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

Stem definitionDrug idCAS RN
dipeptidyl aminopeptidase-IV inhibitors 2448 486460-32-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • sitagliptin
  • sitagliptin phosphate
  • januvia
  • ristaben
  • sitagliptin phosphate hydrate
  • sitagliptin phosphate monohydrate
  • MK-0431
  • MK 0431
  • sitagliptin monophosphate monohydrate
  • sitagliptin phosphate anhydrous
A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.
  • Molecular weight: 407.32
  • Formula: C16H15F6N5O
  • CLOGP: 0.69
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 1
  • TPSA: 77.04
  • ALOGS: -4.08
  • ROTB: 5

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 78 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.35 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 87 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.80 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 6 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.62 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 12 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 20, 2007 EMA MERCK SHARP DOHME
Oct. 16, 2006 FDA MERCK SHARP DOHME

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
Blood glucose increased 953.56 10.81 769 59413 71244 46554636
Pancreatitis 598.36 10.81 476 59706 43151 46582729
Hypoglycaemia 582.04 10.81 514 59668 53835 46572045
Lactic acidosis 521.45 10.81 396 59786 33513 46592367
Pancreatic carcinoma 486.35 10.81 214 59968 6343 46619537
Diabetes mellitus inadequate control 455.26 10.81 256 59926 12958 46612922
Glycosylated haemoglobin increased 337.91 10.81 197 59985 10679 46615201
Diabetic ketoacidosis 305.10 10.81 224 59958 17986 46607894
Pancreatic carcinoma metastatic 289.23 10.81 111 60071 2297 46623583
Acute kidney injury 250.44 10.81 769 59413 235086 46390794
Pemphigoid 203.44 10.81 113 60069 5578 46620302
Blood glucose abnormal 189.31 10.81 114 60068 6558 46619322
Pancreatitis acute 183.92 10.81 192 59990 24680 46601200
Ketoacidosis 145.39 10.81 80 60102 3875 46622005
Product dose omission issue 144.92 10.81 512 59670 168008 46457872
No adverse event 142.06 10.81 197 59985 34034 46591846
Hyperglycaemia 141.33 10.81 199 59983 34872 46591008
Carotid artery thrombosis 137.77 10.81 47 60135 683 46625197
Neurologic neglect syndrome 128.81 10.81 44 60138 642 46625238
Hyperkalaemia 121.18 10.81 227 59955 50482 46575398
Adenocarcinoma pancreas 120.58 10.81 48 60134 1098 46624782
Blood glucose decreased 108.84 10.81 128 60054 18764 46607116
Blood glucose fluctuation 105.27 10.81 66 60116 4080 46621800
Product residue present 104.14 10.81 64 60118 3818 46622062
Personality disorder 100.61 10.81 58 60124 3075 46622805
Euglycaemic diabetic ketoacidosis 100.47 10.81 50 60132 1966 46623914
Bile duct stent insertion 99.97 10.81 22 60160 45 46625835
Adjustment disorder 98.38 10.81 44 60138 1355 46624525
Lipase increased 85.28 10.81 78 60104 8525 46617355
Pancreaticoduodenectomy 82.49 10.81 17 60165 21 46625859
Treatment failure 76.01 10.81 14 60168 93073 46532807
Hemiplegia 74.89 10.81 66 60116 6872 46619008
Wrong technique in product usage process 74.63 10.81 195 59987 54227 46571653
Off label use 72.75 10.81 249 59933 379592 46246288
Contraindicated product administered 69.80 10.81 10 60172 79937 46545943
Pain 66.53 10.81 353 59829 476595 46149285
Diabetes mellitus 66.22 10.81 177 60005 49888 46575992
Adverse event 61.40 10.81 136 60046 34048 46591832
Rheumatoid arthritis 60.37 10.81 138 60044 240077 46385803
Drug abuse 60.12 10.81 6 60176 63402 46562478
Metastases to liver 58.85 10.81 97 60085 19488 46606392
Completed suicide 58.54 10.81 61 60121 145859 46480021
Toxicity to various agents 57.91 10.81 116 60066 211650 46414230
Affect lability 55.87 10.81 60 60122 7960 46617920
Systemic lupus erythematosus 54.96 10.81 9 60173 65171 46560709
Drug ineffective 54.37 10.81 586 59596 677252 45948628
Metabolic acidosis 52.18 10.81 138 60044 38642 46587238
Exposure during pregnancy 52.16 10.81 38 60144 108174 46517706
Maternal exposure during pregnancy 52.11 10.81 34 60148 102515 46523365
Inappropriate schedule of product administration 51.07 10.81 192 59990 64821 46561059
Hypoglycaemic coma 50.79 10.81 35 60147 2539 46623341
Pancreatitis chronic 48.91 10.81 30 60152 1783 46624097
Synovitis 48.14 10.81 10 60172 61065 46564815
Drug intolerance 47.01 10.81 73 60109 146976 46478904
Pemphigus 46.48 10.81 3 60179 45271 46580609
MELAS syndrome 44.66 10.81 13 60169 108 46625772
Seronegative arthritis 44.51 10.81 21 60161 733 46625147
Diarrhoea 44.41 10.81 987 59195 558615 46067265
Diabetic metabolic decompensation 43.64 10.81 24 60158 1161 46624719
Therapeutic product effect decreased 42.49 10.81 27 60155 82574 46543306
Product prescribing error 42.08 10.81 85 60097 19962 46605918
Sensory loss 41.81 10.81 48 60134 6854 46619026
Temperature perception test abnormal 41.72 10.81 9 60173 16 46625864
Product packaging quantity issue 41.66 10.81 23 60159 1121 46624759
Motor dysfunction 41.37 10.81 49 60133 7233 46618647
Joint swelling 41.21 10.81 96 60086 165977 46459903
Pneumobilia 41.07 10.81 13 60169 147 46625733
Anuria 36.22 10.81 58 60124 11373 46614507
Muscle spasticity 36.19 10.81 58 60124 11382 46614498
Pancreatectomy 36.15 10.81 8 60174 17 46625863
Neutropenia 36.15 10.81 82 60100 143122 46482758
Renal cyst 35.70 10.81 50 60132 8709 46617171
Tubulointerstitial nephritis 35.05 10.81 66 60116 14722 46611158
Gangrene 34.25 10.81 36 60146 4659 46621221
General physical health deterioration 34.24 10.81 261 59921 115508 46510372
Arterial occlusive disease 33.57 10.81 36 60146 4768 46621112
Radiotherapy 32.31 10.81 13 60169 306 46625574
Injection site erythema 32.28 10.81 29 60153 74398 46551482
Drug hypersensitivity 31.93 10.81 184 59998 243641 46382239
Hepatic steatosis 31.78 10.81 85 60097 23957 46601923
Dysphagia 31.68 10.81 189 59993 77123 46548757
Tubulointerstitial nephritis and uveitis syndrome 31.37 10.81 10 60172 116 46625764
Pancreatic mass 30.73 10.81 17 60165 832 46625048
Bursitis infective 30.54 10.81 19 60163 1158 46624722
Mixed liver injury 30.18 10.81 28 60154 3115 46622765
Abdominal pain upper 30.16 10.81 303 59879 145002 46480878
Glossodynia 29.78 10.81 10 60172 44363 46581517
Infusion related reaction 29.77 10.81 53 60129 101155 46524725
Coordination abnormal 28.64 10.81 51 60131 10898 46614982
Circumstance or information capable of leading to medication error 28.61 10.81 27 60155 3069 46622811
Pancreatic stent placement 28.28 10.81 5 60177 0 46625880
Insulin-requiring type 2 diabetes mellitus 28.20 10.81 8 60174 60 46625820
Renal disorder 28.15 10.81 87 60095 26599 46599281
Genital infection female 27.65 10.81 9 60173 112 46625768
Hemiparesis 27.59 10.81 72 60110 19997 46605883
Diabetic neuropathy 27.55 10.81 29 60153 3760 46622120
Explorative laparotomy 26.93 10.81 7 60175 36 46625844
Tumour invasion 26.69 10.81 9 60173 126 46625754
Pancreatic carcinoma stage IV 26.46 10.81 7 60175 39 46625841
Eating disorder 25.97 10.81 58 60124 14596 46611284
Splenic vein occlusion 25.93 10.81 5 60177 3 46625877
Flatulence 25.82 10.81 89 60093 28789 46597091
Migraine 25.11 10.81 32 60150 69994 46555886
Diabetic hyperosmolar coma 24.94 10.81 12 60170 438 46625442
Febrile neutropenia 24.84 10.81 53 60129 94574 46531306
Musculoskeletal stiffness 24.81 10.81 56 60126 97937 46527943
Seizure 24.61 10.81 79 60103 122975 46502905
Splenectomy 24.49 10.81 12 60170 456 46625424
Death 24.42 10.81 296 59886 335252 46290628
Metastases to lymph nodes 24.32 10.81 36 60146 6595 46619285
Product use in unapproved indication 24.17 10.81 50 60132 90223 46535657
Therapeutic drug monitoring analysis not performed 23.97 10.81 12 60170 478 46625402
Pancreatic duct dilatation 23.82 10.81 9 60173 178 46625702
Decreased vibratory sense 23.68 10.81 10 60172 267 46625613
Tonsillectomy 23.34 10.81 14 60168 799 46625081
Nausea 23.24 10.81 1095 59087 686359 45939521
Aphasia 22.94 10.81 85 60097 28482 46597398
Radiotherapy to pancreas 22.62 10.81 4 60178 0 46625880
Urine ketone body present 22.37 10.81 20 60162 2122 46623758
Lower respiratory tract infection 22.10 10.81 23 60159 55066 46570814
Alopecia 22.09 10.81 121 60061 162293 46463587
Hyperlactacidaemia 21.79 10.81 20 60162 2195 46623685
Arthropathy 21.77 10.81 48 60134 84652 46541228
Cerebral infarction 21.76 10.81 73 60109 23293 46602587
Loss of personal independence in daily activities 21.70 10.81 25 60157 57158 46568722
Weight decreased 21.31 10.81 386 59796 210463 46415417
Hysterectomy 21.25 10.81 37 60145 7769 46618111
Hand deformity 21.18 10.81 9 60173 34565 46591315
Prevertebral soft tissue swelling of cervical space 20.81 10.81 6 60176 48 46625832
Glycosylated haemoglobin decreased 20.77 10.81 11 60171 493 46625387
Flushing 20.70 10.81 32 60150 64582 46561298
Amylase increased 20.54 10.81 30 60152 5429 46620451
Multiple sclerosis relapse 20.02 10.81 15 60167 42110 46583770
Muscular weakness 19.75 10.81 193 59989 91651 46534229
Mucosal inflammation 19.68 10.81 13 60169 38963 46586917
Pancreatic cyst 19.67 10.81 15 60167 1274 46624606
Disease progression 19.40 10.81 57 60125 91243 46534637
Pancreatic pseudocyst 19.34 10.81 11 60171 568 46625312
Internal haemorrhage 19.01 10.81 26 60156 4429 46621451
Diabetic ulcer 18.97 10.81 8 60174 213 46625667
Incisional hernia repair 18.58 10.81 4 60178 7 46625873
Aortic arteriosclerosis 18.09 10.81 29 60153 5692 46620188
Central obesity 17.99 10.81 12 60170 825 46625055
C-reactive protein abnormal 17.79 10.81 3 60179 21267 46604613
Dizziness 17.78 10.81 569 59613 339845 46286035
Vomiting 17.61 10.81 732 59450 452062 46173818
Type 2 diabetes mellitus 17.55 10.81 61 60121 19814 46606066
Dysarthria 17.54 10.81 95 60087 37403 46588477
Dehydration 17.51 10.81 296 59886 159244 46466636
Urine albumin/creatinine ratio increased 17.43 10.81 7 60175 164 46625716
Anaemia vitamin B12 deficiency 17.42 10.81 9 60173 383 46625497
Product use issue 17.40 10.81 63 60119 94581 46531299
Glomerular filtration rate decreased 17.15 10.81 43 60139 11651 46614229
Injury 16.98 10.81 19 60163 44008 46581872
Biliary sphincterotomy 16.97 10.81 3 60179 0 46625880
Renal failure 16.86 10.81 222 59960 113372 46512508
Pericarditis 16.75 10.81 5 60177 23922 46601958
Fear-related avoidance of activities 16.67 10.81 6 60176 103 46625777
Pancreatic neuroendocrine tumour 16.37 10.81 8 60174 302 46625578
Diabetic complication 16.31 10.81 12 60170 965 46624915
Pancreatic atrophy 16.25 10.81 6 60176 111 46625769
Dysuria 16.19 10.81 75 60107 27758 46598122
Cerebrovascular accident 16.06 10.81 200 59982 100839 46525041
Abdominal pain 16.05 10.81 399 59783 229632 46396248
Injection site reaction 16.00 10.81 23 60159 47826 46578054
Multiple sclerosis 15.93 10.81 6 60176 24785 46601095
Cervix neoplasm 15.88 10.81 7 60175 208 46625672
Obstructive pancreatitis 15.67 10.81 7 60175 215 46625665
Product colour issue 15.62 10.81 10 60172 641 46625239
Type 1 diabetes mellitus 15.58 10.81 19 60163 2891 46622989
Pyrexia 15.57 10.81 337 59845 348465 46277415
Rhinorrhoea 15.52 10.81 110 60072 47555 46578325
Papilloma 15.46 10.81 7 60175 222 46625658
Metastases to peritoneum 15.34 10.81 18 60164 2630 46623250
Haemoglobin increased 15.30 10.81 18 60164 2637 46623243
Osteonecrosis 15.30 10.81 7 60175 25737 46600143
Tri-iodothyronine free decreased 15.28 10.81 7 60175 228 46625652
Arthralgia 15.21 10.81 356 59826 364247 46261633
Leukopenia 15.00 10.81 42 60140 68301 46557579
Bladder cancer 14.99 10.81 19 60163 3007 46622873
Respiratory arrest 14.87 10.81 13 60169 33803 46592077
Angioedema 14.74 10.81 94 60088 39248 46586632
Peripheral vascular disorder 14.57 10.81 27 60155 5950 46619930
Biliary obstruction 14.56 10.81 17 60165 2472 46623408
Pancreatic neuroendocrine tumour metastatic 14.47 10.81 4 60178 27 46625853
Glycosylated haemoglobin abnormal 14.45 10.81 5 60177 76 46625804
Inability to afford medication 14.34 10.81 12 60170 1164 46624716
Micturition disorder 14.32 10.81 14 60168 1662 46624218
Pancreatic neoplasm 14.28 10.81 10 60172 744 46625136
Blood creatinine increased 14.26 10.81 156 60026 76247 46549633
Gingival hypertrophy 14.25 10.81 13 60169 1416 46624464
Gastrointestinal disorder 14.21 10.81 128 60054 59448 46566432
Hunger 14.15 10.81 21 60161 3854 46622026
Sopor 14.15 10.81 4 60178 19824 46606056
Pancreatic failure 13.94 10.81 9 60173 585 46625295
Pancreatitis necrotising 13.94 10.81 13 60169 1456 46624424
Therapy non-responder 13.55 10.81 20 60162 41132 46584748
Intensive care unit acquired weakness 13.32 10.81 9 60173 632 46625248
Adrenal mass 13.30 10.81 10 60172 831 46625049
Biliary dilatation 13.25 10.81 15 60167 2109 46623771
Product blister packaging issue 13.20 10.81 6 60176 192 46625688
Hepatic cancer 13.10 10.81 18 60164 3079 46622801
Peripheral artery haematoma 13.08 10.81 4 60178 40 46625840
Vitamin B12 decreased 13.08 10.81 17 60165 2758 46623122
Cholecystectomy 13.00 10.81 33 60149 9009 46616871
Infusion site scar 12.92 10.81 6 60176 202 46625678
Acquired mitochondrial DNULL mutation 12.82 10.81 3 60179 9 46625871
Abortion spontaneous 12.70 10.81 23 60159 43623 46582257
Cataract 12.64 10.81 101 60081 45314 46580566
Multiple drug therapy 12.59 10.81 10 60172 901 46624979
Meibomianitis 12.50 10.81 4 60178 47 46625833
Product monitoring error 12.38 10.81 14 60168 1967 46623913
Cytomegalovirus infection 12.33 10.81 4 60178 18140 46607740
Acidosis 12.31 10.81 37 60145 11137 46614743
Dyslipidaemia 12.24 10.81 24 60158 5516 46620364
Altered state of consciousness 12.20 10.81 61 60121 23287 46602593
Increased appetite 12.14 10.81 31 60151 8496 46617384
Coma acidotic 12 10.81 5 60177 129 46625751
Splenic granuloma 11.96 10.81 3 60179 13 46625867
Intertrigo 11.94 10.81 7 60175 383 46625497
Ketonuria 11.94 10.81 7 60175 383 46625497
Hypersensitivity 11.92 10.81 130 60052 150191 46475689
Carcinoid crisis 11.87 10.81 6 60176 244 46625636
Mesenteric neoplasm 11.78 10.81 3 60179 14 46625866
Cholestatic liver injury 11.77 10.81 14 60168 2076 46623804
Product size issue 11.69 10.81 7 60175 398 46625482
Pulmonary haematoma 11.67 10.81 4 60178 59 46625821
Premature delivery 11.64 10.81 7 60175 22062 46603818
Acute abdomen 11.63 10.81 12 60170 1520 46624360
Subacute kidney injury 11.61 10.81 3 60179 15 46625865
Rash pruritic 11.59 10.81 97 60085 44118 46581762
Abnormal loss of weight 11.53 10.81 22 60160 4953 46620927
Coronavirus infection 11.46 10.81 16 60166 2778 46623102
Endometrial disorder 11.39 10.81 8 60174 598 46625282
Cardiac arrest 11.39 10.81 69 60113 90330 46535550
Device dislocation 11.38 10.81 7 60175 21795 46604085
Appendicectomy 11.29 10.81 15 60167 2486 46623394
Hypoglycaemic encephalopathy 11.21 10.81 6 60176 275 46625605
Oesophageal mucosal tear 11.15 10.81 3 60179 18 46625862
Gallbladder enlargement 11.09 10.81 8 60174 624 46625256
Pollakiuria 11.03 10.81 61 60121 24200 46601680
Rhabdomyolysis 11.01 10.81 92 60090 41817 46584063
Nephroangiosclerosis 11.00 10.81 5 60177 160 46625720
Pneumonia 10.98 10.81 386 59796 375934 46249946
Bile duct stenosis 10.94 10.81 10 60172 1091 46624789
Injection site pain 10.93 10.81 87 60095 107065 46518815
Posterior reversible encephalopathy syndrome 10.90 10.81 3 60179 15138 46610742
Infrequent bowel movements 10.89 10.81 10 60172 1098 46624782
Intestinal transit time abnormal 10.89 10.81 4 60178 73 46625807
Splenic vein thrombosis 10.88 10.81 6 60176 292 46625588
Hyperlipidaemia 10.82 10.81 50 60132 18489 46607391

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
Pancreatitis 649.55 10.54 552 58154 35938 29857834
Hypoglycaemia 543.68 10.54 581 58125 50400 29843372
Pancreatic carcinoma 517.04 10.54 269 58437 7568 29886204
Blood glucose increased 482.03 10.54 598 58108 60932 29832840
Diabetes mellitus inadequate control 385.99 10.54 265 58441 12497 29881275
Pancreatic carcinoma metastatic 378.70 10.54 165 58541 3082 29890690
Lactic acidosis 372.42 10.54 378 58328 30835 29862937
Glycosylated haemoglobin increased 268.04 10.54 189 58517 9302 29884470
Diabetic ketoacidosis 230.71 10.54 215 58491 15771 29878001
Adenocarcinoma pancreas 214.39 10.54 86 58620 1292 29892480
Pancreatitis acute 212.60 10.54 257 58449 25438 29868334
Metastases to liver 172.78 10.54 161 58545 11804 29881968
Pancreaticoduodenectomy 158.12 10.54 35 58671 37 29893735
Lipase increased 147.48 10.54 128 58578 8548 29885224
Toxicity to various agents 137.67 10.54 89 58617 177094 29716678
Bile duct stent insertion 136.37 10.54 33 58673 67 29893705
No adverse event 124.53 10.54 162 58544 17257 29876515
Ketoacidosis 120.86 10.54 81 58625 3665 29890107
Pemphigoid 115.88 10.54 105 58601 7423 29886349
Hyperglycaemia 112.56 10.54 227 58479 34973 29858799
Pancreatectomy 110.64 10.54 24 58682 21 29893751
Radiotherapy 109.81 10.54 38 58668 367 29893405
Bladder cancer 104.39 10.54 108 58598 8994 29884778
Blood glucose abnormal 100.49 10.54 83 58623 5176 29888596
Hyperkalaemia 98.57 10.54 319 58387 65691 29828081
Acute kidney injury 95.36 10.54 885 57821 272957 29620815
Product dose omission issue 86.25 10.54 382 58324 91249 29802523
Pancreatitis chronic 83.88 10.54 49 58657 1735 29892037
Pancreatic stent placement 69.22 10.54 15 58691 13 29893759
Euglycaemic diabetic ketoacidosis 66.54 10.54 43 58663 1828 29891944
Blood glucose decreased 66.09 10.54 103 58603 12950 29880822
Renal cyst 63.50 10.54 78 58628 7839 29885933
Off label use 62.52 10.54 264 58442 249026 29644746
Pancreatic neoplasm 57.78 10.54 31 58675 928 29892844
Metabolic acidosis 57.65 10.54 183 58523 37278 29856494
Product residue present 56.95 10.54 45 58661 2633 29891139
Diabetes mellitus 56.83 10.54 196 58510 41669 29852103
Interstitial lung disease 56.62 10.54 251 58455 59946 29833826
Diverticulum intestinal 54.92 10.54 48 58658 3234 29890538
Hyperlipidaemia 54.71 10.54 98 58608 13809 29879963
Prostatomegaly 53.14 10.54 55 58651 4581 29889191
Cholelithiasis 51.51 10.54 119 58587 20106 29873666
Explorative laparotomy 51.11 10.54 12 58694 20 29893752
Febrile neutropenia 50.49 10.54 82 58624 106611 29787161
Blood glucose fluctuation 48.53 10.54 47 58659 3614 29890158
Death 47.88 10.54 459 58247 356824 29536948
Pyrexia 47.65 10.54 360 58346 294129 29599643
Pancreatic enzymes increased 46.32 10.54 23 58683 584 29893188
Amylase increased 45.96 10.54 57 58649 5784 29887988
Cholecystectomy 45.88 10.54 38 58668 2378 29891394
Seronegative arthritis 45.42 10.54 25 58681 788 29892984
General physical health deterioration 45.22 10.54 343 58363 99601 29794171
Neutropenia 44.59 10.54 118 58588 128422 29765350
Insulin-requiring type 2 diabetes mellitus 43.99 10.54 15 58691 138 29893634
Splenectomy 41.91 10.54 19 58687 391 29893381
Metastases to lymph nodes 41.70 10.54 45 58661 3932 29889840
Pancreatic cyst 40.89 10.54 23 58683 757 29893015
Biliary sphincterotomy 40.43 10.54 9 58697 10 29893762
Blood lactic acid 40.08 10.54 18 58688 362 29893410
Product use in unapproved indication 39.39 10.54 52 58654 73641 29820131
Weight decreased 39.14 10.54 460 58246 150461 29743311
Cerebral infarction 38.90 10.54 127 58579 26246 29867526
Hypoglycaemic coma 38.82 10.54 34 58672 2297 29891475
Inappropriate schedule of product administration 38.36 10.54 167 58539 39561 29854211
Circumstance or information capable of leading to medication error 38.34 10.54 29 58677 1590 29892182
Diabetic foetopathy 38.28 10.54 15 58691 211 29893561
Pancreatitis necrotising 37.85 10.54 34 58672 2375 29891397
Therapeutic drug monitoring analysis not performed 35.89 10.54 17 58689 388 29893384
Seizure 34.44 10.54 90 58616 98385 29795387
Completed suicide 33.98 10.54 92 58614 99400 29794372
Diabetic metabolic decompensation 33.86 10.54 25 58681 1321 29892451
Hyperlactacidaemia 33.68 10.54 33 58673 2573 29891199
Disease progression 33.62 10.54 66 58640 79808 29813964
Glycosylated haemoglobin decreased 31.48 10.54 15 58691 347 29893425
Gastroenterostomy 31.26 10.54 9 58697 44 29893728
Prostatic calcification 31.01 10.54 11 58695 115 29893657
Metastases to peritoneum 30.64 10.54 25 58681 1532 29892240
Adverse event 30.36 10.54 82 58624 15259 29878513
Pancreatic disorder 29.89 10.54 25 58681 1586 29892186
Tonsillectomy 29.38 10.54 14 58692 324 29893448
Autoimmune pancreatitis 28.70 10.54 13 58693 267 29893505
Pemphigus 28.57 10.54 22 58684 1239 29892533
Large for dates baby 28.51 10.54 19 58687 851 29892921
Pancreatic pseudocyst 27.48 10.54 18 58688 783 29892989
Plasma cell myeloma 27.28 10.54 39 58667 53423 29840349
Product packaging quantity issue 27.25 10.54 17 58689 679 29893093
Pneumobilia 27.01 10.54 8 58698 44 29893728
Gastrooesophageal reflux disease 26.98 10.54 130 58576 32125 29861647
Mucosal inflammation 26.95 10.54 13 58693 30481 29863291
Pancreatic mass 26.76 10.54 18 58688 819 29892953
Diabetic nephropathy 26.68 10.54 25 58681 1844 29891928
Respiratory arrest 26.59 10.54 12 58694 29246 29864526
Toe amputation 26.43 10.54 27 58679 2214 29891558
Electrolyte imbalance 26.40 10.54 65 58641 11435 29882337
Nephrolithiasis 26.04 10.54 107 58599 24703 29869069
Aortic arteriosclerosis 25.46 10.54 35 58671 3929 29889843
Spinal osteoarthritis 25.04 10.54 45 58661 6354 29887418
Discoloured vomit 24.60 10.54 13 58693 377 29893395
Polyuria 24.39 10.54 48 58658 7258 29886514
Cytomegalovirus infection 24.35 10.54 8 58698 23666 29870106
Product monitoring error 24.30 10.54 23 58683 1718 29892054
Urine ketone body present 24.22 10.54 18 58688 961 29892811
Drug dependence 24.11 10.54 6 58700 21289 29872483
Alcoholic ketoacidosis 23.93 10.54 6 58700 15 29893757
Splenic vein thrombosis 23.63 10.54 12 58694 320 29893452
Vomiting projectile 23.46 10.54 15 58691 626 29893146
Biliary dilatation 23.44 10.54 16 58690 746 29893026
Unevaluable event 23.24 10.54 17 58689 31768 29862004
Type 2 diabetes mellitus 23.23 10.54 69 58637 13553 29880219
Sprue-like enteropathy 23.13 10.54 12 58694 335 29893437
Inability to afford medication 23.01 10.54 16 58690 769 29893003
Stent placement 22.89 10.54 36 58670 4560 29889212
Wrong technique in product usage process 22.84 10.54 121 58585 31034 29862738
Dizziness 22.53 10.54 520 58186 194389 29699383
Adrenal mass 22.34 10.54 14 58692 564 29893208
Ductal adenocarcinoma of pancreas 22.32 10.54 7 58699 48 29893724
Vena cava filter insertion 22.22 10.54 6 58700 22 29893750
Pancreatic carcinoma stage III 21.82 10.54 5 58701 7 29893765
Chronic gastritis 21.68 10.54 18 58688 1130 29892642
Glycosylated haemoglobin abnormal 21.64 10.54 8 58698 95 29893677
Suicide attempt 21.60 10.54 24 58682 36673 29857099
Food aversion 21.57 10.54 11 58695 296 29893476
Osteonecrosis 21.57 10.54 3 58703 16132 29877640
Pulmonary mass 21.43 10.54 58 58648 10804 29882968
Peripancreatic fluid collection 21.43 10.54 6 58700 26 29893746
Lower respiratory tract infection 21.26 10.54 13 58693 26701 29867071
Pancreatic carcinoma recurrent 21.25 10.54 6 58700 27 29893745
Malignant ascites 21.22 10.54 12 58694 399 29893373
Pancreatic carcinoma stage IV 21.06 10.54 8 58698 103 29893669
Diverticulum 21.00 10.54 43 58663 6690 29887082
Intestinal adhesion lysis 20.95 10.54 4 58702 0 29893772
Pancreatic sphincterotomy 20.95 10.54 4 58702 0 29893772
Radiotherapy to pancreas 20.95 10.54 4 58702 0 29893772
Angioedema 20.90 10.54 127 58579 34257 29859515
Psychotic disorder 20.88 10.54 8 58698 21507 29872265
Hepatic steatosis 20.71 10.54 70 58636 14723 29879049
Metastases to lung 20.70 10.54 47 58659 7848 29885924
Haemoglobin decreased 20.56 10.54 135 58571 113963 29779809
Drug resistance 20.36 10.54 7 58699 20126 29873646
Suicidal ideation 19.78 10.54 25 58681 36089 29857683
Eczema asteatotic 19.77 10.54 9 58697 187 29893585
Pancreatolithiasis 19.75 10.54 7 58699 73 29893699
Unresponsive to stimuli 19.48 10.54 14 58692 26405 29867367
Pyelitis 19.41 10.54 7 58699 77 29893695
Hypoosmolar state 19.41 10.54 7 58699 77 29893695
Infusion related reaction 19.33 10.54 31 58675 40533 29853239
Duodenitis 19.23 10.54 31 58675 4009 29889763
Thirst 18.93 10.54 42 58664 6907 29886865
Hyperlipasaemia 18.89 10.54 12 58694 495 29893277
Hypoxia 18.89 10.54 41 58665 47813 29845959
Foetal exposure during pregnancy 18.70 10.54 27 58679 36844 29856928
Respiratory failure 18.68 10.54 118 58588 100524 29793248
Drug intolerance 18.55 10.54 38 58668 45253 29848519
Drug ineffective 18.52 10.54 517 58189 339870 29553902
Chills 18.43 10.54 76 58630 72262 29821510
Diabetic neuropathy 18.33 10.54 30 58676 3929 29889843
Coronavirus infection 18.26 10.54 28 58678 3470 29890302
Vitamin B12 deficiency 18.25 10.54 24 58682 2581 29891191
Urticaria chronic 18.16 10.54 7 58699 94 29893678
Bile duct cancer 18.10 10.54 13 58693 658 29893114
Encephalopathy 17.95 10.54 22 58684 32183 29861589
Hallucination 17.78 10.54 44 58662 49015 29844757
Pancytopenia 17.77 10.54 96 58610 84956 29808816
Intraductal papillary-mucinous carcinoma of pancreas 17.71 10.54 4 58702 5 29893767
Staphylococcal infection 17.54 10.54 20 58686 30204 29863568
Small intestine carcinoma 17.53 10.54 11 58695 444 29893328
Renal mass 17.52 10.54 18 58688 1486 29892286
Pollakiuria 17.03 10.54 72 58634 16834 29876938
Intentional self-injury 16.99 10.54 3 58703 13529 29880243
Pancreatic duct dilatation 16.89 10.54 6 58700 63 29893709
Bile duct stenosis 16.68 10.54 16 58690 1215 29892557
Pancreatic duct obstruction 16.57 10.54 4 58702 8 29893764
Large intestine polyp 16.56 10.54 39 58667 6670 29887102
Alanine aminotransferase increased 16.55 10.54 82 58624 74194 29819578
Superinfection 16.46 10.54 18 58688 1596 29892176
Biliary obstruction 16.27 10.54 22 58684 2431 29891341
Phlebolith 16.25 10.54 4 58702 9 29893763
Hepatic lesion 16.22 10.54 25 58681 3111 29890661
Pain 16.01 10.54 240 58466 172401 29721371
Choledochoenterostomy 15.71 10.54 3 58703 0 29893772
Blood elastase increased 15.71 10.54 3 58703 0 29893772
Duodenal sphincterotomy 15.71 10.54 3 58703 0 29893772
Bile duct adenocarcinoma 15.71 10.54 3 58703 0 29893772
Biopsy pancreas 15.71 10.54 3 58703 0 29893772
Splenic vein occlusion 15.71 10.54 3 58703 0 29893772
Decreased ventricular preload 15.62 10.54 5 58701 37 29893735
Oscillopsia 15.50 10.54 5 58701 38 29893734
Nephrogenic anaemia 15.44 10.54 20 58686 2119 29891653
Cholecystitis chronic 15.44 10.54 13 58693 832 29892940
Abdominal pain upper 15.44 10.54 189 58517 62362 29831410
Mental status changes 15.28 10.54 31 58675 37048 29856724
Lithotripsy 15.19 10.54 4 58702 13 29893759
Treatment failure 15.15 10.54 28 58678 34651 29859121
Intentional product misuse 15.14 10.54 28 58678 34639 29859133
Acetonaemia 15.02 10.54 6 58700 89 29893683
Metastases to spleen 15.02 10.54 9 58697 334 29893438
Pseudohyponatraemia 14.96 10.54 6 58700 90 29893682
Umbilical hernia repair 14.86 10.54 5 58701 44 29893728
Gastrointestinal mucosal necrosis 14.81 10.54 7 58699 159 29893613
Rhinorrhoea 14.80 10.54 80 58626 20674 29873098
Bladder transitional cell carcinoma 14.77 10.54 21 58685 2432 29891340
Wrong patient received product 14.73 10.54 18 58688 1799 29891973
Ketonuria 14.71 10.54 11 58695 593 29893179
Hypomagnesaemia 14.68 10.54 68 58638 16530 29877242
Oedematous pancreatitis 14.67 10.54 9 58697 349 29893423
Osteoarthritis 14.66 10.54 73 58633 18276 29875496
Pancreatic failure 14.61 10.54 12 58694 742 29893030
Cockroach allergy 14.47 10.54 5 58701 48 29893724
Abdominal pain 14.45 10.54 358 58348 135296 29758476
Abscess drainage 14.42 10.54 8 58698 256 29893516
Romberg test positive 14.38 10.54 5 58701 49 29893723
Vitamin B1 decreased 14.34 10.54 7 58699 171 29893601
Thrombocytopenia 14.31 10.54 186 58520 136858 29756914
Hernia repair 14.31 10.54 14 58692 1090 29892682
Blood ketone body increased 14.30 10.54 9 58697 365 29893407
Flour sensitivity 14.29 10.54 5 58701 50 29893722
Alopecia universalis 14.29 10.54 5 58701 50 29893722
Renal impairment 14.23 10.54 238 58468 83946 29809826
Acute respiratory distress syndrome 14.20 10.54 15 58691 23457 29870315
Pneumocystis jirovecii pneumonia 14.09 10.54 8 58698 17112 29876660
Thyroid neoplasm 14 10.54 9 58697 379 29893393
Drug withdrawal syndrome 13.96 10.54 11 58695 19798 29873974
Insulin C-peptide increased 13.87 10.54 5 58701 55 29893717
Hyperglycaemic hyperosmolar nonketotic syndrome 13.85 10.54 13 58693 961 29892811
Dyslipidaemia 13.82 10.54 33 58673 5694 29888078
Central venous catheterisation 13.69 10.54 13 58693 975 29892797
Agitation 13.65 10.54 57 58649 54016 29839756
Biliary neoplasm 13.64 10.54 3 58703 3 29893769
Pseudocyst 13.64 10.54 7 58699 191 29893581
Hepatic enzyme decreased 13.63 10.54 5 58701 58 29893714
Campylobacter infection 13.62 10.54 11 58695 664 29893108
Generalised tonic-clonic seizure 13.60 10.54 11 58695 19540 29874232
Amaurosis 13.59 10.54 11 58695 666 29893106
Knee operation 13.53 10.54 15 58691 1351 29892421
Palindromic rheumatism 13.41 10.54 7 58699 198 29893574
Nephroangiosclerosis 13.37 10.54 7 58699 199 29893573
Intra-abdominal fluid collection 13.35 10.54 14 58692 1184 29892588
Gallbladder disorder 13.29 10.54 33 58673 5834 29887938
Appendicectomy 13.25 10.54 12 58694 847 29892925
Infection 13.25 10.54 94 58612 77980 29815792
Product availability issue 13.23 10.54 11 58695 692 29893080
Pancreatic fistula 13.19 10.54 5 58701 64 29893708
Dependence on respirator 13.07 10.54 4 58702 25 29893747
Intentional overdose 12.95 10.54 40 58666 41441 29852331
Hypotension 12.92 10.54 297 58409 200268 29693504
Pruritus 12.90 10.54 313 58393 117891 29775881
Bladder irrigation 12.85 10.54 5 58701 69 29893703
Nephropathy 12.84 10.54 31 58675 5385 29888387
Toxic skin eruption 12.76 10.54 49 58657 10966 29882806
Rhabdomyolysis 12.75 10.54 185 58521 63395 29830377
Injection site nodule 12.73 10.54 15 58691 1443 29892329
Flushing 12.72 10.54 24 58682 29468 29864304
Large intestinal polypectomy 12.72 10.54 5 58701 71 29893701
Aggression 12.68 10.54 34 58672 36873 29856899
Subdural hygroma 12.68 10.54 8 58698 326 29893446
Hypoglycaemic encephalopathy 12.51 10.54 7 58699 228 29893544
Obstruction gastric 12.35 10.54 12 58694 926 29892846
Diarrhoea 12.30 10.54 785 57921 333318 29560454
Cyst removal 12.22 10.54 4 58702 32 29893740
Musculoskeletal pain 12.22 10.54 103 58603 30837 29862935
Bone marrow failure 12.19 10.54 25 58681 29760 29864012
Brain contusion 12.17 10.54 11 58695 775 29892997
Somnolence 12.16 10.54 126 58580 96637 29797135
Pancreatic leak 12.11 10.54 3 58703 7 29893765
Genital lesion 12.08 10.54 7 58699 244 29893528
Restlessness 12.01 10.54 16 58690 22583 29871189
Condition aggravated 11.98 10.54 194 58512 137672 29756100
Rheumatoid arthritis 11.97 10.54 41 58665 41156 29852616
Dyspnoea 11.94 10.54 533 58173 332762 29561010
Renal stone removal 11.91 10.54 4 58702 35 29893737
Abdominal discomfort 11.86 10.54 147 58559 48644 29845128
Granulomatous liver disease 11.84 10.54 9 58697 497 29893275
Hypercapnic coma 11.71 10.54 6 58700 163 29893609
Sedation 11.65 10.54 9 58697 16364 29877408
White blood cell count decreased 11.52 10.54 107 58599 83840 29809932
Pneumonia 11.49 10.54 537 58169 333769 29560003
Pulmonary embolism 11.42 10.54 98 58608 78037 29815735
Leukopenia 11.39 10.54 64 58642 56095 29837677
Arthroscopy 11.34 10.54 5 58701 96 29893676
Device related infection 11.31 10.54 10 58696 17005 29876767
Anxiety 11.31 10.54 117 58589 89754 29804018
Lung opacity 11.18 10.54 11 58695 862 29892910
Polydipsia 11.18 10.54 23 58683 3590 29890182
Colon cancer 11.18 10.54 39 58667 8333 29885439
Accidental exposure to product 11.16 10.54 3 58703 10112 29883660
Necrotising myositis 11.14 10.54 8 58698 405 29893367
Procedural headache 11.09 10.54 4 58702 44 29893728
Suspected counterfeit product 11.06 10.54 7 58699 287 29893485
Aspartate aminotransferase increased 10.93 10.54 76 58630 63346 29830426
Malignant neoplasm of ampulla of Vater 10.91 10.54 3 58703 12 29893760
Respiratory distress 10.86 10.54 31 58675 32941 29860831
Drug eruption 10.81 10.54 65 58641 17461 29876311
Gastrostomy 10.81 10.54 10 58696 726 29893046
Hyperadrenalism 10.78 10.54 4 58702 48 29893724
Hypoglycaemic seizure 10.76 10.54 7 58699 301 29893471
Generalised oedema 10.74 10.54 49 58657 11836 29881936
Cardio-respiratory arrest 10.72 10.54 67 58639 57239 29836533
Blood glucose 10.71 10.54 3 58703 13 29893759
Hypercholesterolaemia 10.69 10.54 36 58670 7556 29886216
Pancreatic calcification 10.68 10.54 6 58700 197 29893575
Rotator cuff repair 10.66 10.54 7 58699 306 29893466
Nasal neoplasm 10.64 10.54 5 58701 112 29893660
Haemophagocytic lymphohistiocytosis 10.63 10.54 3 58703 9788 29883984
Intraocular pressure decreased 10.60 10.54 5 58701 113 29893659
Tachycardia 10.55 10.54 93 58613 73646 29820126
Hepatic cyst 10.55 10.54 18 58688 2440 29891332

Pharmacologic Action:

SourceCodeDescription
ATC A10BH01 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Dipeptidyl peptidase 4 (DPP-4) inhibitors
ATC A10BD07 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 A10BD24 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Combinations of oral blood glucose lowering drugs
ATC A10BH51 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Dipeptidyl peptidase 4 (DPP-4) inhibitors
MeSH PA D054873 Dipeptidyl-Peptidase IV Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D006728 Hormones
MeSH PA D007004 Hypoglycemic Agents
MeSH PA D054795 Incretins
MeSH PA D011480 Protease Inhibitors
FDA MoA N0000175912 Dipeptidyl Peptidase 4 Inhibitors
FDA EPC N0000175913 Dipeptidyl Peptidase 4 Inhibitor
CHEBI has role CHEBI:35526 hypoglycemic drug
CHEBI has role CHEBI:35703 xenobiotic
CHEBI has role CHEBI:48353 serine proteinase inhibitors
CHEBI has role CHEBI:68612 dpp-4 inhibitor
CHEBI has role CHEBI:78298 environmental contaminants

Drug Use (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
Infectious disease contraindication 40733004
Ketoacidosis contraindication 56051008
Metabolic acidosis contraindication 59455009
Hypopituitarism contraindication 74728003 DOID:9406
Cardiogenic shock contraindication 89138009
Kidney disease contraindication 90708001 DOID:557
Lactic acidosis contraindication 91273001 DOID:3650
Cobalamin deficiency contraindication 190634004
Decompensated cardiac failure contraindication 195111005
Acute pancreatitis contraindication 197456007 DOID:2913
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Sepsis syndrome contraindication 238150007
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Fever contraindication 386661006
Surgical procedure contraindication 387713003
Severe diarrhea contraindication 409587002
Traumatic injury contraindication 417746004
Fever greater than 100.4 Fahrenheit contraindication 426000000
Radiography with IV Iodinated Contrast Agent contraindication
Severe Hypoxemia contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.1 Basic
pKa2 2.67 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
EQ 25MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
EQ 50MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
1GM;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
500MG;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
1GM;EQ 100MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
1GM;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
500MG;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Aug. 12, 2022 INFORMATION ADDED TO THE LABELING REGARDING EFFICACY AND SAFETY OF THE CONTINUATION OF SITAGLIPTIN COMPARED WITH THE WITHDRAWAL OF SITAGLIPTIN DURING INITIATION AND TITRATION OF INSULIN GLARGINE IN SUBJECTS WITH TYPE 2 DIABETES MELLITUS
15MG;EQ 100MG BASE STEGLUJAN MERCK SHARP DOHME N209805 Dec. 19, 2017 RX TABLET ORAL Dec. 19, 2022 NEW CHEMICAL ENTITY
5MG;EQ 100MG BASE STEGLUJAN MERCK SHARP DOHME N209805 Dec. 19, 2017 RX TABLET ORAL Dec. 19, 2022 NEW CHEMICAL ENTITY
EQ 100MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
EQ 25MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
EQ 50MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
1GM;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
500MG;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
1GM;EQ 100MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
1GM;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
500MG;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Feb. 12, 2023 PEDIATRIC EXCLUSIVITY
EQ 100MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
EQ 25MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
EQ 50MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
1GM;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
500MG;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
1GM;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
500MG;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL Dec. 4, 2023 ADDITION OF CLINICAL INFORMATION OBTAINED FROM A PEDIATRIC TRIAL TO SECTION 8.4 OF THE LABELING
EQ 100MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY
EQ 25MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY
EQ 50MG BASE JANUVIA MERCK SHARP DOHME N021995 Oct. 16, 2006 RX TABLET ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY
1GM;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY
500MG;EQ 50MG BASE JANUMET MERCK SHARP DOHME N022044 March 30, 2007 RX TABLET ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY
1GM;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY
500MG;EQ 50MG BASE JANUMET XR MERCK SHARP DOHME N202270 Feb. 2, 2012 RX TABLET, EXTENDED RELEASE ORAL June 4, 2024 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Dipeptidyl peptidase 4 Enzyme INHIBITOR Ki 7.77 WOMBAT-PK CHEMBL
Dipeptidyl peptidase 2 Enzyme IC50 4.22 CHEMBL
Dipeptidyl peptidase 8 Enzyme IC50 4.96 CHEMBL
Dipeptidyl peptidase 9 Enzyme IC50 4.70 CHEMBL
Prolyl endopeptidase FAP Enzyme IC50 5.23 CHEMBL
Dipeptidyl peptidase 4 Enzyme IC50 7.16 CHEMBL

External reference:

IDSource
4025780 VUID
N0000179787 NUI
D06645 KEGG_DRUG
654671-77-9 SECONDARY_CAS_RN
4025780 VANDF
4025781 VANDF
C1702177 UMLSCUI
CHEBI:40237 CHEBI
715 PDB_CHEM_ID
CHEMBL1422 ChEMBL_ID
CHEMBL1201174 ChEMBL_ID
CHEMBL393336 ChEMBL_ID
D000068900 MESH_DESCRIPTOR_UI
6286 IUPHAR_LIGAND_ID
8692 INN_ID
DB01261 DRUGBANK_ID
QFP0P1DV7Z UNII
4369359 PUBCHEM_CID
593411 RXNORM
23649 MMSL
89034 MMSL
d05896 MMSL
011790 NDDF
011791 NDDF
423307000 SNOMEDCT_US
424106006 SNOMEDCT_US
425508009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
JANUMET XR HUMAN PRESCRIPTION DRUG LABEL 2 0006-0078 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 31 sections
JANUMET XR HUMAN PRESCRIPTION DRUG LABEL 2 0006-0080 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 31 sections
JANUMET XR HUMAN PRESCRIPTION DRUG LABEL 2 0006-0081 TABLET, FILM COATED, EXTENDED RELEASE 100 mg ORAL NDA 31 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 0006-0112 TABLET, FILM COATED 50 mg ORAL NDA 28 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 0006-0221 TABLET, FILM COATED 25 mg ORAL NDA 28 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 0006-0277 TABLET, FILM COATED 100 mg ORAL NDA 28 sections
JANUMET HUMAN PRESCRIPTION DRUG LABEL 2 0006-0575 TABLET, FILM COATED 50 mg ORAL NDA 30 sections
JANUMET HUMAN PRESCRIPTION DRUG LABEL 2 0006-0577 TABLET, FILM COATED 50 mg ORAL NDA 30 sections
STEGLUJAN HUMAN PRESCRIPTION DRUG LABEL 2 0006-5367 TABLET, FILM COATED 100 mg ORAL NDA 28 sections
STEGLUJAN HUMAN PRESCRIPTION DRUG LABEL 2 0006-5368 TABLET, FILM COATED 100 mg ORAL NDA 28 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-1036 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-3472 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-3527 TABLET, FILM COATED 25 mg ORAL NDA 26 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-4084 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-4086 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-4087 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
JANUMET XR HUMAN PRESCRIPTION DRUG LABEL 2 50090-4411 TABLET, FILM COATED, EXTENDED RELEASE 50 mg ORAL NDA 30 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-5517 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 50090-5547 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 54868-5840 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 54868-6031 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 55154-5040 TABLET, FILM COATED 50 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 55154-5042 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
JANUVIA HUMAN PRESCRIPTION DRUG LABEL 1 58118-0277 TABLET, FILM COATED 100 mg ORAL NDA 27 sections
JANUMET HUMAN PRESCRIPTION DRUG LABEL 2 70518-2548 TABLET, FILM COATED 50 mg ORAL NDA 29 sections