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

Stem definitionDrug idCAS RN
Glucagon-like Peptide (GLP) analogues 4164 204656-20-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • saxenda
  • liraglutide [rDNA origin]
  • liraglutide rDNA origin
  • liraglutide [rNDA origin] injection
  • liraglutide
  • NN2211
  • victoza
  • liraglutide recombinant
An analog of GLUCAGON-LIKE PEPTIDE 1 and agonist of the GLUCAGON-LIKE PEPTIDE 1 RECEPTOR that is used as a HYPOGLYCEMIC AGENT and supplemental therapy in the treatment of DIABETES MELLITUS by patients who do not respond to METFORMIN.
  • Molecular weight: 3751.26
  • Formula: C172H265N43O51
  • CLOGP:
  • LIPINSKI: None
  • HAC: 94
  • HDO: 54
  • TPSA: 1513.76
  • ALOGS:
  • ROTB: 130

Drug dosage:

DoseUnitRoute
40 U P
1.50 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 6 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.01 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
CL (Clearance) 0.01 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) 8.10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 30, 2009 EMA
Jan. 25, 2010 FDA NOVO NORDISK INC

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
Pancreatitis 2167.04 15.37 766 17823 42861 46624612
Pancreatitis acute 624.29 15.37 267 18322 24605 46642868
Nausea 494.34 15.37 931 17658 686523 45980950
Pancreatic carcinoma 412.63 15.37 138 18451 6419 46661054
Diabetic ketoacidosis 330.57 15.37 156 18433 18054 46649419
Vomiting 269.39 15.37 569 18020 452225 46215248
Blood glucose increased 264.11 15.37 223 18366 71790 46595683
Lipase increased 254.67 15.37 104 18485 8499 46658974
Injection site urticaria 164.86 15.37 85 18504 11882 46655591
Eructation 155.78 15.37 70 18519 7225 46660248
Injection site rash 153.21 15.37 89 18500 15724 46651749
Weight decreased 148.38 15.37 285 18304 210564 46456909
Injection site erythema 128.19 15.37 153 18436 74274 46593199
Glycosylated haemoglobin increased 123.70 15.37 68 18521 10808 46656665
Pancreatic carcinoma metastatic 121.55 15.37 43 18546 2365 46665108
Abdominal pain 119.85 15.37 275 18314 229756 46437717
Diabetes mellitus inadequate control 111.39 15.37 68 18521 13146 46654327
Diarrhoea 109.89 15.37 476 18113 559126 46108347
Blood glucose decreased 109.75 15.37 77 18512 18815 46648658
Ketoacidosis 104.15 15.37 44 18545 3911 46663562
Hypoglycaemia 100.65 15.37 116 18473 54233 46613240
Injection site pruritus 100.38 15.37 100 18489 39643 46627830
Medullary thyroid cancer 94.16 15.37 19 18570 105 46667368
Cholelithiasis 93.42 15.37 95 18494 38586 46628887
Papillary thyroid cancer 87.00 15.37 32 18557 1969 46665504
Amylase increased 81.64 15.37 41 18548 5418 46662055
Lactic acidosis 81.36 15.37 83 18506 33826 46633647
Abdominal pain upper 75.81 15.37 174 18415 145131 46522342
Injection site reaction 72.06 15.37 92 18497 47757 46619716
Thyroid mass 68.50 15.37 31 18558 3250 46664223
Dehydration 63.17 15.37 172 18417 159368 46508105
Adenocarcinoma pancreas 59.88 15.37 21 18568 1125 46666348
Thyroid neoplasm 59.14 15.37 29 18560 3640 46663833
Euglycaemic diabetic ketoacidosis 58.37 15.37 24 18565 1992 46665481
Thyroid cancer 54.70 15.37 28 18561 3850 46663623
Rheumatoid arthritis 49.45 15.37 17 18572 240198 46427275
Decreased appetite 49.04 15.37 179 18410 193657 46473816
Drug dose titration not performed 48.87 15.37 14 18575 385 46667088
Drug ineffective 47.71 15.37 127 18462 677711 45989762
Acute kidney injury 46.94 15.37 202 18387 235653 46431820
Impaired gastric emptying 44.78 15.37 32 18557 8040 46659433
Constipation 43.37 15.37 160 18429 173937 46493536
Injection site haematoma 42.85 15.37 28 18561 6084 46661389
Pancreatic neoplasm 40.10 15.37 14 18575 740 46666733
Pyrexia 34.07 15.37 54 18535 348748 46318725
Flatulence 33.57 15.37 49 18540 28829 46638644
Neutropenia 33.37 15.37 8 18581 143196 46524277
Cholecystitis acute 33.15 15.37 26 18563 7512 46659961
Completed suicide 32.38 15.37 9 18580 145911 46521562
Drug titration error 31.33 15.37 11 18578 591 46666882
Pancreatic mass 31.18 15.37 12 18577 837 46666636
Death 30.86 15.37 54 18535 335494 46331979
Hyperglycaemia 30.37 15.37 52 18537 35019 46632454
Pancreatic enzymes increased 29.79 15.37 11 18578 684 46666789
Weight loss poor 29.59 15.37 12 18577 961 46666512
Pancreatic cyst 29.53 15.37 13 18576 1276 46666197
Joint swelling 26.10 15.37 17 18572 166056 46501417
Glycosylated haemoglobin decreased 25.43 15.37 9 18580 495 46666978
Cholecystitis 25.28 15.37 30 18559 14436 46653037
Haemoglobin decreased 25.03 15.37 10 18579 128939 46538534
Injection site pain 24.60 15.37 96 18493 107056 46560417
Abdominal distension 24.06 15.37 74 18515 73277 46594196
Mental disability 23.25 15.37 6 18583 110 46667363
Pancreatic carcinoma stage IV 23.07 15.37 5 18584 41 46667432
White blood cell count decreased 22.96 15.37 8 18581 112223 46555250
Goitre 22.61 15.37 18 18571 5313 46662160
Pneumonia 21.72 15.37 77 18512 376243 46291230
Disease progression 21.46 15.37 5 18584 91295 46576178
Pancytopenia 21.35 15.37 4 18585 85054 46582419
Pain 21.13 15.37 108 18481 476840 46190633
Pancreatic pseudocyst 20.61 15.37 8 18581 571 46666902
Lack of satiety 20.49 15.37 3 18586 0 46667473
Huerthle cell carcinoma 20.49 15.37 3 18586 0 46667473
Blood calcitonin increased 19.69 15.37 4 18585 23 46667450
Anaemia 19.37 15.37 46 18543 255733 46411740
Ductal adenocarcinoma of pancreas 19.01 15.37 5 18584 99 46667374
Pancreatitis necrotising 18.98 15.37 10 18579 1459 46666014
Cholangiocarcinoma 18.93 15.37 9 18580 1055 46666418
Febrile neutropenia 18.92 15.37 7 18582 94620 46572853
Hypoglycaemic unconsciousness 18.65 15.37 8 18581 738 46666735
Aerococcus urinae infection 18.41 15.37 3 18586 3 46667470
General physical health deterioration 17.98 15.37 12 18577 115757 46551716
Infusion related reaction 17.83 15.37 9 18580 101199 46566274
Genotype drug resistance test positive 17.47 15.37 7 18582 543 46666930
Injection site swelling 17.45 15.37 45 18544 40282 46627191
Dysgeusia 17.34 15.37 45 18544 40446 46627027
Thrombocytopenia 17.26 15.37 15 18574 126566 46540907
Blood glucose abnormal 17.22 15.37 17 18572 6655 46660818
Metastases to liver 16.90 15.37 29 18560 19556 46647917
Gastrooesophageal reflux disease 16.56 15.37 66 18523 74278 46593195
Respiratory failure 15.87 15.37 9 18580 94807 46572666
Anuria 15.67 15.37 21 18568 11410 46656063
Injection site nodule 15.63 15.37 12 18577 3359 46664114
Palpitations 15.49 15.37 77 18512 95182 46572291
Dyspepsia 15.42 15.37 61 18528 68411 46599062

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 1806.08 15.93 660 12897 35830 29903091
Pancreatitis acute 515.33 15.93 245 13312 25450 29913471
Pancreatic carcinoma 442.47 15.93 157 13400 7680 29931241
Nausea 333.26 15.93 527 13030 296430 29642491
Diabetic ketoacidosis 285.63 15.93 141 13416 15845 29923076
Lipase increased 218.31 15.93 97 13460 8579 29930342
Pancreatic carcinoma metastatic 205.96 15.93 71 13486 3176 29935745
Blood glucose increased 201.74 15.93 189 13368 61341 29877580
Glycosylated haemoglobin increased 167.31 15.93 83 13474 9408 29929513
Vomiting 156.33 15.93 321 13236 219497 29719424
Adenocarcinoma pancreas 114.74 15.93 37 13520 1341 29937580
Eructation 114.20 15.93 47 13510 3437 29935484
Abdominal pain 114.20 15.93 213 13344 135441 29803480
Diabetes mellitus inadequate control 113.07 15.93 71 13486 12691 29926230
Weight decreased 106.47 15.93 220 13337 150701 29788220
Lactic acidosis 92.86 15.93 91 13466 31122 29907799
Cholelithiasis 77.64 15.93 68 13489 20157 29918764
Injection site rash 71.52 15.93 34 13523 3505 29935416
Amylase increased 71.36 15.93 40 13517 5801 29933120
Pancreatic carcinoma stage IV 70.54 15.93 15 13542 96 29938825
Diarrhoea 68.38 15.93 315 13242 333788 29605133
Papillary thyroid cancer 65.00 15.93 20 13537 620 29938301
Hypoglycaemia 64.13 15.93 96 13461 50885 29888036
Toxicity to various agents 56.33 15.93 7 13550 177176 29761745
Ketoacidosis 55.06 15.93 29 13528 3717 29935204
Acute kidney injury 55.02 15.93 257 13300 273585 29665336
Thyroid cancer 54.60 15.93 21 13536 1284 29937637
Pancreatitis necrotising 51.31 15.93 24 13533 2385 29936536
Abdominal pain upper 49.70 15.93 96 13461 62455 29876466
Weight loss poor 49.25 15.93 12 13545 150 29938771
Medullary thyroid cancer 46.25 15.93 9 13548 34 29938887
Pancreatitis chronic 45.01 15.93 20 13537 1764 29937157
Injection site haematoma 44.79 15.93 19 13538 1498 29937423
Dyspepsia 43.79 15.93 61 13496 30268 29908653
Thyroid mass 43.68 15.93 13 13544 359 29938562
Pancreatic neoplasm 42.16 15.93 16 13541 943 29937978
Injection site pruritus 41.86 15.93 28 13529 5564 29933357
Gastrooesophageal reflux disease 40.90 15.93 61 13496 32194 29906727
Injection site erythema 40.48 15.93 40 13517 13794 29925127
Metastases to liver 39.55 15.93 37 13520 11928 29926993
Pneumonia 35.20 15.93 61 13496 334245 29604676
Pancreatic mass 33.35 15.93 13 13544 824 29938097
Death 31.75 15.93 72 13485 357211 29581710
Neutropenia 30.66 15.93 10 13547 128530 29810391
Abdominal discomfort 30.64 15.93 68 13489 48723 29890198
Dehydration 30.05 15.93 123 13434 123416 29815505
Completed suicide 29.10 15.93 5 13552 99487 29839434
Injection site urticaria 28.63 15.93 14 13543 1535 29937386
Cholangiocarcinoma 28.03 15.93 12 13545 967 29937954
Cholecystectomy 28.03 15.93 16 13541 2400 29936521
Febrile neutropenia 27.84 15.93 7 13550 106686 29832235
Tonsillar ulcer 27.67 15.93 8 13549 199 29938722
Pyrexia 27.24 15.93 58 13499 294431 29644490
Blood calcitonin increased 27.11 15.93 5 13552 13 29938908
Thyroid neoplasm 26.61 15.93 9 13548 379 29938542
Blood glucose decreased 26.32 15.93 31 13526 13022 29925899
Injection site reaction 25.86 15.93 28 13529 10732 29928189
Flatulence 25.47 15.93 36 13521 18093 29920828
Haemoglobin decreased 25.29 15.93 10 13547 114088 29824833
Thyroid adenoma 24.57 15.93 4 13553 3 29938918
Pancreatic pseudocyst 23.54 15.93 10 13547 791 29938130
Glycosylated haemoglobin decreased 23.27 15.93 8 13549 354 29938567
Decreased appetite 23.18 15.93 131 13426 149779 29789142
White blood cell count decreased 22.90 15.93 5 13552 83942 29854979
Pancreatic enzymes increased 22.68 15.93 9 13548 598 29938323
Platelet count decreased 22.40 15.93 10 13547 106119 29832802
Drug dose titration not performed 22.07 15.93 7 13550 240 29938681
Diabetic metabolic decompensation 21.44 15.93 11 13546 1335 29937586
Confusional state 21.12 15.93 18 13539 134816 29804105
Pancreatic cyst 20.50 15.93 9 13548 771 29938150
Ludwig angina 20.25 15.93 6 13551 163 29938758
Skin wound 20.25 15.93 7 13550 315 29938606
Acinar cell carcinoma of pancreas 20.10 15.93 3 13554 0 29938921
Cholecystitis chronic 19.81 15.93 9 13548 836 29938085
Thrombocytopenia 19.46 15.93 20 13537 137024 29801897
Extrasystoles 19.28 15.93 15 13542 3767 29935154
Impaired gastric emptying 19.19 15.93 14 13543 3192 29935729
Ketosis 19.10 15.93 7 13550 374 29938547
Supraventricular extrasystoles 19.04 15.93 14 13543 3230 29935691
Product use in unapproved indication 18.90 15.93 5 13552 73688 29865233
Intraductal papillary mucinous neoplasm 18.47 15.93 5 13552 97 29938824
Gallbladder disorder 17.23 15.93 17 13540 5850 29933071
Pancreatectomy 17.14 15.93 4 13553 41 29938880
Constipation 17.00 15.93 98 13459 112808 29826113
Cholecystitis acute 16.72 15.93 16 13541 5301 29933620
Abdominal distension 16.65 15.93 52 13505 45657 29893264
Catheter site cellulitis 16.60 15.93 5 13552 144 29938777
Follicular thyroid cancer 16.49 15.93 3 13554 7 29938914
Ductal adenocarcinoma of pancreas 16.34 15.93 4 13553 51 29938870

Pharmacologic Action:

SourceCodeDescription
ATC A10AE56 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
INSULINS AND ANALOGUES
Insulins and analogues for injection, long-acting
ATC A10BJ02 ALIMENTARY TRACT AND METABOLISM
DRUGS USED IN DIABETES
BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
Glucagon-like peptide-1 (GLP-1) analogues
FDA CS M0160181 Glucagon-Like Peptide 1
FDA MoA N0000020058 Glucagon-like Peptide-1 (GLP-1) Agonists
FDA EPC N0000178480 GLP-1 Receptor Agonist
MeSH PA D006728 Hormones
MeSH PA D007004 Hypoglycemic Agents
MeSH PA D054795 Incretins
CHEBI has role CHEBI:63726 neuroprotective agents
CHEBI has role CHEBI:71196 glucagon-like peptide-1 receptor agonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352
Weight loss indication 89362005
Disorder of thyroid gland contraindication 14304000 DOID:50
Multiple endocrine neoplasia, type 2 contraindication 61808009
Pancreatitis contraindication 75694006 DOID:4989
C-cell hyperplasia of thyroid contraindication 237552009
Hypoglycemic disorder contraindication 237630007
Medullary thyroid carcinoma contraindication 255032005 DOID:3973
Pregnancy, function contraindication 289908002
Breastfeeding (mother) contraindication 413712001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.06 acidic
pKa2 3.31 acidic
pKa3 3.67 acidic
pKa4 3.82 acidic
pKa5 4.11 acidic
pKa6 4.44 acidic
pKa7 9.65 acidic
pKa8 11.84 acidic
pKa9 12.2 acidic
pKa10 12.53 acidic
pKa11 12.59 acidic
pKa12 12.81 acidic
pKa13 12.86 acidic
pKa14 12.94 acidic
pKa15 13.1 acidic
pKa16 13.15 acidic
pKa17 13.2 acidic
pKa18 13.29 acidic
pKa19 13.43 acidic
pKa20 13.56 acidic
pKa21 13.56 acidic
pKa22 13.6 acidic
pKa23 13.71 acidic
pKa24 13.82 acidic
pKa25 13.82 acidic
pKa26 13.96 acidic
pKa27 13.97 acidic
pKa28 11.05 Basic
pKa29 10.45 Basic
pKa30 7.87 Basic
pKa31 5.98 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
18MG/3ML (6MG/ML) VICTOZA NOVO NORDISK INC N022341 Jan. 25, 2010 RX SOLUTION SUBCUTANEOUS June 17, 2022 NEW PATIENT POPULATION
18MG/3ML (6MG/ML) VICTOZA NOVO NORDISK INC N022341 Jan. 25, 2010 RX SOLUTION SUBCUTANEOUS Dec. 17, 2022 PEDIATRIC EXCLUSIVITY
18MG/3ML (6MG/ML) SAXENDA NOVO N206321 Dec. 23, 2014 RX SOLUTION SUBCUTANEOUS Dec. 4, 2023 NEW PATIENT POPULATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glucagon-like peptide 1 receptor GPCR AGONIST EC50 10.20 WOMBAT-PK CHEMBL

External reference:

IDSource
D06404 KEGG_DRUG
4029703 VANDF
C1456408 UMLSCUI
CHEBI:71193 CHEBI
CHEMBL4524066 ChEMBL_ID
CHEMBL1201866 ChEMBL_ID
D000069450 MESH_DESCRIPTOR_UI
DB06655 DRUGBANK_ID
1133 IUPHAR_LIGAND_ID
8208 INN_ID
839I73S42A UNII
16134956 PUBCHEM_CID
1598264 RXNORM
166619 MMSL
232503 MMSL
26647 MMSL
d07466 MMSL
010773 NDDF
444828003 SNOMEDCT_US
444907006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Saxenda HUMAN PRESCRIPTION DRUG LABEL 1 0169-2800 INJECTION, SOLUTION 6 mg SUBCUTANEOUS NDA 28 sections
Xultophy 100/3.6 HUMAN PRESCRIPTION DRUG LABEL 2 0169-2911 INJECTION, SOLUTION 3.60 mg SUBCUTANEOUS BLA 27 sections
Victoza HUMAN PRESCRIPTION DRUG LABEL 1 0169-4060 INJECTION 6 mg SUBCUTANEOUS NDA 28 sections
Victoza HUMAN PRESCRIPTION DRUG LABEL 1 50090-2853 INJECTION 6 mg SUBCUTANEOUS NDA 28 sections
Saxenda HUMAN PRESCRIPTION DRUG LABEL 1 50090-4257 INJECTION, SOLUTION 6 mg SUBCUTANEOUS NDA 28 sections
Victoza HUMAN PRESCRIPTION DRUG LABEL 1 50090-4503 INJECTION 6 mg SUBCUTANEOUS NDA 28 sections