insulin degludec Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4960 844439-96-9

Description:

MoleculeDescription

Synonyms:

  • insulin degludec
  • tresiba
  • NN1250
insulin degludec is a long-acting basal human insulin analog for subcutaneous injection, differs from human insulin in that the amino acid threonine in position B30 has been omitted and a side-chain consisting of glutamic acid and a C16 fatty acid has been attached
  • Molecular weight: 6104.04
  • Formula: C274H411N65O81S6
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 2356.52
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
40 U P
40 U P
40 U P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 25, 2015 FDA NOVO NORDISK INC
Jan. 21, 2013 EMA
Sept. 28, 2012 PMDA Novo Nordisk Pharma Ltd

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
Hypoglycaemia 746.86 17.43 290 7408 58723 53282645
Blood glucose increased 341.93 17.43 183 7515 77178 53264190
Diabetic ketoacidosis 305.58 17.43 113 7585 19802 53321566
Blood glucose decreased 156.33 17.43 70 7628 19946 53321422
Diabetes mellitus inadequate control 134.39 17.43 57 7641 14253 53327115
Blood glucose fluctuation 112.91 17.43 37 7661 4514 53336854
Diabetic neuropathy 109.10 17.43 35 7663 3992 53337376
Hyperglycaemia 91.06 17.43 62 7636 40022 53301346
Glycosylated haemoglobin increased 88.54 17.43 40 7658 11615 53329753
Hypoglycaemic coma 84.05 17.43 26 7672 2632 53338736
Hypoglycaemic unconsciousness 78.63 17.43 19 7679 759 53340609
Impaired gastric emptying 74.97 17.43 33 7665 9010 53332358
Diabetic retinopathy 57.21 17.43 19 7679 2413 53338955
Ketoacidosis 49.55 17.43 20 7678 4406 53336962
Heart sounds 48.64 17.43 12 7686 523 53340845
Retinopathy 43.22 17.43 16 7682 2796 53338572
Blood glucose abnormal 42.87 17.43 21 7677 7298 53334070
Prolonged expiration 41.82 17.43 11 7687 621 53340747
Taste disorder 38.30 17.43 20 7678 7948 53333420
Neuropathy peripheral 37.25 17.43 59 7639 103128 53238240
Hypoglycaemic encephalopathy 33.72 17.43 8 7690 295 53341073
Depressive symptom 30.61 17.43 13 7685 3251 53338117
Appetite disorder 30.24 17.43 16 7682 6527 53334841
Fear-related avoidance of activities 29.63 17.43 6 7692 104 53341264
Hypoglycaemic seizure 29.28 17.43 8 7690 522 53340846
Hypoglycaemia unawareness 29.21 17.43 6 7692 112 53341256
Acute painful neuropathy of rapid glycaemic control 29.14 17.43 4 7694 3 53341365
Sleep disorder due to a general medical condition 28.28 17.43 16 7682 7441 53333927
Diabetic metabolic decompensation 27.75 17.43 10 7688 1618 53339750
Intentional overdose 26.44 17.43 40 7658 67165 53274203
Suicide attempt 24.86 17.43 36 7662 58132 53283236
Carcinoid crisis 24.82 17.43 6 7692 240 53341128
Ketosis 24.29 17.43 7 7691 555 53340813
Respiration abnormal 24.11 17.43 13 7685 5505 53335863
Hyperkalaemia 23.80 17.43 34 7664 54222 53287146
Product prescribing error 21.06 17.43 21 7677 23010 53318358
Rales 20.50 17.43 15 7683 10817 53330551
Prerenal failure 20.43 17.43 8 7690 1626 53339742
Rheumatoid arthritis 20.34 17.43 10 7688 314521 53026847
Device failure 20.18 17.43 12 7686 6123 53335245
Presbyopia 19.90 17.43 6 7692 557 53340811
Retinal degeneration 19.46 17.43 6 7692 600 53340768
Thirst decreased 19.22 17.43 5 7693 270 53341098
Lactic acidosis 18.83 17.43 25 7673 37228 53304140
Erysipelas 18.26 17.43 12 7686 7289 53334079
Drug intolerance 17.68 17.43 4 7694 205489 53135879
Haemorrhagic disorder 17.66 17.43 6 7692 816 53340552

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
Hypoglycaemia 600.35 18.70 273 6807 54109 32452337
Appendicolith 249.86 18.70 69 7011 3096 32503350
Blood glucose increased 202.59 18.70 143 6937 65098 32441348
Appendicitis 179.48 18.70 69 7011 8868 32497578
Diabetic ketoacidosis 178.12 18.70 84 6996 17848 32488598
Cardiogenic shock 149.40 18.70 78 7002 20584 32485862
Blood glucose decreased 139.30 18.70 65 7015 13469 32492977
Stress 120.37 18.70 71 7009 23711 32482735
Ascites 110.60 18.70 82 6998 40109 32466337
Diabetes mellitus inadequate control 108.21 18.70 55 7025 13713 32492733
Abdominal distension 103.16 18.70 87 6993 51208 32455238
Hypoglycaemic unconsciousness 88.25 18.70 23 7057 823 32505623
Impaired gastric emptying 81.63 18.70 30 7050 3396 32503050
Multiple organ dysfunction syndrome 71.67 18.70 82 6998 69772 32436674
Glycosylated haemoglobin increased 68.75 18.70 37 7043 10352 32496094
Hyperglycaemia 60.95 18.70 57 7023 38334 32468112
General physical health deterioration 55.56 18.70 94 6986 115165 32391281
Hyponatraemia 53.24 18.70 73 7007 74440 32432006
Abdominal pain 50.87 18.70 105 6975 149424 32357022
Nausea 42.18 18.70 159 6921 320690 32185756
Constipation 39.76 18.70 86 6994 126287 32380159
Hypoglycaemic seizure 39.14 18.70 10 7070 330 32506116
Sepsis 37.89 18.70 97 6983 158737 32347709
Pancreatic carcinoma 37.33 18.70 23 7057 8283 32498163
Hypoglycaemia unawareness 36.43 18.70 8 7072 135 32506311
Ventricular fibrillation 33.99 18.70 29 7051 17281 32489165
Vomiting 33.62 18.70 120 6960 235437 32271009
Hypoglycaemic coma 32.33 18.70 14 7066 2429 32504017
Hyperkinetic heart syndrome 31.50 18.70 7 7073 125 32506321
Suicide attempt 31.17 18.70 40 7040 38204 32468242
Toxicity to various agents 28.18 18.70 3 7077 178038 32328408
Pancreatitis 28.15 18.70 38 7042 38113 32468333
Diabetic metabolic decompensation 27.59 18.70 11 7069 1551 32504895
Neuropathy peripheral 27.22 18.70 55 7025 76927 32429519
Oedematous pancreatitis 26.78 18.70 8 7072 474 32505972
Euglycaemic diabetic ketoacidosis 24.38 18.70 12 7068 2786 32503660
Ketoacidosis 22.53 18.70 13 7067 4151 32502295
Hypoglycaemic encephalopathy 21.11 18.70 6 7074 298 32506148
Diabetic foot 20.98 18.70 11 7069 2915 32503531
Blood glucose fluctuation 20.33 18.70 12 7068 3997 32502449
Blood glucose abnormal 19.02 18.70 13 7067 5575 32500871
Acute coronary syndrome 18.90 18.70 19 7061 13922 32492524

Pharmacologic Action:

SourceCodeDescription
ATC A10AD06 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
INSULINS AND ANALOGUES
Insulins and analogues for injection, intermediate- or long-acting combined with fast-acting
ATC A10AE06 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
INSULINS AND ANALOGUES
Insulins and analogues for injection, long-acting
ATC A10AE56 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
INSULINS AND ANALOGUES
Insulins and analogues for injection, long-acting
FDA CS M0011417 Insulin
FDA EPC N0000175453 Insulin Analog
CHEBI has role CHEBI:35526 hypoglycemic drug
FDA EPC N0000175944 Insulin

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus indication 73211009 DOID:9351

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Insulin receptor Kinase AGONIST DRUG LABEL DRUG LABEL

External reference:

IDSource
D09727 KEGG_DRUG
4017559 VANDF
4017569 VANDF
4019786 VANDF
4035011 VANDF
CHEBI:5931 CHEBI
CHEMBL2107869 ChEMBL_ID
C571886 MESH_SUPPLEMENTAL_RECORD_UI
9170 INN_ID
5186 INN_ID
DB09564 DRUGBANK_ID
54Q18076QB UNII
118984462 PUBCHEM_CID
118984375 PUBCHEM_CID
DB00030 DRUGBANK_ID
1670007 RXNORM
236826 MMSL
29260 MMSL
4885 MMSL
4886 MMSL
d00262 MMSL
d04369 MMSL
d08054 MMSL
000869 NDDF
000870 NDDF
006518 NDDF
015340 NDDF
126210001 SNOMEDCT_US
417423002 SNOMEDCT_US
420609005 SNOMEDCT_US
710281005 SNOMEDCT_US
715774000 SNOMEDCT_US
96367001 SNOMEDCT_US
C3491971 UMLSCUI
C0795635 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tresiba HUMAN PRESCRIPTION DRUG LABEL 1 0169-2550 INJECTION, SOLUTION 200 U SUBCUTANEOUS BLA 27 sections
Tresiba HUMAN PRESCRIPTION DRUG LABEL 1 0169-2660 INJECTION, SOLUTION 100 U SUBCUTANEOUS BLA 27 sections
Tresiba HUMAN PRESCRIPTION DRUG LABEL 1 0169-2662 INJECTION, SOLUTION 100 U SUBCUTANEOUS BLA 27 sections
Xultophy 100/3.6 HUMAN PRESCRIPTION DRUG LABEL 2 0169-2911 INJECTION, SOLUTION 100 [iU] SUBCUTANEOUS BLA 27 sections
Tresiba HUMAN PRESCRIPTION DRUG LABEL 1 50090-3491 INJECTION, SOLUTION 200 U SUBCUTANEOUS BLA 28 sections