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

Stem definitionDrug idCAS RN
muscarinic receptors agonists/antagonists 4816 869113-09-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • incruse
  • umeclidinium
  • GSK573719A
  • umeclidinium bromide
a long-acting antimuscarinic agent with similar affinity to the subtypes of muscarinic receptors M1 to M5, in the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation
  • Molecular weight: 428.60
  • Formula: C29H34NO2
  • CLOGP: 1.60
  • LIPINSKI: 0
  • HAC: 3
  • HDO: 1
  • TPSA: 29.46
  • ALOGS: -7.38
  • ROTB: 8
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
55 mcg Inhal.powder

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1.23 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 35.95 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.11 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 19 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 0.13 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK7,NTRK2,PDK2,PDK4,PRKDC,TEK,TGFBR1 22
kinase-selectivity-class AXL,ERBB2,GRK2,PDK4,PIK3CD 5
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Dec. 18, 2013 FDA GLAXOSMITHKLINE
July 4, 2014 PMDA GLAXOSMITHKLINE K.K.
March 20, 2017 EMA GlaxoSmithKline Trading Services Limited

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
Nasal polyps 522.32 24.09 147 12962 10733 90604605
Wheezing 433.17 24.09 321 12788 237759 90377579
Obstructive airways disorder 408.22 24.09 150 12959 25719 90589619
Asthma-chronic obstructive pulmonary disease overlap syndrome 396.05 24.09 100 13009 4799 90610539
Total lung capacity increased 378.85 24.09 97 13012 4924 90610414
Chronic obstructive pulmonary disease 331.73 24.09 177 12932 73652 90541686
Asthma 328.92 24.09 275 12834 241885 90373453
Sarcoidosis 306.52 24.09 97 13012 10576 90604762
Rhinitis allergic 282.08 24.09 102 13007 16683 90598655
Bronchiectasis 274.69 24.09 108 13001 22222 90593116
Full blood count abnormal 263.45 24.09 121 12988 36476 90578862
Cardiac murmur 263.11 24.09 99 13010 18095 90597243
Lung neoplasm malignant 232.10 24.09 98 13011 24175 90591163
Gastrooesophageal reflux disease 205.21 24.09 179 12930 166158 90449180
Hypomania 195.32 24.09 66 13043 8831 90606507
Cough 192.48 24.09 251 12858 368711 90246627
Jaundice cholestatic 183.67 24.09 65 13044 9978 90605360
Sputum discoloured 164.38 24.09 73 13036 20318 90595020
Dyspnoea 162.88 24.09 378 12731 880577 89734761
Schizophrenia 158.67 24.09 65 13044 14849 90600489
Oedema peripheral 157.50 24.09 190 12919 257725 90357613
Dyspnoea exertional 152.66 24.09 107 13002 72181 90543157
Therapeutic product effect incomplete 150.84 24.09 162 12947 193734 90421604
Productive cough 137.50 24.09 103 13006 76960 90538378
Salpingo-oophorectomy unilateral 131.19 24.09 30 13079 938 90614400
Sputum increased 128.51 24.09 37 13072 2920 90612418
Sinusitis fungal 124.24 24.09 33 13076 1931 90613407
Psychotic disorder 121.06 24.09 68 13041 31162 90584176
Respiratory symptom 115.25 24.09 37 13072 4215 90611123
Loss of personal independence in daily activities 113.36 24.09 118 12991 135987 90479351
Sleep disorder due to a general medical condition 112.96 24.09 74 13035 44664 90570674
Embolism venous 112.65 24.09 35 13074 3585 90611753
Hiatus hernia 103.15 24.09 57 13052 25304 90590034
Sputum purulent 96.49 24.09 25 13084 1327 90614011
Diastolic dysfunction 95.53 24.09 37 13072 7296 90608042
Blood bilirubin increased 93.25 24.09 65 13044 43405 90571933
Cholelithiasis 93.22 24.09 70 13039 52436 90562902
Nicotine dependence 92.64 24.09 23 13086 1027 90614311
Hepatotoxicity 90.13 24.09 65 13044 45777 90569561
Emphysema 86.80 24.09 40 13069 12115 90603223
Chest discomfort 82.75 24.09 101 13008 138264 90477074
Sleep apnoea syndrome 74.06 24.09 50 13059 31697 90583641
Venous pressure jugular increased 72.82 24.09 17 13092 583 90614755
Secondary immunodeficiency 72.27 24.09 22 13087 2104 90613234
Osteoporosis 72.04 24.09 79 13030 96452 90518886
Diverticulum 71.60 24.09 35 13074 12078 90603260
Kyphosis 69.48 24.09 23 13086 2885 90612453
Tricuspid valve incompetence 69.11 24.09 38 13071 16693 90598645
Eczema 61.25 24.09 55 13054 52815 90562523
Hysterectomy 61.16 24.09 31 13078 11553 90603785
Analgesic therapy 60.69 24.09 15 13094 657 90614681
Antacid therapy 58.98 24.09 15 13094 739 90614599
Appendicolith 58.84 24.09 15 13094 746 90614592
Female genital tract fistula 58.83 24.09 35 13074 17833 90597505
Blood test abnormal 58.65 24.09 37 13072 20915 90594423
Drug therapy 57.93 24.09 15 13094 794 90614544
Anticoagulant therapy 57.78 24.09 15 13094 802 90614536
Iron deficiency anaemia 56.94 24.09 38 13071 23624 90591714
Disease recurrence 55.53 24.09 45 13064 37608 90577730
Pneumonia 53.82 24.09 208 12901 637851 89977487
Candida infection 50.86 24.09 41 13068 34016 90581322
Rectal prolapse 50.46 24.09 17 13092 2250 90613088
Chronic sinusitis 49.65 24.09 35 13074 23767 90591571
Aortic stenosis 48.86 24.09 22 13087 6314 90609024
Bundle branch block left 44.27 24.09 22 13087 7863 90607475
Infusion related reaction 42.95 24.09 5 13104 416775 90198563
Impaired quality of life 41.37 24.09 31 13078 23113 90592225
Gastroenteritis bacterial 41.03 24.09 10 13099 413 90614925
Systemic lupus erythematosus 40.86 24.09 3 13106 361893 90253445
Arthropathy 38.73 24.09 4 13105 366238 90249100
Pneumococcal infection 38.58 24.09 12 13097 1233 90614105
Alopecia 38.31 24.09 12 13097 495059 90120279
Upper-airway cough syndrome 38.09 24.09 25 13084 15110 90600228
Chorea 36.08 24.09 13 13096 2097 90613241
Rheumatoid arthritis 35.78 24.09 5 13104 362609 90252729
Hyperphosphataemia 35.50 24.09 15 13094 3696 90611642
Glossodynia 35.39 24.09 3 13106 321776 90293562
Blood phosphorus increased 33.31 24.09 15 13094 4303 90611035
Swelling 32.69 24.09 10 13099 419048 90196290
Pulmonary embolism 30.57 24.09 62 13047 130758 90484580
Wound 30.31 24.09 4 13105 302976 90312362
Fungal infection 30.22 24.09 34 13075 42627 90572711
End stage renal disease 28.76 24.09 17 13092 8554 90606784
Tooth injury 28.65 24.09 10 13099 1471 90613867
Radioallergosorbent test positive 28.57 24.09 5 13104 37 90615301
Pain 26.81 24.09 66 13043 996275 89619063
Respiratory gas exchange disorder 26.48 24.09 7 13102 402 90614936
Cockroach allergy 25.36 24.09 5 13104 75 90615263
Blood uric acid increased 25.12 24.09 15 13094 7689 90607649
Activated partial thromboplastin time prolonged 24.90 24.09 15 13094 7810 90607528
Rash 24.45 24.09 49 13060 796051 89819287
Illness 24.29 24.09 43 13066 81926 90533412
Exposure during pregnancy 24.20 24.09 3 13106 238407 90376931

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
Asthma 700.35 35.52 387 16793 61927 42542228
Obstructive airways disorder 635.69 35.52 271 16909 24488 42579667
Wheezing 544.14 35.52 314 16866 54467 42549688
Full blood count abnormal 509.80 35.52 246 16934 29630 42574525
Therapeutic product effect incomplete 491.23 35.52 323 16857 70616 42533539
Appendicolith 387.62 35.52 160 17020 13296 42590859
Appendicitis 328.19 35.52 162 17018 20451 42583704
Loss of personal independence in daily activities 306.45 35.52 211 16969 49605 42554550
Neuritis 286.23 35.52 104 17076 6116 42598039
Pulmonary vasculitis 281.77 35.52 103 17077 6163 42597992
Sleep disorder due to a general medical condition 265.45 35.52 133 17047 17320 42586835
Respiratory symptom 263.13 35.52 115 17065 10991 42593164
Eosinophilic granulomatosis with polyangiitis 253.05 35.52 104 17076 8534 42595621
Cardiogenic shock 240.64 35.52 160 17020 35480 42568675
Neurological symptom 238.46 35.52 104 17076 9887 42594268
Bronchial wall thickening 236.55 35.52 63 17117 1297 42602858
Vasculitis 221.87 35.52 120 17060 18274 42585881
Stress 218.44 35.52 164 17016 44048 42560107
Ventricular fibrillation 214.91 35.52 140 17040 29983 42574172
Blood phosphorus increased 209.92 35.52 102 17078 12423 42591732
Total lung capacity abnormal 207.06 35.52 75 17105 4368 42599787
Productive cough 204.49 35.52 168 17012 51399 42552756
Pulmonary alveolar haemorrhage 202.28 35.52 105 17075 14711 42589444
Forced expiratory volume decreased 200.40 35.52 85 17095 7545 42596610
Pulmonary function test abnormal 194.02 35.52 63 17117 2631 42601524
Right atrial hypertrophy 186.31 35.52 46 17134 691 42603464
Mycotic allergy 185.57 35.52 71 17109 4820 42599335
Ascites 182.69 35.52 164 17016 56514 42547641
Spirometry abnormal 178.53 35.52 70 17110 5076 42599079
Mite allergy 176.33 35.52 69 17111 4977 42599178
Dust allergy 176.12 35.52 70 17110 5262 42598893
Conjunctivitis allergic 169.14 35.52 70 17110 5841 42598314
Pulmonary fibrosis 166.20 35.52 114 17066 26567 42577588
Iron deficiency 161.41 35.52 82 17098 10979 42593176
Abdominal distension 158.86 35.52 169 17011 71566 42532589
Myasthenia gravis 155.80 35.52 91 17089 16046 42588109
Antineutrophil cytoplasmic antibody positive 153.62 35.52 60 17120 4305 42599850
Right ventricular hypertrophy 152.38 35.52 46 17134 1506 42602649
Bronchial secretion retention 150.80 35.52 46 17134 1561 42602594
Lung disorder 147.19 35.52 135 17045 47788 42556367
Normochromic normocytic anaemia 140.72 35.52 70 17110 8961 42595194
Thrombosis 140.47 35.52 155 17025 68356 42535799
Chronic obstructive pulmonary disease 140.26 35.52 149 17031 62965 42541190
Blood uric acid increased 135.29 35.52 82 17098 15465 42588690
Hyperphosphataemia 129.95 35.52 75 17105 12929 42591226
Sleep disorder 127.68 35.52 125 17055 47970 42556185
Obstruction 124.75 35.52 47 17133 3056 42601099
Dyspnoea 122.34 35.52 423 16757 442198 42161957
Aortic valve stenosis 122.17 35.52 46 17134 2986 42601169
Nodule 121.82 35.52 71 17109 12463 42591692
Hypothyroidism 119.75 35.52 101 17079 31983 42572172
Haemoptysis 118.85 35.52 118 17062 46049 42558106
Hyponatraemia 116.47 35.52 172 17008 101290 42502865
Multiple organ dysfunction syndrome 115.00 35.52 167 17013 96868 42507287
Dry mouth 112.14 35.52 107 17073 39772 42564383
Bronchiectasis 109.84 35.52 76 17104 17943 42586212
Blood cholesterol increased 107.73 35.52 88 17092 26653 42577502
Chest X-ray abnormal 101.30 35.52 45 17135 4463 42599692
Bronchopulmonary aspergillosis allergic 100.44 35.52 45 17135 4553 42599602
Arteriosclerosis coronary artery 98.22 35.52 72 17108 18605 42585550
Incorrect route of product administration 97.94 35.52 80 17100 24225 42579930
Hypophosphataemia 97.39 35.52 75 17105 20870 42583285
Sleep disorder therapy 97.34 35.52 50 17130 6844 42597311
Analgesic therapy 97.02 35.52 49 17131 6475 42597680
Blood test abnormal 96.94 35.52 62 17118 12844 42591311
Gout 95.90 35.52 84 17096 27971 42576184
Neuralgia 94.18 35.52 80 17100 25567 42578588
Capillaritis 94.13 35.52 35 17145 2193 42601962
Arteriosclerosis 93.82 35.52 69 17111 17920 42586235
Drug therapy 92.19 35.52 47 17133 6333 42597822
Anxiety 87.65 35.52 165 17015 118395 42485760
Diastolic dysfunction 85.38 35.52 46 17134 6937 42597218
Bacterial infection 84.49 35.52 78 17102 27801 42576354
Coagulation factor deficiency 83.89 35.52 20 17160 257 42603898
Intervertebral disc degeneration 83.08 35.52 46 17134 7321 42596834
Toxicity to various agents 79.31 35.52 3 17177 229133 42375022
Diarrhoea 78.98 35.52 44 17136 460805 42143350
General physical health deterioration 78.45 35.52 182 16998 151064 42453091
Benign prostatic hyperplasia 75.92 35.52 65 17115 20987 42583168
Condition aggravated 74.99 35.52 253 16927 260501 42343654
Coagulation factor V level abnormal 72.39 35.52 16 17164 143 42604012
Pulmonary embolism 72.22 35.52 153 17027 119459 42484696
Cough 72.09 35.52 195 16985 177908 42426247
Blood immunoglobulin E increased 71.36 35.52 33 17147 3592 42600563
Factor V Leiden mutation 71.12 35.52 17 17163 221 42603934
Hypoxia 66.96 35.52 109 17071 69677 42534478
Constipation 65.97 35.52 178 17002 162113 42442042
Swelling 62.82 35.52 93 17087 54792 42549363
Sleep apnoea syndrome 56.99 35.52 56 17124 21552 42582603
Asthma-chronic obstructive pulmonary disease overlap syndrome 56.87 35.52 22 17158 1537 42602618
Osteoporosis 55.74 35.52 47 17133 14859 42589296
Breath sounds abnormal 55.54 35.52 43 17137 12050 42592105
Multiple allergies 55.42 35.52 28 17152 3700 42600455
Pulmonary function test decreased 54.44 35.52 32 17148 5700 42598455
Neutropenia 54.08 35.52 8 17172 199423 42404732
Pyrexia 52.56 35.52 49 17131 393993 42210162
Acute kidney injury 52.22 35.52 43 17137 367294 42236861
Abdominal pain 52.19 35.52 182 16998 190289 42413866
Diabetes mellitus 51.17 35.52 89 17091 59998 42544157
Hypoacusis 50.31 35.52 49 17131 18653 42585502
Anticoagulant therapy 50.26 35.52 28 17152 4507 42599648
Pleural thickening 49.94 35.52 15 17165 482 42603673
Inspiratory capacity abnormal 49.70 35.52 11 17169 99 42604056
Antacid therapy 49.23 35.52 28 17152 4689 42599466
Eosinophil count increased 46.68 35.52 37 17143 10726 42593429
Pain in extremity 46.63 35.52 150 17030 150454 42453701
Thrombocytopenia 46.46 35.52 10 17170 190269 42413886
Bacteroides infection 46.14 35.52 22 17158 2565 42601590
Rash 45.12 35.52 28 17152 276926 42327229
Sepsis 44.21 35.52 178 17002 199156 42404999
Drug intolerance 44.07 35.52 99 17081 80325 42523830
Diaphragmatic disorder 43.48 35.52 17 17163 1222 42602933
Febrile neutropenia 42.88 35.52 11 17169 185692 42418463
Asthenia 39.70 35.52 33 17147 280760 42323395
Activated partial thromboplastin time prolonged 39.68 35.52 40 17140 15863 42588292
Intentional product misuse 39.42 35.52 81 17099 61819 42542336
Aortic stenosis 37.79 35.52 30 17150 8715 42595440
Drug ineffective 37.39 35.52 130 17050 630067 41974088
Seizure 37.30 35.52 3 17177 120558 42483597
Ulcer 36.78 35.52 39 17141 16402 42587753
Platelet count decreased 36.55 35.52 6 17174 138575 42465580
Disease progression 36.19 35.52 7 17173 143649 42460506
Dehydration 35.52 35.52 7 17173 141760 42462395

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
Obstructive airways disorder 1029.74 24.82 403 28214 45746 110514936
Wheezing 750.86 24.82 580 28037 254650 110306032
Full blood count abnormal 748.89 24.82 340 28277 55712 110504970
Asthma 725.80 24.82 564 28053 249727 110310955
Appendicolith 500.75 24.82 174 28443 14081 110546601
Therapeutic product effect incomplete 478.36 24.82 423 28194 223382 110337300
Chronic obstructive pulmonary disease 455.07 24.82 307 28310 108851 110451831
Respiratory symptom 410.29 24.82 152 28465 14793 110545889
Nasal polyps 402.28 24.82 145 28472 13055 110547627
Asthma-chronic obstructive pulmonary disease overlap syndrome 401.20 24.82 121 28496 6223 110554459
Appendicitis 390.43 24.82 176 28441 28288 110532394
Bronchiectasis 348.76 24.82 176 28441 36317 110524365
Loss of personal independence in daily activities 341.21 24.82 294 28323 149726 110410956
Productive cough 329.13 24.82 257 28360 114048 110446634
Pulmonary vasculitis 325.86 24.82 104 28513 6456 110554226
Total lung capacity increased 321.09 24.82 97 28520 5015 110555667
Neuritis 317.57 24.82 105 28512 7294 110553388
Sleep disorder due to a general medical condition 295.24 24.82 178 28439 51934 110508748
Eosinophilic granulomatosis with polyangiitis 290.78 24.82 108 28509 10578 110550104
Blood phosphorus increased 275.94 24.82 117 28500 16223 110544459
Cardiogenic shock 269.65 24.82 174 28443 57164 110503518
Ventricular fibrillation 244.08 24.82 145 28472 41168 110519514
Total lung capacity abnormal 241.46 24.82 76 28541 4507 110556175
Neurological symptom 241.31 24.82 105 28512 15503 110545179
Sarcoidosis 239.08 24.82 98 28519 12481 110548201
Ascites 229.56 24.82 191 28426 92617 110468065
Mite allergy 219.92 24.82 75 28542 5728 110554954
Pulmonary alveolar haemorrhage 218.67 24.82 106 28511 20044 110540638
Dyspnoea 218.63 24.82 704 27913 1106168 109454514
Rhinitis allergic 218.06 24.82 102 28515 17820 110542862
Forced expiratory volume decreased 214.71 24.82 92 28525 13084 110547598
Spirometry abnormal 208.14 24.82 71 28546 5426 110555256
Cough 207.91 24.82 403 28214 461238 110099444
Pulmonary function test abnormal 206.75 24.82 69 28548 4931 110555751
Mycotic allergy 206.43 24.82 72 28545 5882 110554800
Dust allergy 205.87 24.82 72 28545 5929 110554753
Vasculitis 204.34 24.82 123 28494 35750 110524932
Bronchial wall thickening 193.47 24.82 59 28558 3148 110557534
Right atrial hypertrophy 192.96 24.82 43 28574 648 110560034
Conjunctivitis allergic 192.05 24.82 71 28546 6860 110553822
Gastrooesophageal reflux disease 190.94 24.82 234 28383 179742 110380940
Hyperphosphataemia 189.36 24.82 90 28527 16291 110544391
Stress 189.32 24.82 181 28436 105167 110455515
Myasthenia gravis 185.94 24.82 97 28520 21414 110539268
Blood uric acid increased 185.86 24.82 97 28520 21432 110539250
Cardiac murmur 179.09 24.82 99 28518 24529 110536153
Diastolic dysfunction 177.37 24.82 79 28538 12325 110548357
Sputum discoloured 175.34 24.82 102 28515 27843 110532839
Antineutrophil cytoplasmic antibody positive 174.50 24.82 61 28556 5015 110555667
Iron deficiency 173.22 24.82 88 28529 18388 110542294
Abdominal distension 168.73 24.82 217 28400 174886 110385796
Analgesic therapy 163.55 24.82 64 28553 7220 110553462
Thrombosis 162.56 24.82 169 28448 108493 110452189
Blood test abnormal 160.28 24.82 97 28520 28457 110532225
Drug therapy 156.47 24.82 62 28555 7229 110553453
Right ventricular hypertrophy 154.04 24.82 43 28574 1676 110559006
Hypomania 152.34 24.82 67 28550 10143 110550539
Normochromic normocytic anaemia 148.67 24.82 71 28546 12986 110547696
Lung neoplasm malignant 147.58 24.82 98 28519 33744 110526938
Gout 143.04 24.82 99 28518 36467 110524215
Haemoptysis 140.45 24.82 129 28488 71225 110489457
Multiple organ dysfunction syndrome 135.24 24.82 181 28436 151529 110409153
Sleep disorder therapy 134.49 24.82 56 28561 7415 110553267
Dyspnoea exertional 131.39 24.82 148 28469 103912 110456770
Pulmonary embolism 130.76 24.82 214 28403 214260 110346422
Jaundice cholestatic 126.60 24.82 66 28551 14542 110546140
Obstruction 120.25 24.82 48 28569 5704 110554978
Sleep apnoea syndrome 118.56 24.82 92 28525 40355 110520327
Bronchopulmonary aspergillosis allergic 115.15 24.82 52 28565 8374 110552308
Salpingo-oophorectomy unilateral 113.45 24.82 29 28588 802 110559880
Arteriosclerosis coronary artery 110.14 24.82 73 28544 25045 110535637
Hypophosphataemia 109.46 24.82 81 28536 33101 110527581
Bronchial secretion retention 108.78 24.82 43 28574 4981 110555701
Bacterial infection 108.09 24.82 92 28525 45944 110514738
Schizophrenia 106.92 24.82 68 28549 21758 110538924
Capillaritis 106.20 24.82 35 28582 2404 110558278
Anticoagulant therapy 106.07 24.82 43 28574 5318 110555364
Antacid therapy 105.13 24.82 43 28574 5441 110555241
Benign prostatic hyperplasia 105.05 24.82 63 28554 18171 110542511
Arteriosclerosis 103.84 24.82 70 28547 24697 110535985
Osteoporosis 103.32 24.82 120 28497 87032 110473650
Hypothyroidism 99.45 24.82 108 28509 72791 110487891
Aortic valve stenosis 99.05 24.82 43 28574 6307 110554375
Neuralgia 98.03 24.82 89 28528 48389 110512293
Nodule 95.15 24.82 74 28543 32557 110528125
Oedema peripheral 94.45 24.82 240 28377 328420 110232262
Aortic stenosis 93.57 24.82 52 28565 13007 110547675
Sinusitis fungal 90.86 24.82 32 28585 2688 110557994
Chest discomfort 90.79 24.82 162 28455 173686 110386996
Hyponatraemia 89.25 24.82 183 28434 217470 110343212
Chest X-ray abnormal 84.16 24.82 42 28575 8445 110552237
Pulmonary fibrosis 83.72 24.82 117 28500 101925 110458757
Coagulation factor deficiency 83.67 24.82 19 28598 313 110560369
Sputum increased 83.41 24.82 37 28580 5714 110554968
Infusion related reaction 78.88 24.82 5 28612 381157 110179525
Embolism venous 78.30 24.82 34 28583 4989 110555693
Lung disorder 78.11 24.82 155 28462 179892 110380790
Sputum purulent 77.70 24.82 26 28591 1872 110558810
Condition aggravated 76.70 24.82 384 28233 734452 109826230
Activated partial thromboplastin time prolonged 74.66 24.82 55 28562 22313 110538369
Nicotine dependence 73.99 24.82 23 28594 1308 110559374
Toxicity to various agents 73.73 24.82 17 28600 480538 110080144
Hypoxia 73.20 24.82 125 28492 129390 110431292
Coagulation factor V level abnormal 72.88 24.82 15 28602 151 110560531
Diabetes mellitus 72.81 24.82 108 28509 99273 110461409
Incorrect route of product administration 72.25 24.82 86 28531 63975 110496707
Constipation 72.21 24.82 230 28387 357556 110203126
Rash 70.84 24.82 65 28552 820899 109739783
Hiatus hernia 70.65 24.82 58 28559 27548 110533134
End stage renal disease 69.88 24.82 52 28565 21421 110539261
Factor V Leiden mutation 69.88 24.82 16 28601 274 110560408
Blood immunoglobulin E increased 68.27 24.82 35 28582 7447 110553235
Diarrhoea 67.52 24.82 120 28497 1139385 109421297
Pulmonary function test decreased 60.57 24.82 34 28583 8666 110552016
Alopecia 59.86 24.82 11 28606 364742 110195940
Intervertebral disc degeneration 59.31 24.82 44 28573 18041 110542641
Treatment failure 59.30 24.82 3 28614 277231 110283451
Pain 58.87 24.82 98 28519 954857 109605825
Drug interaction 58.75 24.82 28 28589 500155 110060527
Total lung capacity decreased 58.39 24.82 31 28586 7083 110553599
Pyrexia 58.36 24.82 89 28528 898176 109662506
Arthralgia 57.95 24.82 70 28547 779562 109781120
Neutropenia 57.94 24.82 13 28604 374607 110186075
Psychotic disorder 56.80 24.82 68 28549 50869 110509813
Asthenia 56.55 24.82 57 28560 688942 109871740
Rheumatoid arthritis 56.27 24.82 6 28611 299607 110261075
Sleep disorder 55.89 24.82 144 28473 198500 110362182
Anxiety 54.90 24.82 205 28412 344873 110215809
Inspiratory capacity abnormal 54.26 24.82 11 28606 102 110560580
Emphysema 53.71 24.82 43 28574 19713 110540969
Eosinophil count increased 53.38 24.82 44 28573 21014 110539668
Upper-airway cough syndrome 52.94 24.82 39 28578 15818 110544864
Bacteroides infection 52.94 24.82 22 28595 2897 110557785
Sepsis 51.68 24.82 194 28423 327152 110233530
Breath sounds abnormal 50.10 24.82 46 28571 25358 110535324
Drug ineffective 49.71 24.82 214 28403 1520326 109040356
Cholelithiasis 49.46 24.82 71 28546 63351 110497331
Venous pressure jugular increased 49.37 24.82 17 28600 1335 110559347
Hysterectomy 49.25 24.82 29 28588 8085 110552597
Hyperlipidaemia 48.68 24.82 53 28564 35795 110524887
Blood calcium increased 48.48 24.82 39 28578 18001 110542681
Kyphosis 47.81 24.82 21 28596 3166 110557516
Multiple allergies 47.47 24.82 33 28584 12230 110548452
Thrombocytopenia 46.69 24.82 16 28601 348869 110211813
Arthropathy 46.47 24.82 9 28608 287513 110273169
Dry mouth 44.42 24.82 133 28484 199815 110360867
Hypoacusis 44.29 24.82 50 28567 35141 110525541
Confusional state 44.17 24.82 34 28583 468646 110092036
Diaphragmatic disorder 43.85 24.82 17 28600 1869 110558813
Therapeutic product effect decreased 43.15 24.82 6 28611 244310 110316372
Secondary immunodeficiency 43.03 24.82 22 28595 4654 110556028
Diverticulum 42.65 24.82 34 28583 15492 110545190
Hepatotoxicity 42.32 24.82 66 28551 63334 110497348
C-reactive protein increased 41.86 24.82 4 28613 217915 110342767
Mobility decreased 41.53 24.82 6 28611 237416 110323266
Hypoaesthesia 41.03 24.82 15 28602 314208 110246474
Female genital tract fistula 40.80 24.82 34 28583 16485 110544197
Glossodynia 40.29 24.82 5 28612 221999 110338683
Rectal prolapse 38.81 24.82 17 28600 2546 110558136
Wound 38.60 24.82 7 28610 234430 110326252
Congenital anomaly 37.55 24.82 13 28604 1038 110559644
Abdominal pain 37.49 24.82 244 28373 512745 110047937
Eczema 37.23 24.82 67 28550 72226 110488456
Hypotension 36.83 24.82 49 28568 523800 110036882
Iron deficiency anaemia 36.62 24.82 43 28574 31516 110529166
Bronchial hyperreactivity 36.51 24.82 18 28599 3526 110557156
Blood bilirubin increased 36.09 24.82 68 28549 75904 110484778
Platelet count decreased 35.61 24.82 8 28609 230435 110330247
Pruritus 35.46 24.82 60 28557 581500 109979182
Tricuspid valve incompetence 35.42 24.82 37 28580 23836 110536846
White blood cell count decreased 35.37 24.82 8 28609 229382 110331300
Troponin increased 35.28 24.82 41 28576 29725 110530957
Stomatitis 35.11 24.82 13 28604 270229 110290453
Abdominal discomfort 34.11 24.82 31 28586 393827 110166855
General physical health deterioration 33.99 24.82 207 28410 425088 110135594
Acute kidney injury 33.96 24.82 71 28546 635359 109925323
Febrile neutropenia 33.82 24.82 20 28597 316747 110243935
Intentional product use issue 33.80 24.82 11 28606 247895 110312787
Inflammation 33.53 24.82 5 28612 193233 110367449
Gastroenteritis bacterial 33.35 24.82 10 28607 503 110560179
Lung opacity 33.04 24.82 26 28591 11626 110549056
Exposure during pregnancy 32.34 24.82 3 28614 167421 110393261
Psoriatic arthropathy 32.12 24.82 6 28611 196755 110363927
Congenital hiatus hernia 31.90 24.82 20 28597 6239 110554443
Product use issue 31.46 24.82 21 28596 311674 110249008
Musculoskeletal pain 31.15 24.82 5 28612 183018 110377664
Fall 30.94 24.82 69 28548 603413 109957269
Joint swelling 30.53 24.82 42 28575 442803 110117879
Ulcer 30.34 24.82 46 28571 43070 110517612
Therapy non-responder 29.91 24.82 3 28614 157304 110403378
Drug abuse 29.85 24.82 5 28612 177406 110383276
Disease progression 29.65 24.82 13 28604 244021 110316661
Cardiac failure congestive 29.42 24.82 96 28521 150904 110409778
Malignant neoplasm progression 29.20 24.82 5 28612 174562 110386120
Intentional product misuse 29.12 24.82 88 28529 132816 110427866
Chronic sinusitis 28.81 24.82 34 28583 25050 110535632
Abdominal pain upper 28.45 24.82 29 28588 349082 110211600
Pleural thickening 28.43 24.82 15 28602 3384 110557298
Liver injury 28.26 24.82 3 28614 150410 110410272
Dehydration 27.98 24.82 19 28598 279492 110281190
Blister 27.80 24.82 12 28605 227364 110333318
Systolic dysfunction 27.38 24.82 16 28601 4399 110556283
Pneumococcal infection 27.33 24.82 12 28605 1807 110558875
Seizure 26.52 24.82 12 28605 221173 110339509
Paraesthesia 26.11 24.82 20 28597 276501 110284181
Contusion 25.96 24.82 14 28603 233347 110327335
Radioallergosorbent test positive 25.79 24.82 5 28612 36 110560646
Alanine aminotransferase increased 25.32 24.82 8 28609 183765 110376917

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R03AL03 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03AL08 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC R03BB07 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Anticholinergics
FDA MoA N0000175370 Cholinergic Antagonists
FDA EPC N0000175574 Anticholinergic
CHEBI has role CHEBI:48876 muscarinic antagonist

Related Drugs by ATC class:

R03AL Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids 14 drugs
aclidinium bromidebeclometasone dipropionatebudesonidefenoterolfluticasone furoateformoterolglycopyrronium bromideindacaterolipratropiummometasone furoateolodaterolsalbutamol show all 14 →
R03BB Anticholinergics 6 drugs
aclidinium bromideglycopyrronium bromideipratropiumoxitropiumrevefenacintiotropium bromide

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

DiseaseRelationSNOMED_IDDOID
Chronic obstructive lung disease indication 13645005 DOID:3083
Chronic bronchitis indication 63480004 DOID:6132
Pulmonary emphysema indication 87433001
Asthma indication 195967001 DOID:2841




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION 8511304 June 14, 2027 INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH ANORO ELLIPTA GLAXOSMITHKLINE N203975 Dec. 18, 2013 RX POWDER INHALATION 11090294 Nov. 29, 2030 MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION 11090294 Nov. 29, 2030 MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) COMPRISING THE ONCE PER DAY ADMINISTRATION OF TRELEGY ELLIPTA, 100 MCG FLUTICASONE FUROATE/62.5 MCG UMECLIDINIUM/25 MCG VILANTEROL

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 10.22 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M5 GPCR ANTAGONIST Ki 9.90 IUPHAR
Muscarinic acetylcholine receptor M4 GPCR ANTAGONIST Ki 10.30 IUPHAR
Muscarinic acetylcholine receptor M1 GPCR Ki 9.80 SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M2 GPCR Ki 9.82 SCIENTIFIC LITERATURE

External reference:

IDSource
D10180 KEGG_DRUG
869185-19-3 SECONDARY_CAS_RN
4033108 VANDF
4033109 VANDF
CHEMBL1187833 ChEMBL_ID
CHEMBL523299 ChEMBL_ID
C573971 MESH_SUPPLEMENTAL_RECORD_UI
7354 IUPHAR_LIGAND_ID
DB09076 DRUGBANK_ID
GE2T1418SV UNII
1487512 RXNORM
29953 MMSL
402784 MMSL
d08187 MMSL
015344 NDDF
015345 NDDF
706898002 SNOMEDCT_US
706899005 SNOMEDCT_US
715611006 SNOMEDCT_US
C3661274 UMLSCUI
CHEBI:79040 CHEBI
11519070 PUBCHEM_CID
9551 INN_ID
GE2T1418SV INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Anoro Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0869 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA 27 sections
Anoro Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0869 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA 27 sections
Incruse Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0873 AEROSOL, POWDER 62.50 ug ORAL NDA 27 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0887 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA 26 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0893 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA 26 sections
Umeclidinium and Vilanterol Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 66993-134 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA authorized generic 29 sections
Umeclidinium and Vilanterol Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 66993-134 POWDER 62.50 ug RESPIRATORY (INHALATION) NDA authorized generic 29 sections
Umeclidinium Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 66993-189 AEROSOL, POWDER 62.50 ug ORAL NDA authorized generic 27 sections