Stem definition | Drug id | CAS RN |
---|---|---|
dipeptidyl aminopeptidase-IV inhibitors | 3642 | 274901-16-5 |
Dose | Unit | Route |
---|---|---|
0.10 | g | O |
Property | Value | Reference |
---|---|---|
BA (Bioavailability) | 85 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 1.03 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 9.90 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.89 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 1.67 hours | Lombardo F, Berellini G, Obach RS |
S (Water solubility) | 60 mg/mL | Bocci G, Oprea TI, Benet LZ |
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Date | Agency | Company | Orphan |
---|---|---|---|
Sept. 26, 2007 | EMA |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Pemphigoid | 1098.77 | 23.58 | 217 | 4266 | 7127 | 63477412 |
Lactic acidosis | 239.66 | 23.58 | 93 | 4390 | 38194 | 63446345 |
Acute kidney injury | 133.02 | 23.58 | 125 | 4358 | 263290 | 63221249 |
Hypoglycaemia | 108.92 | 23.58 | 62 | 4421 | 60003 | 63424536 |
Diabetes mellitus inadequate control | 74.58 | 23.58 | 31 | 4452 | 15095 | 63469444 |
Dermatitis bullous | 61.49 | 23.58 | 23 | 4460 | 8485 | 63476054 |
Crush syndrome | 60.03 | 23.58 | 10 | 4473 | 119 | 63484420 |
Sensorimotor disorder | 52.52 | 23.58 | 11 | 4472 | 475 | 63484064 |
Compartment syndrome | 48.68 | 23.58 | 14 | 4469 | 2270 | 63482269 |
Hyperkalaemia | 48.63 | 23.58 | 36 | 4447 | 54167 | 63430372 |
Drug interaction | 47.57 | 23.58 | 69 | 4414 | 229062 | 63255477 |
Ketoacidosis | 47.48 | 23.58 | 16 | 4467 | 4362 | 63480177 |
Glycosylated haemoglobin increased | 46.65 | 23.58 | 21 | 4462 | 12377 | 63472162 |
Euglycaemic diabetic ketoacidosis | 46.14 | 23.58 | 15 | 4468 | 3659 | 63480880 |
Diabetic ketoacidosis | 44.90 | 23.58 | 24 | 4459 | 20481 | 63464058 |
Hyperglycaemia | 44.90 | 23.58 | 31 | 4452 | 41836 | 63442703 |
Acute generalised exanthematous pustulosis | 42.40 | 23.58 | 19 | 4464 | 11080 | 63473459 |
Shock | 41.87 | 23.58 | 24 | 4459 | 23439 | 63461100 |
Blood glucose increased | 36.87 | 23.58 | 37 | 4446 | 83719 | 63400820 |
Rhabdomyolysis | 36.76 | 23.58 | 28 | 4455 | 43923 | 63440616 |
Language disorder | 36.23 | 23.58 | 11 | 4472 | 2149 | 63482390 |
Pancreatitis acute | 36.10 | 23.58 | 23 | 4460 | 27143 | 63457396 |
Capillary leak syndrome | 36.03 | 23.58 | 11 | 4472 | 2189 | 63482350 |
Hyperparathyroidism secondary | 35.81 | 23.58 | 10 | 4473 | 1457 | 63483082 |
Hyperphosphataemia | 35.80 | 23.58 | 11 | 4472 | 2237 | 63482302 |
Altered state of consciousness | 35.13 | 23.58 | 22 | 4461 | 25208 | 63459331 |
Hypomagnesaemia | 34.92 | 23.58 | 23 | 4460 | 28714 | 63455825 |
Polymyalgia rheumatica | 33.92 | 23.58 | 12 | 4471 | 3779 | 63480760 |
Cerebral infarction | 33.68 | 23.58 | 21 | 4462 | 23872 | 63460667 |
Renal impairment | 33.44 | 23.58 | 36 | 4447 | 88319 | 63396220 |
Hypoparathyroidism | 33.00 | 23.58 | 8 | 4475 | 670 | 63483869 |
Blood phosphorus increased | 32.16 | 23.58 | 11 | 4472 | 3134 | 63481405 |
Eosinophilia | 32.07 | 23.58 | 20 | 4463 | 22736 | 63461803 |
Bladder sphincter atony | 31.48 | 23.58 | 6 | 4477 | 159 | 63484380 |
Diabetic metabolic decompensation | 29.93 | 23.58 | 9 | 4474 | 1701 | 63482838 |
Overdose | 28.84 | 23.58 | 38 | 4445 | 115040 | 63369499 |
Urine ketone body present | 26.56 | 23.58 | 9 | 4474 | 2494 | 63482045 |
Acetonaemia | 26.25 | 23.58 | 5 | 4478 | 132 | 63484407 |
Cutaneous lupus erythematosus | 25.85 | 23.58 | 9 | 4474 | 2703 | 63481836 |
Thrombocytosis | 25.59 | 23.58 | 11 | 4472 | 5807 | 63478732 |
Drug reaction with eosinophilia and systemic symptoms | 24.92 | 23.58 | 20 | 4463 | 33816 | 63450723 |
Thyroglobulin increased | 23.90 | 23.58 | 4 | 4479 | 49 | 63484490 |
Inflammatory marker increased | 23.88 | 23.58 | 11 | 4472 | 6828 | 63477711 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Pemphigoid | 881.43 | 20.47 | 215 | 5214 | 8451 | 34943051 |
Diabetes mellitus inadequate control | 80.27 | 20.47 | 40 | 5389 | 13424 | 34938078 |
Hyperglycaemia | 65.49 | 20.47 | 52 | 5377 | 39428 | 34912074 |
Cardiac failure | 62.81 | 20.47 | 74 | 5355 | 91174 | 34860328 |
Hypoglycaemia | 56.48 | 20.47 | 55 | 5374 | 54585 | 34896917 |
Acute kidney injury | 53.42 | 20.47 | 134 | 5295 | 304854 | 34646648 |
Cerebral infarction | 51.70 | 20.47 | 39 | 5390 | 27416 | 34924086 |
Euglycaemic diabetic ketoacidosis | 50.63 | 20.47 | 19 | 5410 | 3203 | 34948299 |
Glycosylated haemoglobin increased | 45.77 | 20.47 | 26 | 5403 | 11334 | 34940168 |
Ketonuria | 41.39 | 20.47 | 11 | 5418 | 600 | 34950902 |
Drug interaction | 38.11 | 20.47 | 98 | 5331 | 225848 | 34725654 |
Hyperkalaemia | 37.65 | 20.47 | 50 | 5379 | 69339 | 34882163 |
Interstitial lung disease | 36.90 | 20.47 | 48 | 5381 | 65234 | 34886268 |
Diabetic ketoacidosis | 34.79 | 20.47 | 26 | 5403 | 18006 | 34933496 |
MELAS syndrome | 32.62 | 20.47 | 6 | 5423 | 56 | 34951446 |
Lactic acidosis | 32.20 | 20.47 | 33 | 5396 | 34739 | 34916763 |
Bone marrow oedema | 31.23 | 20.47 | 9 | 5420 | 663 | 34950839 |
Pancreatic carcinoma | 27.07 | 20.47 | 17 | 5412 | 8884 | 34942618 |
Orbital oedema | 26.91 | 20.47 | 6 | 5423 | 155 | 34951347 |
Agnosia | 25.74 | 20.47 | 5 | 5424 | 64 | 34951438 |
Intercepted medication error | 24.48 | 20.47 | 7 | 5422 | 501 | 34951001 |
Anal incontinence | 23.89 | 20.47 | 15 | 5414 | 7834 | 34943668 |
Ketoacidosis | 23.50 | 20.47 | 12 | 5417 | 4231 | 34947271 |
Heart rate abnormal | 22.38 | 20.47 | 9 | 5420 | 1822 | 34949680 |
Blister | 21.71 | 20.47 | 22 | 5407 | 22836 | 34928666 |
Nervous system disorder | 21.64 | 20.47 | 18 | 5411 | 14525 | 34936977 |
Acetonaemia | 21.43 | 20.47 | 5 | 5424 | 159 | 34951343 |
Blister rupture | 21.02 | 20.47 | 5 | 5424 | 173 | 34951329 |
Eosinophilia | 20.92 | 20.47 | 23 | 5406 | 26199 | 34925303 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Pemphigoid | 1894.95 | 18.12 | 427 | 9498 | 14888 | 79719575 |
Lactic acidosis | 216.75 | 18.12 | 125 | 9800 | 70234 | 79664229 |
Acute kidney injury | 171.29 | 18.12 | 262 | 9663 | 519142 | 79215321 |
Hypoglycaemia | 147.64 | 18.12 | 113 | 9812 | 101481 | 79632982 |
Diabetes mellitus inadequate control | 116.58 | 18.12 | 58 | 9867 | 24206 | 79710257 |
Hyperglycaemia | 108.24 | 18.12 | 81 | 9844 | 70254 | 79664209 |
Hyperkalaemia | 90.48 | 18.12 | 90 | 9835 | 114308 | 79620155 |
Euglycaemic diabetic ketoacidosis | 88.58 | 18.12 | 33 | 9892 | 6811 | 79727652 |
Cerebral infarction | 84.87 | 18.12 | 59 | 9866 | 45617 | 79688846 |
Drug interaction | 77.72 | 18.12 | 164 | 9761 | 415019 | 79319444 |
Diabetic ketoacidosis | 75.19 | 18.12 | 49 | 9876 | 34073 | 79700390 |
Dermatitis bullous | 68.25 | 18.12 | 34 | 9891 | 14211 | 79720252 |
Glycosylated haemoglobin increased | 66.71 | 18.12 | 37 | 9888 | 19223 | 79715240 |
Ketoacidosis | 60.31 | 18.12 | 26 | 9899 | 7828 | 79726635 |
Interstitial lung disease | 55.16 | 18.12 | 69 | 9856 | 112531 | 79621932 |
Renal impairment | 50.78 | 18.12 | 79 | 9846 | 157704 | 79576759 |
Eosinophilia | 50.03 | 18.12 | 43 | 9882 | 45302 | 79689161 |
Crush syndrome | 49.60 | 18.12 | 10 | 9915 | 198 | 79734265 |
Altered state of consciousness | 49.26 | 18.12 | 42 | 9883 | 43780 | 79690683 |
Cardiac failure | 44.99 | 18.12 | 74 | 9851 | 154768 | 79579695 |
Acetonaemia | 44.64 | 18.12 | 10 | 9915 | 332 | 79734131 |
Toxicity to various agents | 41.00 | 18.12 | 3 | 9922 | 421537 | 79312926 |
Ketonuria | 40.71 | 18.12 | 12 | 9913 | 1196 | 79733267 |
Sensorimotor disorder | 39.65 | 18.12 | 11 | 9914 | 883 | 79733580 |
Polymyalgia rheumatica | 38.08 | 18.12 | 16 | 9909 | 4521 | 79729942 |
Urine ketone body present | 34.78 | 18.12 | 14 | 9911 | 3551 | 79730912 |
Thrombocytosis | 34.03 | 18.12 | 18 | 9907 | 8508 | 79725955 |
Pancreatitis acute | 33.69 | 18.12 | 36 | 9889 | 49568 | 79684895 |
Blister rupture | 33.66 | 18.12 | 9 | 9916 | 629 | 79733834 |
Blood glucose increased | 33.45 | 18.12 | 55 | 9870 | 114920 | 79619543 |
Hypomagnesaemia | 31.78 | 18.12 | 34 | 9891 | 46877 | 79687586 |
Pain | 31.45 | 18.12 | 25 | 9900 | 703777 | 79030686 |
Rhabdomyolysis | 30.90 | 18.12 | 50 | 9875 | 103081 | 79631382 |
Fatigue | 30.42 | 18.12 | 43 | 9882 | 929684 | 78804779 |
Compartment syndrome | 30.00 | 18.12 | 14 | 9911 | 5068 | 79729395 |
Bladder sphincter atony | 29.38 | 18.12 | 6 | 9919 | 127 | 79734336 |
Diabetic metabolic decompensation | 28.80 | 18.12 | 12 | 9913 | 3320 | 79731143 |
Cardiac failure acute | 27.31 | 18.12 | 21 | 9904 | 18908 | 79715555 |
MELAS syndrome | 26.70 | 18.12 | 6 | 9919 | 202 | 79734261 |
Language disorder | 25.86 | 18.12 | 11 | 9914 | 3203 | 79731260 |
Joint swelling | 25.53 | 18.12 | 3 | 9922 | 288643 | 79445820 |
Inflammatory marker increased | 25.07 | 18.12 | 16 | 9909 | 10724 | 79723739 |
Bone marrow oedema | 24.91 | 18.12 | 9 | 9916 | 1702 | 79732761 |
Headache | 24.73 | 18.12 | 27 | 9898 | 653745 | 79080718 |
Hypoparathyroidism | 24.70 | 18.12 | 8 | 9917 | 1090 | 79733373 |
Acute generalised exanthematous pustulosis | 24.59 | 18.12 | 19 | 9906 | 17235 | 79717228 |
Hyperparathyroidism secondary | 24.42 | 18.12 | 10 | 9915 | 2650 | 79731813 |
Pancreatic carcinoma | 23.95 | 18.12 | 17 | 9908 | 13560 | 79720903 |
Capillary leak syndrome | 23.75 | 18.12 | 11 | 9914 | 3914 | 79730549 |
Anal incontinence | 23.72 | 18.12 | 19 | 9906 | 18149 | 79716314 |
Shock | 23.43 | 18.12 | 28 | 9897 | 43520 | 79690943 |
Metabolic acidosis | 23.35 | 18.12 | 39 | 9886 | 82490 | 79651973 |
Contraindication to medical treatment | 23.34 | 18.12 | 8 | 9917 | 1298 | 79733165 |
Orbital oedema | 22.41 | 18.12 | 6 | 9919 | 421 | 79734042 |
Cholangitis acute | 22.09 | 18.12 | 8 | 9917 | 1524 | 79732939 |
Erythema multiforme | 22.07 | 18.12 | 18 | 9907 | 17633 | 79716830 |
Hyperphosphataemia | 21.39 | 18.12 | 12 | 9913 | 6364 | 79728099 |
Angina pectoris | 21.11 | 18.12 | 29 | 9896 | 51703 | 79682760 |
Agnosia | 20.89 | 18.12 | 5 | 9920 | 223 | 79734240 |
Drug reaction with eosinophilia and systemic symptoms | 20.40 | 18.12 | 32 | 9893 | 64212 | 79670251 |
Toxic skin eruption | 20.34 | 18.12 | 19 | 9906 | 22274 | 79712189 |
Arthralgia | 20.12 | 18.12 | 25 | 9900 | 571778 | 79162685 |
Shock haemorrhagic | 20.07 | 18.12 | 18 | 9907 | 20042 | 79714421 |
Cutaneous lupus erythematosus | 20.01 | 18.12 | 9 | 9916 | 2994 | 79731469 |
Cardiac failure chronic | 19.77 | 18.12 | 14 | 9911 | 11121 | 79723342 |
Nephrotic syndrome | 19.73 | 18.12 | 14 | 9911 | 11160 | 79723303 |
Thyroglobulin increased | 19.66 | 18.12 | 4 | 9921 | 83 | 79734380 |
Diabetes mellitus | 19.50 | 18.12 | 35 | 9890 | 78355 | 79656108 |
Glycosuria | 19.32 | 18.12 | 8 | 9917 | 2180 | 79732283 |
Neutrophilia | 18.94 | 18.12 | 12 | 9913 | 7939 | 79726524 |
Infusion related reaction | 18.92 | 18.12 | 3 | 9922 | 230234 | 79504229 |
Monoparesis | 18.67 | 18.12 | 9 | 9916 | 3502 | 79730961 |
Hypophosphataemia | 18.22 | 18.12 | 17 | 9908 | 19896 | 79714567 |
None
Source | Code | Description |
---|---|---|
ATC | A10BD08 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Combinations of oral blood glucose lowering drugs |
ATC | A10BH02 | 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 | D007004 | Hypoglycemic Agents |
MeSH PA | D011480 | Protease Inhibitors |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 6.1 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Dipeptidyl peptidase 4 | Enzyme | INHIBITOR | Ki | 8.52 | CHEMBL | DRUG LABEL | |||
Dipeptidyl peptidase 8 | Enzyme | Ki | 6.09 | CHEMBL | |||||
Dipeptidyl peptidase 9 | Enzyme | Ki | 7.17 | CHEMBL | |||||
Prolyl endopeptidase FAP | Enzyme | IC50 | 5.43 | CHEMBL | |||||
Dipeptidyl peptidase 9 | Unclassified | IC50 | 6.17 | CHEMBL | |||||
Dipeptidyl peptidase IV | Unclassified | Ki | 7.77 | CHEMBL | |||||
Prolyl endopeptidase FAP | Enzyme | IC50 | 4.28 | CHEMBL |
ID | Source |
---|---|
D07080 | KEGG_DRUG |
C1570906 | UMLSCUI |
CHEBI:135285 | CHEBI |
CHEMBL142703 | ChEMBL_ID |
DB04876 | DRUGBANK_ID |
D000077597 | MESH_DESCRIPTOR_UI |
6918537 | PUBCHEM_CID |
6310 | IUPHAR_LIGAND_ID |
8399 | INN_ID |
924914-75-0 | SECONDARY_CAS_RN |
I6B4B2U96P | UNII |
596554 | RXNORM |
012358 | NDDF |
428611002 | SNOMEDCT_US |
428807006 | SNOMEDCT_US |
LF7 | PDB_CHEM_ID |
None