydrate
A glucoside-derived SODIUM-GLUCOSE TRANSPORTER 2 inhibitor that stimulates urinary excretion of glucose by suppressing renal glucose reabsorption. It is used to manage BLOOD GLUCOSE levels in patients with TYPE 2 DIABETES.
  • Molecular weight: 444.52
  • Formula: C24H25FO5S
  • CLOGP: 4.55
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 4
  • TPSA: 90.15
  • ALOGS: -5
  • ROTB: 5
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.20 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.19 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.74 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 10.30 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 0.00 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 3.214 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 3.681 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 46.132 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.305 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 1.180 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 2.680 % High 1
herg hERG pIC50 4.914 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 5.224 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.920 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 1.070 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MAP2K6,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PIM2,PRKDC,TEK,TGFBR1,ZAP70 28
kinase-selectivity-class AXL,GRK2,MAP2K6 3
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 12.218 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 18.923 High 1
mh-clint Mouse hepatocyte intrinsic clearance 11.402 High 1
mppb Mouse plasma protein binding (% unbound) 1.330 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 51.642 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 2.410 % High 1
rat-kpuu-brain Rat brain Kpuu 0.014 % High 1
rh-clint Rat hepatocyte intrinsic clearance 10.864 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 16.890 % High 1
rppb Rat plasma protein binding (% unbound) 0.720 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 16.293 uM High 1

Approvals:

DateAgencyCompanyOrphan
July 4, 2014 PMDA MITSUBISHI TANABE PHARMA CORPORATION
March 29, 2013 FDA JANSSEN PHARMS
Nov. 15, 2013 EMA JANSSEN-CILAG INTERNATIONAL NV

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 3458.45 19.73 800 14161 23607 90589879
Fungal infection 2234.89 19.73 633 14328 42028 90571458
Genital infection fungal 778.72 19.73 111 14850 112 90613374
Ketoacidosis 605.00 19.73 148 14813 5447 90608039
Euglycaemic diabetic ketoacidosis 579.92 19.73 146 14815 6055 90607431
Urinary tract infection 437.31 19.73 378 14583 305254 90308232
Full blood count abnormal 272.44 19.73 129 14832 36468 90577018
Toe amputation 260.96 19.73 62 14899 2007 90611479
Glycosylated haemoglobin increased 236.46 19.73 91 14870 15471 90598015
Malignant mediastinal neoplasm 181.77 19.73 43 14918 1365 90612121
Blood glucose increased 173.63 19.73 136 14825 95110 90518376
Hyperglycaemia 171.29 19.73 106 14855 50864 90562622
Urine ketone body present 161.03 19.73 44 14917 2508 90610978
Vulvovaginal mycotic infection 152.44 19.73 52 14909 6262 90607224
Glomerular filtration rate decreased 151.97 19.73 68 14893 16864 90596622
Dehydration 141.12 19.73 167 14794 194280 90419206
Diabetic foot infection 135.13 19.73 25 14936 226 90613260
Blood immunoglobulin E increased 133.03 19.73 43 14918 4382 90609104
Asthma 126.96 19.73 177 14784 241983 90371503
Weight decreased 126.04 19.73 225 14736 379685 90233801
Metabolic acidosis 122.47 19.73 89 14872 55587 90557899
Pancreatitis 106.69 19.73 90 14871 69736 90543750
Gangrene 100.71 19.73 47 14914 12829 90600657
Urine output increased 100.20 19.73 28 14933 1734 90611752
Pollakiuria 82.36 19.73 57 14904 32948 90580538
Myopathy toxic 80.55 19.73 19 14942 595 90612891
Hypoglycaemia 78.99 19.73 76 14885 69772 90543714
Osteomyelitis 76.40 19.73 51 14910 27795 90585691
Vulvovaginal pruritus 73.92 19.73 27 14934 3966 90609520
Pyelonephritis 73.26 19.73 45 14916 21271 90592215
Foot amputation 69.15 19.73 15 14946 319 90613167
Bronchiectasis 66.37 19.73 43 14918 22287 90591199
Ketosis 65.53 19.73 17 14944 792 90612694
Urosepsis 63.39 19.73 41 14920 21191 90592295
Leg amputation 59.36 19.73 20 14941 2317 90611169
Acute kidney injury 58.53 19.73 149 14812 320238 90293248
Vaginal infection 57.43 19.73 28 14933 8412 90605074
Acidosis 57.26 19.73 32 14929 12704 90600782
Gastrooesophageal reflux disease 55.59 19.73 99 14862 166238 90447248
Incorrect dose administered 54.20 19.73 66 14895 78864 90534622
Necrotising fasciitis 52.95 19.73 21 14940 3859 90609627
Polyuria 50.03 19.73 27 14934 10013 90603473
Diabetic foot 49.63 19.73 16 14945 1615 90611871
Blood ketone body increased 46.46 19.73 11 14950 350 90613136
Arthropathy 45.70 19.73 4 14957 366238 90247248
Treatment noncompliance 43.47 19.73 48 14913 51679 90561807
Maternal exposure during pregnancy 42.16 19.73 5 14956 360058 90253428
Contraindicated product administered 41.33 19.73 3 14958 320136 90293350
Limb amputation 40.95 19.73 7 14954 38 90613448
Amputation 39.02 19.73 9 14952 255 90613231
Blood glucose decreased 37.41 19.73 31 14930 23398 90590088
Vulvovaginal candidiasis 36.06 19.73 16 14945 3884 90609602
Wound 35.98 19.73 4 14957 302976 90310510
Vascular access site haemorrhage 35.88 19.73 8 14953 194 90613292
Nasal congestion 34.99 19.73 55 14906 83359 90530127
General physical health deterioration 34.78 19.73 8 14953 355107 90258379
Infusion related reaction 34.25 19.73 13 14948 416767 90196719
Drug intolerance 33.52 19.73 16 14945 447575 90165911
Pain 33.29 19.73 72 14889 996269 89617217
Low density lipoprotein increased 32.80 19.73 19 14942 8066 90605420
Hypoacusis 32.78 19.73 31 14930 27819 90585667
Dizziness 32.76 19.73 187 14774 589097 90024389
Vascular stenosis 32.69 19.73 9 14952 527 90612959
Intercepted medication error 32.28 19.73 10 14951 887 90612599
Glucose urine present 31.99 19.73 10 14951 914 90612572
Joint swelling 31.98 19.73 22 14939 503278 90110208
Glycosuria 31.41 19.73 11 14950 1431 90612055
Rhinorrhoea 31.34 19.73 54 14907 88262 90525224
Hyperkalaemia 30.30 19.73 45 14916 64919 90548567
Flank pain 29.79 19.73 25 14936 19197 90594289
Gastroenteritis 29.67 19.73 30 14931 29199 90584287
Lactic acidosis 29.56 19.73 39 14922 50424 90563062
Stomatitis 29.38 19.73 5 14956 274693 90338793
Abdominal discomfort 28.84 19.73 22 14939 477306 90136180
Haematuria 28.62 19.73 32 14929 34905 90578581
Fungal skin infection 28.50 19.73 15 14946 5286 90608200
Cerebral fungal infection 28.21 19.73 7 14954 272 90613214
Impaired healing 28.04 19.73 3 14958 234196 90379290
Osteomyelitis acute 27.46 19.73 7 14954 304 90613182
Helicobacter infection 26.92 19.73 3 14958 226847 90386639
Hepatic enzyme increased 26.84 19.73 13 14948 360723 90252763
Genital rash 26.57 19.73 8 14953 645 90612841
Diabetes mellitus inadequate control 26.31 19.73 23 14938 18661 90594825
Rhabdomyolysis 26.08 19.73 37 14924 51219 90562267
Vulvovaginitis 25.68 19.73 7 14954 395 90613091
Condition aggravated 25.28 19.73 37 14924 595508 90017978
Pyrexia 25.25 19.73 44 14917 660441 89953045
Ketonuria 25.16 19.73 8 14953 773 90612713
Diabetes mellitus 24.78 19.73 41 14920 64834 90548652
Cerebral infarction 24.65 19.73 26 14935 26570 90586916
Hemianopia homonymous 24.35 19.73 8 14953 857 90612629
Neutropenia 24.25 19.73 4 14957 224900 90388586
Haemorrhagic erosive gastritis 24.18 19.73 7 14954 492 90612994
Irritable bowel syndrome 23.97 19.73 3 14958 207445 90406041
Cystitis 23.94 19.73 41 14920 66677 90546809
Micturition disorder 23.54 19.73 11 14950 3009 90610477
Anion gap increased 23.22 19.73 10 14951 2260 90611226
Thirst 22.82 19.73 20 14941 16275 90597211
Dysuria 22.39 19.73 30 14931 39371 90574115
Renal abscess 22.32 19.73 8 14953 1113 90612373
Type 2 diabetes mellitus 22.27 19.73 79 14882 203165 90410321
Exposure during pregnancy 22.11 19.73 6 14955 238404 90375082
Urine ketone body 22.02 19.73 5 14956 132 90613354
Discomfort 21.79 19.73 9 14952 274326 90339160
Musculoskeletal stiffness 21.58 19.73 11 14950 296521 90316965
Diabetic ulcer 20.94 19.73 5 14956 165 90613321
Swelling 20.92 19.73 23 14938 419035 90194451
Alopecia 20.76 19.73 31 14930 495040 90118446
Hyperglycaemic hyperosmolar nonketotic syndrome 20.76 19.73 8 14953 1361 90612125
Therapeutic product effect decreased 20.64 19.73 10 14951 277561 90335925
Insomnia 20.60 19.73 15 14946 333459 90280027
Genital infection 20.29 19.73 5 14956 189 90613297
Thrombocytopenia 19.83 19.73 5 14956 208720 90404766

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 2195.80 19.98 640 14370 21727 42584598
Toe amputation 694.69 19.98 169 14841 2760 42603565
Genital infection fungal 548.16 19.98 91 14919 140 42606185
Fungal infection 500.57 19.98 206 14804 19516 42586809
Euglycaemic diabetic ketoacidosis 382.41 19.98 122 14888 5538 42600787
Ketoacidosis 339.61 19.98 110 14900 5242 42601083
Diabetic foot infection 326.98 19.98 71 14939 675 42605650
Osteomyelitis 301.67 19.98 141 14869 18082 42588243
Balanoposthitis 286.74 19.98 74 14936 1547 42604778
Leg amputation 251.47 19.98 74 14936 2549 42603776
Glycosylated haemoglobin increased 223.16 19.98 103 14907 12821 42593504
Gangrene 213.98 19.98 77 14933 5049 42601276
Urine output increased 206.68 19.98 56 14954 1420 42604905
Foot amputation 185.60 19.98 46 14964 811 42605514
Glomerular filtration rate decreased 177.33 19.98 95 14915 16256 42590069
Diabetic foot 150.53 19.98 52 14958 3021 42603304
Pollakiuria 141.72 19.98 92 14918 22413 42583912
Weight decreased 136.23 19.98 254 14756 207694 42398631
Osteomyelitis acute 134.95 19.98 29 14981 261 42606064
Limb amputation 134.12 19.98 24 14986 70 42606255
Urine ketone body present 132.17 19.98 39 14971 1355 42604970
Dehydration 122.69 19.98 196 14814 141571 42464754
Blood glucose increased 120.64 19.98 139 14871 73560 42532765
Pancreatitis 117.07 19.98 107 14903 43161 42563164
Metabolic acidosis 117.03 19.98 116 14894 51742 42554583
Urinary tract infection 115.78 19.98 158 14852 99126 42507199
Amputation 109.33 19.98 30 14980 798 42605527
Skin injury 96.59 19.98 36 14974 2605 42603720
Skin ulcer 76.51 19.98 67 14943 25534 42580791
Ketosis 75.75 19.98 23 14987 882 42605443
Hepatic fibrosis 75.33 19.98 36 14974 4836 42601489
Necrotising oesophagitis 74.16 19.98 23 14987 948 42605377
Ketonuria 73.70 19.98 21 14989 643 42605682
Bone cyst 73.41 19.98 26 14984 1625 42604700
Joint ankylosis 73.02 19.98 26 14984 1651 42604674
Localised infection 70.47 19.98 58 14952 20315 42586010
Anti-cyclic citrullinated peptide antibody positive 69.69 19.98 26 14984 1886 42604439
Hypoglycaemia 67.79 19.98 94 14916 59760 42546565
Prostatitis 61.32 19.98 34 14976 6214 42600111
Blood ketone body increased 59.64 19.98 17 14993 521 42605804
Osteolysis 53.97 19.98 26 14984 3554 42602771
Anaemia 53.82 19.98 16 14994 280262 42326063
Febrile neutropenia 53.28 19.98 3 15007 185700 42420625
Cerebral infarction 52.97 19.98 60 14950 31109 42575216
Hand deformity 52.70 19.98 26 14984 3742 42602583
Lactic acidosis 52.61 19.98 72 14938 45189 42561136
Red blood cell sedimentation rate abnormal 52.26 19.98 26 14984 3810 42602515
Gas gangrene 52.12 19.98 11 14999 90 42606235
Hyperkalaemia 52.10 19.98 98 14912 80360 42525965
Alanine aminotransferase abnormal 51.54 19.98 28 14982 4916 42601409
Bone erosion 48.88 19.98 26 14984 4377 42601948
Gastrointestinal infection 48.49 19.98 30 14980 6713 42599612
Glucose urine present 47.57 19.98 18 14992 1357 42604968
Cellulitis 46.22 19.98 80 14930 61505 42544820
Acute kidney injury 45.90 19.98 252 14758 367085 42239240
Neutropenia 44.98 19.98 8 15002 199423 42406902
Thrombocytopenia 44.32 19.98 7 15003 190272 42416053
Hepatic cirrhosis 44.26 19.98 44 14966 19658 42586667
Thirst 42.56 19.98 31 14979 9077 42597248
Adverse event 41.00 19.98 46 14964 23594 42582731
Genital infection 40.97 19.98 8 15002 42 42606283
Polyuria 39.94 19.98 31 14979 9980 42596345
Toxicity to various agents 38.95 19.98 16 14994 229120 42377205
C-reactive protein abnormal 37.65 19.98 29 14981 9232 42597093
Diabetes mellitus inadequate control 35.73 19.98 35 14975 15355 42590970
Neuropathic arthropathy 34.73 19.98 9 15001 191 42606134
Osteomyelitis chronic 33.89 19.98 10 15000 347 42605978
Renal pain 33.58 19.98 19 14991 3608 42602717
Blood ketone body 33.42 19.98 8 15002 121 42606204
Treatment noncompliance 32.35 19.98 52 14958 37620 42568705
Asthma-chronic obstructive pulmonary disease overlap syndrome 31.90 19.98 14 14996 1545 42604780
Blood creatinine increased 31.81 19.98 98 14912 109905 42496420
Product prescribing error 31.03 19.98 42 14968 26070 42580255
Diabetic ulcer 30.74 19.98 7 15003 84 42606241
Pancytopenia 30.64 19.98 3 15007 117740 42488585
Dysuria 29.59 19.98 45 14965 31051 42575274
Pyrexia 29.52 19.98 59 14951 393983 42212342
Urinary tract infection fungal 29.10 19.98 10 15000 571 42605754
Phimosis 28.87 19.98 12 14998 1159 42605166
Incorrect dose administered 28.80 19.98 60 14950 52914 42553411
Multiple allergies 27.86 19.98 17 14993 3711 42602614
Acetonaemia 27.83 19.98 8 15002 253 42606072
Dizziness 27.75 19.98 166 14844 249088 42357237
Product use issue 27.63 19.98 74 14936 76677 42529648
Glycosylated haemoglobin decreased 27.58 19.98 9 15001 438 42605887
Mycobacterial infection 27.50 19.98 15 14995 2653 42603672
Therapeutic response increased 27.38 19.98 8 15002 268 42606057
General physical health deterioration 26.60 19.98 10 15000 151236 42455089
Abdominal discomfort 26.53 19.98 72 14938 75183 42531142
Psoriatic arthropathy 26.44 19.98 38 14972 24929 42581396
Haemoglobin decreased 26.43 19.98 7 15003 132464 42473861
Condition aggravated 26.22 19.98 32 14978 260722 42345603
Micturition disorder 25.72 19.98 14 14996 2466 42603859
Peripheral ischaemia 25.69 19.98 20 14990 6465 42599860
Acidosis 24.98 19.98 26 14984 12253 42594072
Diabetes mellitus 24.80 19.98 61 14949 60026 42546299
Hepatic steatosis 24.73 19.98 34 14976 21414 42584911
Death 24.30 19.98 85 14925 471100 42135225
Penile infection 24.03 19.98 6 15004 109 42606216
Extremity necrosis 23.80 19.98 13 14997 2306 42604019
Somnolence 23.71 19.98 10 15000 141095 42465230
Diabetic gangrene 23.42 19.98 7 15003 254 42606071
Malignant neoplasm progression 23.05 19.98 5 15005 108395 42497930
Disease progression 22.86 19.98 11 14999 143645 42462680
Necrotising fasciitis 22.44 19.98 16 14994 4530 42601795
Urine ketone body 22.27 19.98 5 15005 56 42606269
Anion gap increased 22.22 19.98 12 14998 2082 42604243
Genital rash 22.12 19.98 9 15001 823 42605502
Pneumonia 21.85 19.98 76 14934 422073 42184252
Drug interaction 21.71 19.98 38 14972 266961 42339364
Microalbuminuria 21.69 19.98 9 15001 865 42605460
Penile burning sensation 21.58 19.98 4 15006 15 42606310
Blood triglycerides increased 21.10 19.98 27 14983 15869 42590456
Flank pain 21.00 19.98 19 14991 7544 42598781
Penile adhesion 20.86 19.98 3 15007 0 42606325
Cellulitis of male external genital organ 20.80 19.98 5 15005 77 42606248
Polydipsia 20.34 19.98 15 14995 4473 42601852
Nausea 20.26 19.98 221 14789 396578 42209747
Blood lactic acid increased 20.01 19.98 19 14991 8020 42598305

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 4484.61 15.63 1154 22507 40904 110524734
Euglycaemic diabetic ketoacidosis 966.81 15.63 263 23398 11360 110554278
Toe amputation 838.80 15.63 193 23468 4145 110561493
Ketoacidosis 791.27 15.63 218 23443 9869 110555769
Fungal infection 571.24 15.63 258 23403 50548 110515090
Diabetic foot infection 471.39 15.63 91 23570 793 110564845
Genital infection fungal 420.57 15.63 69 23592 199 110565439
Osteomyelitis 373.99 15.63 174 23487 36426 110529212
Gangrene 297.50 15.63 117 23544 16224 110549414
Leg amputation 284.30 15.63 81 23580 4137 110561501
Glycosylated haemoglobin increased 259.10 15.63 118 23543 23501 110542137
Urine ketone body present 255.37 15.63 73 23588 3773 110561865
Metabolic acidosis 245.17 15.63 189 23472 99555 110466083
Foot amputation 233.07 15.63 53 23608 1075 110564563
Diabetic foot 203.04 15.63 62 23599 4033 110561605
Full blood count abnormal 192.11 15.63 130 23531 55922 110509716
Blood glucose increased 187.14 15.63 183 23478 132313 110433325
Urinary tract infection 176.89 15.63 278 23383 326004 110239634
Malignant mediastinal neoplasm 166.61 15.63 42 23619 1336 110564302
Hyperglycaemia 166.16 15.63 141 23520 84949 110480689
Pancreatitis 164.49 15.63 146 23515 93387 110472251
Dehydration 163.88 15.63 247 23414 279264 110286374
Osteomyelitis acute 160.02 15.63 35 23626 590 110565048
Glomerular filtration rate decreased 146.56 15.63 86 23575 28870 110536768
Acute kidney injury 129.56 15.63 362 23299 635068 109930570
Limb amputation 128.88 15.63 23 23638 123 110565515
Ketosis 128.69 15.63 36 23625 1718 110563920
Weight decreased 118.19 15.63 289 23372 467768 110097870
Blood ketone body increased 107.03 15.63 27 23634 861 110564777
Hypoglycaemia 102.03 15.63 125 23536 115979 110449659
Cerebral infarction 99.31 15.63 85 23576 51753 110513885
Blood immunoglobulin E increased 96.86 15.63 42 23619 7440 110558198
Asthma 90.89 15.63 179 23482 250112 110315526
Amputation 90.75 15.63 24 23637 925 110564713
Lactic acidosis 89.88 15.63 105 23556 92706 110472932
Pollakiuria 89.86 15.63 75 23586 44120 110521518
Ketonuria 89.73 15.63 26 23635 1409 110564229
Urine output increased 88.17 15.63 30 23631 2756 110562882
Skin ulcer 77.15 15.63 81 23580 63564 110502074
Joint ankylosis 75.56 15.63 26 23635 2471 110563167
Necrotising oesophagitis 74.13 15.63 23 23638 1577 110564061
Balanoposthitis 73.21 15.63 22 23639 1354 110564284
Polyuria 70.11 15.63 45 23616 17693 110547945
Cellulitis 68.97 15.63 108 23553 125908 110439730
Acidosis 67.18 15.63 48 23613 22483 110543155
Bone cyst 66.26 15.63 26 23635 3577 110562061
Bronchiectasis 66.17 15.63 58 23603 36435 110529203
Localised infection 65.49 15.63 62 23599 42986 110522652
Hyperkalaemia 64.31 15.63 109 23552 135687 110429951
Skin injury 63.74 15.63 26 23635 3956 110561682
Diabetes mellitus 62.67 15.63 91 23570 99290 110466348
Necrotising fasciitis 62.06 15.63 31 23630 7560 110558078
Diabetes mellitus inadequate control 61.50 15.63 51 23610 29724 110535914
Pyelonephritis 60.12 15.63 47 23614 25203 110540435
Gas gangrene 59.39 15.63 14 23647 334 110565304
Myopathy toxic 57.01 15.63 18 23643 1307 110564331
Prostatitis 55.84 15.63 25 23636 4776 110560862
Osteolysis 55.57 15.63 26 23635 5497 110560141
General physical health deterioration 52.83 15.63 13 23648 425282 110140356
Blood ketone body 50.42 15.63 11 23650 183 110565455
Urosepsis 50.17 15.63 46 23615 30629 110535009
Vulvovaginal mycotic infection 50.07 15.63 24 23637 5353 110560285
Febrile neutropenia 49.82 15.63 5 23656 316762 110248876
Alanine aminotransferase abnormal 47.95 15.63 28 23633 9306 110556332
Incorrect dose administered 47.49 15.63 82 23579 103559 110462079
Thrombocytopenia 46.70 15.63 9 23652 348876 110216762
Hepatic fibrosis 46.26 15.63 26 23635 8040 110557598
Neutropenia 45.46 15.63 12 23649 374608 110191030
Anion gap increased 45.41 15.63 21 23640 4323 110561315
Treatment noncompliance 44.80 15.63 66 23595 72924 110492714
Infusion related reaction 44.78 15.63 13 23648 381149 110184489
Urine ketone body 44.69 15.63 10 23651 188 110565450
Gastrooesophageal reflux disease 44.08 15.63 110 23551 179866 110385772
Acetonaemia 43.30 15.63 12 23649 553 110565085
Diabetic ulcer 43.24 15.63 10 23651 219 110565419
Gastrointestinal infection 42.13 15.63 30 23631 13975 110551663
Glucose urine present 40.28 15.63 16 23645 2273 110563365
Condition aggravated 39.62 15.63 60 23601 734776 109830862
Osteomyelitis chronic 39.22 15.63 12 23649 785 110564853
Anaemia 38.74 15.63 36 23625 547050 110018588
Flank pain 38.44 15.63 35 23626 23095 110542543
Pancreatitis acute 37.71 15.63 55 23606 60219 110505419
Maternal exposure during pregnancy 37.64 15.63 5 23656 254878 110310760
Diabetic ketosis 37.32 15.63 12 23649 924 110564714
Glossodynia 36.25 15.63 3 23658 222001 110343637
Pyrexia 35.68 15.63 88 23573 898177 109667461
Glycosuria 34.81 15.63 15 23646 2615 110563023
Stomatitis 34.05 15.63 8 23653 270234 110295404
Peripheral ischaemia 33.98 15.63 24 23637 11034 110554604
Blood triglycerides increased 33.63 15.63 33 23628 23893 110541745
Contraindicated product administered 31.98 15.63 7 23654 248260 110317378
Pancreatic carcinoma 31.81 15.63 26 23635 14846 110550792
Vascular access site haemorrhage 31.78 15.63 8 23653 253 110565385
Blood bicarbonate decreased 31.40 15.63 18 23643 5779 110559859
Overdose 31.34 15.63 6 23655 233788 110331850
Gastroenteritis 31.22 15.63 40 23621 38760 110526878
Pancytopenia 31.22 15.63 4 23657 209609 110356029
Vascular stenosis 31.13 15.63 10 23651 768 110564870
Neuropathic arthropathy 29.88 15.63 9 23652 558 110565080
Urinary tract infection fungal 29.78 15.63 11 23650 1284 110564354
Hepatic steatosis 29.74 15.63 44 23617 48787 110516851
Blood glucose decreased 29.59 15.63 34 23627 29454 110536184
Alopecia 28.25 15.63 22 23639 364731 110200907
Dry gangrene 28.06 15.63 10 23651 1054 110564584
Diabetic gangrene 27.43 15.63 7 23654 234 110565404
Mycobacterial infection 27.42 15.63 15 23646 4402 110561236
Extremity necrosis 26.65 15.63 14 23647 3788 110561850
Genital rash 25.84 15.63 10 23651 1325 110564313
Wound 25.73 15.63 9 23652 234428 110331210
Vulvovaginal candidiasis 25.64 15.63 13 23648 3272 110562366
Product prescribing error 25.34 15.63 42 23619 51289 110514349
Blood creatinine increased 24.99 15.63 91 23570 182798 110382840
Renal pain 24.95 15.63 19 23642 9798 110555840
Swelling 24.95 15.63 23 23638 351018 110214620
Irritable bowel syndrome 24.78 15.63 3 23658 164212 110401426
Dysuria 24.18 15.63 45 23616 60186 110505452
Pemphigus 23.96 15.63 8 23653 214562 110351076
Penile infection 23.93 15.63 5 23656 67 110565571
Low density lipoprotein increased 23.56 15.63 19 23642 10647 110554991
Thirst 23.44 15.63 26 23635 21681 110543957
Ill-defined disorder 23.34 15.63 3 23658 156850 110408788
Hypoacusis 23.31 15.63 33 23628 35158 110530480
Intercepted medication error 23.16 15.63 9 23652 1207 110564431
Bladder cancer 23.12 15.63 25 23636 20267 110545371
Musculoskeletal toxicity 22.77 15.63 6 23655 228 110565410
Headache 22.34 15.63 105 23556 882272 109683366
Polydipsia 22.05 15.63 16 23645 7672 110557966
Somnolence 21.72 15.63 19 23642 297430 110268208
Post streptococcal glomerulonephritis 21.26 15.63 5 23656 118 110565520
Nephrolithiasis 21.20 15.63 45 23616 66167 110499471
Disease progression 21.17 15.63 13 23648 244021 110321617
Dizziness 21.01 15.63 235 23426 697958 109867680
Exposure during pregnancy 21.00 15.63 5 23656 167419 110398219
Nasal congestion 20.90 15.63 57 23604 98225 110467413
Injury 20.89 15.63 6 23655 177259 110388379
Red blood cell sedimentation rate abnormal 20.88 15.63 26 23635 24483 110541155
Haemoglobin decreased 20.55 15.63 14 23647 248713 110316925
Blood glucose abnormal 20.40 15.63 19 23642 12897 110552741
Renal impairment 20.28 15.63 87 23574 188358 110377280
Osteoarthritis 20.06 15.63 7 23654 182616 110383022
Asthma-chronic obstructive pulmonary disease overlap syndrome 20.03 15.63 14 23647 6330 110559308
Helicobacter infection 19.93 15.63 7 23654 181870 110383768
Cerebral fungal infection 19.92 15.63 7 23654 708 110564930
Vulvovaginal pruritus 19.82 15.63 11 23650 3320 110562318
Oedema peripheral 19.51 15.63 25 23636 328635 110237003
Hepatic enzyme increased 19.47 15.63 24 23637 320868 110244770
Haemorrhagic erosive gastritis 19.31 15.63 7 23654 775 110564863
Discomfort 19.24 15.63 11 23650 214696 110350942
Acute myocardial infarction 19.24 15.63 50 23611 83727 110481911
Type 2 diabetes mellitus 19.20 15.63 82 23579 177150 110388488
White blood cell count decreased 18.84 15.63 13 23648 229377 110336261
Phimosis 18.83 15.63 7 23654 832 110564806
Mobility decreased 18.78 15.63 14 23647 237408 110328230
Penile burning sensation 18.74 15.63 3 23658 7 110565631
Sepsis 18.69 15.63 127 23534 327219 110238419
Malignant neoplasm progression 18.65 15.63 7 23654 174560 110391078
Hypovolaemia 18.48 15.63 23 23638 21651 110543987
Necrosis 18.44 15.63 17 23644 11389 110554249
Hepatic cirrhosis 18.32 15.63 43 23618 67583 110498055
Toxicity to various agents 18.32 15.63 48 23613 480507 110085131
Hyperglycaemic hyperosmolar nonketotic syndrome 18.08 15.63 10 23651 2999 110562639
Genital infection 18.01 15.63 5 23656 232 110565406
Hemianopia homonymous 17.87 15.63 8 23653 1527 110564111
Hallucination, auditory 17.85 15.63 25 23636 26372 110539266
Renal abscess 17.77 15.63 8 23653 1548 110564090
Sudden hearing loss 17.77 15.63 9 23652 2260 110563378
Breast disorder 17.60 15.63 9 23652 2305 110563333
Drug intolerance 17.56 15.63 38 23623 406474 110159164
Peripheral arterial occlusive disease 17.32 15.63 15 23646 9265 110556373
Blood lactic acid increased 17.17 15.63 19 23642 15802 110549836
Product use in unapproved indication 16.81 15.63 45 23616 447332 110118306
Colon cancer 16.57 15.63 19 23642 16424 110549214
Sinusitis 16.17 15.63 24 23637 296664 110268974
Liver injury 16.12 15.63 6 23655 150407 110415231
Blood glucose normal 15.99 15.63 3 23658 22 110565616
Completed suicide 15.92 15.63 17 23644 242364 110323274
Spinal ligament ossification 15.88 15.63 3 23658 23 110565615
Albumin urine present 15.87 15.63 6 23655 747 110564891
Rhinorrhoea 15.67 15.63 53 23608 102613 110463025

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A10BD16 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BK02 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Sodium-glucose co-transporter 2 (SGLT2) inhibitors
MeSH PA D000077203 Sodium-Glucose Transporter 2 Inhibitors
MeSH PA D007004 Hypoglycemic Agents
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000187058 Sodium-Glucose Transporter 2 Inhibitors
FDA EPC N0000187059 Sodium-Glucose Cotransporter 2 Inhibitor
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:73273 sodium-glucose transport protein subtype 2 inhibitor

Related Drugs by ATC class:

A10BD Combinations of oral blood glucose lowering drugs 19 drugs
acarbosealogliptindapagliflozinempagliflozinertugliflozinevogliptingemigliptinglimepiridelinagliptinlobeglitazonemetforminphenformin show all 19 →
A10BK Sodium-glucose co-transporter 2 (SGLT2) inhibitors 7 drugs
bexagliflozindapagliflozinempagliflozinertugliflozinipragliflozinluseogliflozinsotagliflozin

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

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Chronic kidney disease (CKD) associated with type 2 diabetes (T2D) indication




🐶 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
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 8513202 Dec. 3, 2027 TREATMENT OF TYPE 2 DIABETES MELLITUS
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL 7943582 Feb. 26, 2029 TREATMENT OF TYPE 2 DIABETES MELLITUS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL Dec. 18, 2027 NEW PATIENT POPULATION
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL Dec. 18, 2027 NEW PATIENT POPULATION
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL Dec. 18, 2027 NEW PATIENT POPULATION
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL Dec. 18, 2027 NEW PATIENT POPULATION
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL Dec. 18, 2027 NEW PATIENT POPULATION
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL Dec. 18, 2027 NEW PATIENT POPULATION
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL Dec. 18, 2027 NEW PATIENT POPULATION
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL Dec. 18, 2027 NEW PATIENT POPULATION
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL Dec. 18, 2027 NEW PATIENT POPULATION
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL Dec. 18, 2027 NEW PATIENT POPULATION
100MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
300MG INVOKANA JANSSEN PHARMS N204042 March 29, 2013 RX TABLET ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
150MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
150MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
50MG;1GM INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
50MG;500MG INVOKAMET JANSSEN PHARMS N204353 Aug. 8, 2014 RX TABLET ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
150MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
150MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
50MG;1GM INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY
50MG;500MG INVOKAMET XR JANSSEN PHARMS N205879 Sept. 20, 2016 RX TABLET, EXTENDED RELEASE ORAL June 18, 2028 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Sodium/glucose cotransporter 2 Transporter INHIBITOR IC50 8.66 WOMBAT-PK CHEMBL
Sodium/glucose cotransporter 1 Transporter IC50 5.72 CHEMBL
Sodium/glucose cotransporter 2 Transporter IC50 8.63 CHEMBL
Protease Enzyme Ki 6.20 CHEMBL
Sodium/glucose cotransporter 2 Transporter IC50 8.70 CHEMBL

External reference:

IDSource
D09592 KEGG_DRUG
928672-86-0 SECONDARY_CAS_RN
4032289 VANDF
CHEBI:73272 CHEBI
L3R PDB_CHEM_ID
CHEMBL4594217 ChEMBL_ID
CHEMBL2048484 ChEMBL_ID
4582 IUPHAR_LIGAND_ID
DB08907 DRUGBANK_ID
0SAC974Z85 UNII
1373458 RXNORM
200558 MMSL
29373 MMSL
d08080 MMSL
014959 NDDF
1268978008 SNOMEDCT_US
703676004 SNOMEDCT_US
703681008 SNOMEDCT_US
725664009 SNOMEDCT_US
C2974540 UMLSCUI
D000068896 MESH_DESCRIPTOR_UI
9225 INN_ID
24812758 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
INVOKANA HUMAN PRESCRIPTION DRUG LABEL 1 50090-4364 TABLET, FILM COATED 300 mg ORAL NDA 29 sections
INVOKANA HUMAN PRESCRIPTION DRUG LABEL 1 50090-5034 TABLET, FILM COATED 100 mg ORAL NDA 29 sections
INVOKANA HUMAN PRESCRIPTION DRUG LABEL 1 50458-140 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
INVOKANA HUMAN PRESCRIPTION DRUG LABEL 1 50458-141 TABLET, FILM COATED 300 mg ORAL NDA 32 sections
INVOKAMET HUMAN PRESCRIPTION DRUG LABEL 2 50458-540 TABLET, FILM COATED 50 mg ORAL NDA 34 sections
INVOKAMET HUMAN PRESCRIPTION DRUG LABEL 2 50458-541 TABLET, FILM COATED 50 mg ORAL NDA 34 sections
INVOKAMET HUMAN PRESCRIPTION DRUG LABEL 2 50458-542 TABLET, FILM COATED 150 mg ORAL NDA 34 sections
INVOKAMET HUMAN PRESCRIPTION DRUG LABEL 2 50458-543 TABLET, FILM COATED 150 mg ORAL NDA 34 sections
INVOKAMET XR HUMAN PRESCRIPTION DRUG LABEL 2 50458-940 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 34 sections
INVOKAMET XR HUMAN PRESCRIPTION DRUG LABEL 2 50458-941 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 34 sections
INVOKAMET XR HUMAN PRESCRIPTION DRUG LABEL 2 50458-942 TABLET, FILM COATED, EXTENDED RELEASE 150 mg ORAL NDA 34 sections
INVOKAMET XR HUMAN PRESCRIPTION DRUG LABEL 2 50458-943 TABLET, FILM COATED, EXTENDED RELEASE 150 mg ORAL NDA 34 sections
INVOKANA HUMAN PRESCRIPTION DRUG LABEL 1 55154-1425 TABLET, FILM COATED 100 mg ORAL NDA 32 sections
INVOKANA HUMAN PRESCRIPTION DRUG LABEL 1 55154-1426 TABLET, FILM COATED 300 mg ORAL NDA 32 sections