fluticasone furoate Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4554 397864-44-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fluticasone furoate
  • avamys
  • veramyst
Fluticasone furoate is a synthetic trifluorinated corticosteroid with anti‑inflammatory activity. Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. The precise mechanism of corticosteroid action on asthma is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma.
  • Molecular weight: 538.58
  • Formula: C27H29F3O6S
  • CLOGP: 4.26
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 1
  • TPSA: 93.81
  • ALOGS: -4.09
  • ROTB: 6

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
0.20 mg N
0.11 mg N
0.60 mg Inhal.aerosol
0.60 mg Inhal.powder
1.50 mg Inhal.solution

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 4.95 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13.40 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 10.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
April 27, 2007 FDA GLAXOSMITHKLINE

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
Asthma 1122.13 12.44 696 27821 90846 46566699
Wheezing 496.07 12.44 342 28175 53044 46604501
Obstructive airways disorder 409.81 12.44 188 28329 13224 46644321
Dyspnoea 249.01 12.44 783 27734 514765 46142780
Blood count abnormal 220.72 12.44 137 28380 17741 46639804
Cough 212.19 12.44 447 28070 229802 46427743
Chronic obstructive pulmonary disease 206.19 12.44 213 28304 57420 46600125
Nasal polyps 146.60 12.44 54 28463 2156 46655389
Therapeutic product effect incomplete 144.85 12.44 207 28310 77946 46579599
Productive cough 135.62 12.44 161 28356 50554 46606991
Chest discomfort 105.53 12.44 194 28323 90075 46567470
Sleep disorder due to a general medical condition 88.24 12.44 43 28474 3456 46654089
Sputum discoloured 87.07 12.44 68 28449 12710 46644835
Nasal congestion 79.77 12.44 121 28396 47992 46609553
Respiratory symptom 72.68 12.44 32 28485 2038 46655507
Dyspnoea exertional 70.32 12.44 117 28400 50172 46607373
Lower respiratory tract infection 70.22 12.44 123 28394 54966 46602579
Embolism venous 69.87 12.44 33 28484 2474 46655071
Anosmia 69.25 12.44 38 28479 3906 46653639
Sleep apnoea syndrome 65.19 12.44 74 28443 22127 46635418
Toxicity to various agents 61.82 12.44 26 28491 211740 46445805
Sputum increased 61.18 12.44 27 28490 1729 46655816
Dysphonia 53.19 12.44 89 28428 38325 46619220
Dust allergy 50.73 12.44 17 28500 511 46657034
Sinusitis fungal 49.33 12.44 19 28498 859 46656686
Completed suicide 49.32 12.44 14 28503 145906 46511639
Chronic sinusitis 48.41 12.44 33 28484 5000 46652545
Gastrooesophageal reflux disease 48.11 12.44 126 28391 74218 46583327
Asthma-chronic obstructive pulmonary disease overlap syndrome 48.00 12.44 16 28501 473 46657072
Salpingo-oophorectomy unilateral 47.61 12.44 15 28502 369 46657176
Rheumatoid arthritis 46.40 12.44 47 28470 240168 46417377
Pneumonia 45.96 12.44 389 28128 375931 46281614
Forced expiratory volume decreased 45.65 12.44 32 28485 5072 46652473
Treatment failure 45.09 12.44 3 28514 93084 46564461
Total lung capacity increased 44.38 12.44 17 28500 757 46656788
Bronchitis 44.34 12.44 154 28363 105825 46551720
Secretion discharge 44.07 12.44 40 28477 9179 46648366
Malaise 42.34 12.44 346 28171 330886 46326659
Eosinophilic granulomatosis with polyangiitis 41.66 12.44 21 28496 1815 46655730
Bronchial haemorrhage 40.80 12.44 13 28504 332 46657213
Emphysema 40.79 12.44 38 28479 9016 46648529
Bronchiectasis 39.86 12.44 38 28479 9278 46648267
Bronchial disorder 39.60 12.44 17 28500 1018 46656527
Hyper IgE syndrome 37.44 12.44 11 28506 212 46657333
Bronchial neoplasm 36.25 12.44 11 28506 238 46657307
Idiopathic intracranial hypertension 35.51 12.44 21 28496 2488 46655057
Middle insomnia 35.48 12.44 36 28481 9479 46648066
Small cell carcinoma 35.27 12.44 10 28507 169 46657376
Nasal turbinate hypertrophy 34.15 12.44 12 28505 417 46657128
Sinusitis 33.90 12.44 163 28354 129605 46527940
Eosinophil count increased 33.49 12.44 32 28485 7834 46649711
Respiratory tract inflammation 33.46 12.44 12 28505 443 46657102
Eczema 33.36 12.44 51 28466 20349 46637196
Rales 33.31 12.44 35 28482 9596 46647949
Female genital tract fistula 32.98 12.44 22 28495 3217 46654328
Blood test abnormal 31.87 12.44 34 28483 9486 46648059
Lung neoplasm malignant 31.58 12.44 43 28474 15446 46642099
Tooth injury 30.72 12.44 14 28503 967 46656578
Eye pruritus 30.50 12.44 37 28480 11861 46645684
Haemoptysis 30.19 12.44 56 28461 26133 46631412
Rhinitis 29.64 12.44 30 28487 7876 46649669
Rhinitis allergic 29.22 12.44 28 28489 6880 46650665
Intentional overdose 28.95 12.44 3 28514 64941 46592604
Eosinophilia 28.59 12.44 46 28471 19171 46638374
Asthmatic crisis 28.06 12.44 15 28502 1463 46656082
Urticaria 27.89 12.44 144 28373 117748 46539797
Drug hypersensitivity 27.74 12.44 68 28449 243757 46413788
Reversible airways obstruction 27.60 12.44 11 28506 545 46657000
Subclavian vein thrombosis 27.57 12.44 16 28501 1830 46655715
Respiratory gas exchange disorder 27.46 12.44 10 28507 386 46657159
Throat clearing 26.98 12.44 10 28507 406 46657139
Oesophageal spasm 26.47 12.44 16 28501 1973 46655572
Macular degeneration 26.39 12.44 27 28490 7178 46650367
Overdose 25.97 12.44 15 28502 101964 46555581
Endometrial ablation 25.15 12.44 11 28506 689 46656856
Alopecia 24.81 12.44 38 28479 162376 46495169
Influenza 24.66 12.44 114 28403 89156 46568389
Synovitis 24.39 12.44 4 28513 61071 46596474
Aphonia 24.20 12.44 27 28490 7918 46649627
Thrombocytopenia 24.14 12.44 25 28492 126556 46530989
Febrile neutropenia 23.98 12.44 14 28503 94613 46562932
Bronchial obstruction 23.93 12.44 13 28504 1309 46656236
Diastolic dysfunction 23.43 12.44 22 28495 5270 46652275
Sputum purulent 23.18 12.44 11 28506 833 46656712
Angioedema 22.75 12.44 64 28453 39278 46618267
Lung hyperinflation 22.58 12.44 12 28505 1157 46656388
Rhonchi 22.44 12.44 15 28502 2200 46655345
Ligament pain 22.26 12.44 7 28510 171 46657374
Ageusia 22.12 12.44 31 28486 11441 46646104
Swelling face 22.08 12.44 77 28440 52982 46604563
Restrictive pulmonary disease 22.04 12.44 12 28505 1214 46656331
Sarcoidosis 21.99 12.44 21 28496 5138 46652407
Throat irritation 21.85 12.44 52 28465 28849 46628696
Contraindicated product administered 21.46 12.44 11 28506 79936 46577609
Lactose intolerance 21.30 12.44 15 28502 2394 46655151
Hyperplastic cholecystopathy 21.13 12.44 6 28511 102 46657443
Suicide attempt 21.12 12.44 4 28513 55032 46602513
Pulmonary function test decreased 21.11 12.44 18 28499 3802 46653743
Pancytopenia 20.97 12.44 13 28504 85045 46572500
Parotid gland enlargement 20.75 12.44 10 28507 784 46656761
Oropharyngeal pain 20.69 12.44 95 28422 74073 46583472
Oesophageal pain 20.57 12.44 15 28502 2528 46655017
Neutropenia 20.46 12.44 35 28482 143169 46514376
Rhinorrhoea 19.68 12.44 69 28448 47596 46609949
Sneezing 19.64 12.44 31 28486 12710 46644835
Breath sounds abnormal 19.54 12.44 24 28493 7791 46649754
Sinus pain 19.51 12.44 13 28504 1897 46655648
Drug ineffective 18.95 12.44 296 28221 677542 45980003
Palpitations 18.93 12.44 111 28406 95148 46562397
Seizure 18.58 12.44 29 28488 123025 46534520
Lip swelling 18.46 12.44 45 28472 25350 46632195
Dizziness 18.42 12.44 301 28216 340113 46317432
Nasopharyngitis 18.08 12.44 158 28359 153840 46503705
Blood immunoglobulin E increased 17.95 12.44 12 28505 1761 46655784
Candida infection 17.89 12.44 41 28476 22199 46635346
Atopy 17.76 12.44 6 28511 185 46657360
Bronchospasm 17.37 12.44 33 28484 15674 46641871
Oral pruritus 17.32 12.44 11 28506 1480 46656065
Eosinophilic oesophagitis 17.17 12.44 6 28511 205 46657340
Blood creatinine increased 17.07 12.44 13 28504 76390 46581155
Allergy to animal 16.81 12.44 8 28509 610 46656935
White blood cell count decreased 16.43 12.44 27 28490 112204 46545341
Upper-airway cough syndrome 16.32 12.44 22 28495 7825 46649720
Staphylococcus test positive 16.06 12.44 15 28502 3569 46653976
Ear pruritus 16.01 12.44 12 28505 2108 46655437
Nasal inflammation 15.91 12.44 7 28510 445 46657100
Aspartate aminotransferase increased 15.62 12.44 15 28502 78685 46578860
Sensitivity to weather change 15.54 12.44 18 28499 5498 46652047
Blood pressure systolic abnormal 15.53 12.44 18 28499 5499 46652046
Contraindicated product prescribed 15.45 12.44 8 28509 731 46656814
Tricuspid valve incompetence 15.39 12.44 29 28488 13688 46643857
Aspirin-exacerbated respiratory disease 15.36 12.44 8 28509 740 46656805
Sinus congestion 15.07 12.44 28 28489 13081 46644464
Anaemia 15.06 12.44 93 28424 255686 46401859
Nicotine dependence 14.93 12.44 7 28510 516 46657029
Hepatic enzyme increased 14.65 12.44 17 28500 81770 46575775
Pruritus 14.50 12.44 218 28299 242134 46415411
Stent placement 14.26 12.44 14 28503 3542 46654003
Off label use 14.19 12.44 156 28361 379685 46277860
Dyspnoea at rest 14.16 12.44 14 28503 3574 46653971
Increased bronchial secretion 14.16 12.44 10 28507 1604 46655941
Subclavian artery thrombosis 14.09 12.44 5 28512 179 46657366
Pertussis 14.04 12.44 7 28510 591 46656954
Blood pressure increased 13.85 12.44 128 28389 126538 46531007
Disease recurrence 13.71 12.44 33 28484 18438 46639107
Blood pressure diastolic abnormal 13.64 12.44 18 28499 6276 46651269
Lacrimation increased 13.60 12.44 30 28487 15831 46641714
Vomiting 13.54 12.44 195 28322 452599 46204946
Granuloma 13.49 12.44 14 28503 3784 46653761
Nasal mucosal disorder 13.48 12.44 6 28511 392 46657153
Product quality issue 13.35 12.44 50 28467 35598 46621947
Pneumonia respiratory syncytial viral 13.22 12.44 7 28510 670 46656875
Weight increased 13.17 12.44 156 28361 164317 46493228
Polycystic ovaries 13.13 12.44 9 28508 1375 46656170
Inspiratory capacity decreased 13.12 12.44 4 28513 88 46657457
Increased viscosity of upper respiratory secretion 12.99 12.44 4 28513 91 46657454
Respiratory tract infection 12.90 12.44 44 28473 29928 46627617
Bronchial hyperreactivity 12.89 12.44 9 28508 1417 46656128
Adenoma benign 12.83 12.44 7 28510 711 46656834
Blood pressure diastolic increased 12.81 12.44 17 28500 5957 46651588
Venous pressure jugular increased 12.75 12.44 6 28511 446 46657099
Arthropathy 12.75 12.44 20 28497 84680 46572865
Visceral pain 12.63 12.44 3 28514 24 46657521

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 852.90 13.55 414 16665 35760 29899639
Wheezing 387.34 13.55 233 16846 30705 29904694
Chronic obstructive pulmonary disease 375.16 13.55 265 16814 45861 29889538
Obstructive airways disorder 330.96 13.55 141 16938 8918 29926481
Therapeutic product effect incomplete 251.05 13.55 184 16895 33650 29901749
Blood count abnormal 205.70 13.55 110 16969 11542 29923857
Dyspnoea 202.90 13.55 526 16553 332769 29602630
Cough 182.91 13.55 286 16793 125356 29810043
Sputum discoloured 155.59 13.55 76 17003 6592 29928807
Nasal congestion 128.67 13.55 97 16982 18469 29916930
Asthma-chronic obstructive pulmonary disease overlap syndrome 128.12 13.55 36 17043 633 29934766
Bronchiectasis 114.51 13.55 57 17022 5147 29930252
Sinus pain 113.55 13.55 33 17046 658 29934741
Nasal obstruction 109.55 13.55 32 17047 650 29934749
Bronchial obstruction 103.86 13.55 37 17042 1439 29933960
Forced expiratory volume decreased 100.45 13.55 45 17034 3205 29932194
Chest discomfort 99.40 13.55 126 16953 45354 29890045
Lower respiratory tract infection 96.15 13.55 96 16983 26618 29908781
Mycobacterium avium complex infection 82.07 13.55 37 17042 2674 29932725
Lung consolidation 79.70 13.55 44 17035 4908 29930491
Pulmonary function test decreased 77.03 13.55 41 17038 4254 29931145
Middle insomnia 76.03 13.55 45 17034 5728 29929671
Productive cough 60.73 13.55 80 16999 29873 29905526
Throat irritation 57.73 13.55 44 17035 8504 29926895
Blood immunoglobulin E increased 56.82 13.55 25 17054 1705 29933694
Sleep disorder due to a general medical condition 56.79 13.55 24 17055 1483 29933916
Nasal polyps 55.45 13.55 23 17056 1356 29934043
Lymph node calcification 52.92 13.55 14 17065 194 29935205
Pulmonary mass 52.48 13.55 46 17033 10816 29924583
Foetal malformation 52.23 13.55 13 17066 139 29935260
Vocal cord dysfunction 50.41 13.55 13 17066 162 29935237
Osteopenia 50.39 13.55 32 17047 4616 29930783
Emphysema 49.86 13.55 42 17037 9360 29926039
Pneumonia 49.80 13.55 343 16736 333963 29601436
Anosmia 46.18 13.55 23 17056 2077 29933322
Trisomy 18 46.18 13.55 13 17066 230 29935169
Rhinitis 46.00 13.55 30 17049 4529 29930870
Toxicity to various agents 45.68 13.55 22 17057 177161 29758238
Completed suicide 45.00 13.55 3 17076 99489 29835910
Appendicolith 42.68 13.55 17 17062 902 29934497
Forced vital capacity decreased 41.94 13.55 16 17063 756 29934643
Blood test abnormal 40.78 13.55 30 17049 5495 29929904
Lung hyperinflation 40.44 13.55 16 17063 834 29934565
Cortisol decreased 39.25 13.55 16 17063 902 29934497
Eosinophil count 39.12 13.55 10 17069 120 29935279
Nasal disorder 38.71 13.55 17 17062 1154 29934245
Pancytopenia 37.21 13.55 3 17076 85049 29850350
Respiratory disorder 32.81 13.55 45 17034 17449 29917950
Bronchial disorder 32.60 13.55 14 17065 900 29934499
Suffocation feeling 31.78 13.55 12 17067 551 29934848
Rhinitis allergic 31.56 13.55 20 17059 2874 29932525
Platelet count decreased 30.83 13.55 11 17068 106118 29829281
Total lung capacity abnormal 30.61 13.55 9 17070 187 29935212
Bronchial hyperreactivity 28.97 13.55 14 17065 1184 29934215
Bronchial wall thickening 26.85 13.55 10 17069 442 29934957
Secretion discharge 26.74 13.55 20 17059 3755 29931644
Drug abuse 26.55 13.55 7 17072 82065 29853334
Sputum increased 25.83 13.55 15 17064 1842 29933557
Perfume sensitivity 25.70 13.55 7 17072 109 29935290
Nasal oedema 25.56 13.55 9 17070 338 29935061
Eosinophilic granulomatosis with polyangiitis 24.84 13.55 13 17066 1302 29934097
Central obesity 24.80 13.55 10 17069 548 29934851
Gastrooesophageal reflux disease 24.79 13.55 56 17023 32199 29903200
Oropharyngeal pain 24.78 13.55 52 17027 28444 29906955
Sinusitis 24.64 13.55 57 17022 33288 29902111
Dermatitis atopic 24.43 13.55 12 17067 1052 29934347
Pharyngeal paraesthesia 24.29 13.55 9 17070 392 29935007
Vital capacity decreased 24.20 13.55 9 17070 396 29935003
Thrombocytopenia 23.61 13.55 26 17053 137018 29798381
Infective exacerbation of chronic obstructive airways disease 23.58 13.55 13 17066 1445 29933954
Eosinophil count increased 23.51 13.55 25 17054 7448 29927951
Loss of personal independence in daily activities 23.20 13.55 43 17036 21492 29913907
Rhinorrhoea 23.06 13.55 42 17037 20712 29914687
Neutropenia 22.57 13.55 24 17055 128516 29806883
Polyp 22.46 13.55 17 17062 3249 29932150
Cortisol increased 21.87 13.55 7 17072 195 29935204
Convulsive threshold lowered 21.87 13.55 9 17070 520 29934879
Crepitations 21.38 13.55 16 17063 3008 29932391
Lung disorder 21.31 13.55 52 17027 31417 29903982
Death 20.90 13.55 302 16777 356981 29578418
Hospitalisation 20.79 13.55 64 17015 44255 29891144
Nasal inflammation 20.71 13.55 7 17072 232 29935167
Growth retardation 19.84 13.55 12 17067 1588 29933811
Bronchitis 18.81 13.55 57 17022 39068 29896331
Faecal calprotectin 18.73 13.55 4 17075 20 29935379
Otosalpingitis 18.73 13.55 4 17075 20 29935379
Alpha 2 globulin decreased 18.73 13.55 4 17075 20 29935379
Diarrhoea 18.66 13.55 113 16966 333990 29601409
Bronchopulmonary aspergillosis allergic 18.59 13.55 7 17072 319 29935080
Sex hormone binding globulin decreased 18.56 13.55 4 17075 21 29935378
Free androgen index decreased 18.56 13.55 4 17075 21 29935378
Panic reaction 18.49 13.55 11 17068 1412 29933987
Viral acanthoma 18.41 13.55 4 17075 22 29935377
Androgen insensitivity syndrome 18.41 13.55 4 17075 22 29935377
Upper-airway cough syndrome 18.40 13.55 14 17065 2696 29932703
Meralgia paraesthetica 18.35 13.55 6 17073 179 29935220
Creatinine urine decreased 18.26 13.55 4 17075 23 29935376
Adrenal insufficiency 18.25 13.55 26 17053 10437 29924962
Breath sounds abnormal 18.23 13.55 18 17061 4917 29930482
Blood pressure diastolic increased 18.19 13.55 14 17065 2744 29932655
Testicular microlithiasis 18.11 13.55 4 17075 24 29935375
Dehydroepiandrosterone decreased 18.11 13.55 4 17075 24 29935375
Urine calcium/creatinine ratio increased 17.97 13.55 4 17075 25 29935374
Eye infection 17.81 13.55 14 17065 2828 29932571
Gastroenteritis eosinophilic 17.69 13.55 6 17073 201 29935198
Nasal discomfort 17.42 13.55 10 17069 1201 29934198
Blood creatinine increased 17.25 13.55 16 17063 91359 29844040
Nasal septum deviation 17.11 13.55 9 17070 911 29934488
Blood immunoglobulin G decreased 16.93 13.55 9 17070 931 29934468
Oxygen consumption increased 16.85 13.55 10 17069 1278 29934121
Carbon dioxide increased 16.20 13.55 9 17070 1016 29934383
Pulmonary function test abnormal 16.11 13.55 10 17069 1386 29934013
Asthmatic crisis 16.04 13.55 7 17072 468 29934931
Malaise 15.86 13.55 155 16924 166807 29768592
Apnoeic attack 15.74 13.55 6 17073 283 29935116
Urine phosphorus decreased 15.73 13.55 4 17075 47 29935352
Post 5-alpha-reductase inhibitor syndrome 15.57 13.55 4 17075 49 29935350
Dyspnoea exertional 15.54 13.55 50 17029 35380 29900019
Febrile neutropenia 15.51 13.55 23 17056 106670 29828729
Snoring 15.50 13.55 13 17066 2878 29932521
Alanine aminotransferase increased 15.25 13.55 12 17067 74264 29861135
Lipohypertrophy 15.03 13.55 6 17073 320 29935079
Appendicitis 14.97 13.55 18 17061 6126 29929273
Hand dermatitis 14.96 13.55 5 17074 160 29935239
Blue toe syndrome 14.81 13.55 5 17074 165 29935234
Lung opacity 14.72 13.55 8 17071 865 29934534
Pain 14.64 13.55 50 17029 172591 29762808
Choking 14.60 13.55 16 17063 4930 29930469
Multiple allergies 14.40 13.55 11 17068 2132 29933267
Eosinophilia 14.34 13.55 36 17043 22124 29913275
Somnambulism 14.31 13.55 13 17066 3201 29932198
Spleen congestion 14.21 13.55 6 17073 370 29935029
Renal failure 14.14 13.55 33 17046 128933 29806466
Adrenal suppression 14.12 13.55 7 17072 626 29934773
Transient psychosis 14.04 13.55 3 17076 15 29935384
Total lung capacity decreased 14.04 13.55 7 17072 633 29934766
Fear of crowded places 14.04 13.55 3 17076 15 29935384
Muscle tone disorder 13.99 13.55 4 17075 75 29935324
Eye pruritus 13.90 13.55 14 17065 3913 29931486
Convulsions local 13.88 13.55 3 17076 16 29935383
Myotonic dystrophy 13.84 13.55 4 17075 78 29935321
Prolonged expiration 13.80 13.55 5 17074 204 29935195
Cataract 13.64 13.55 35 17044 21800 29913599
Blood immunoglobulin M decreased 13.59 13.55 6 17073 412 29934987

Pharmacologic Action:

SourceCodeDescription
ATC R01AD12 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R03BA09 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Glucocorticoids
ATC R03AK10 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AL08 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC D07AC17 DERMATOLOGICALS
CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
CORTICOSTEROIDS, PLAIN
Corticosteroids, potent (group III)
ATC R01AD08 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R01AD58 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Corticosteroids
ATC R03AK06 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03AK11 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
ADRENERGICS, INHALANTS
Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC R03BA05 RESPIRATORY SYSTEM
DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
Glucocorticoids
CHEBI has role CHEBI:49167 anti-asthmatic agents
CHEBI has role CHEBI:50857 anti-allergic agents
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D003879 Dermatologic Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents
FDA EPC N0000175576 Corticosteroid
FDA MoA N0000175450 Corticosteroid Hormone Receptor Agonists
CHEBI has role CHEBI:50266 prodrugs

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Allergic rhinitis indication 61582004
Asthma indication 195967001 DOID:2841
Chronic Non-Allergic Rhinitis indication
Mycosis contraindication 3218000 DOID:1564
Ocular hypertension contraindication 4210003 DOID:9282
Epistaxis contraindication 12441001
Measles contraindication 14189004 DOID:8622
Disease caused by parasite contraindication 17322007
Glaucoma contraindication 23986001 DOID:1686
Viral disease contraindication 34014006 DOID:934
Hypercortisolism contraindication 47270006
Perforation of nasal septum contraindication 80142000
Bacterial infectious disease contraindication 87628006
Operation on nose contraindication 88733004
Bilateral cataracts contraindication 95722004
Pulmonary tuberculosis contraindication 154283005 DOID:2957
Ophthalmic herpes simplex contraindication 186542001
Varicella-zoster virus infection contraindication 309465005
Adrenal cortical hypofunction contraindication 386584007 DOID:10493
Exposure to varicella contraindication 444453009
Nasal Candidiasis contraindication
Nasal Septal Ulcers contraindication
Nasal Trauma contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.49 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION April 24, 2021 REVISED INDICATION FOR FIXED-DOSE COMBINULLTION OF FLUTICASONE FUROATE, UMECLIDINIUM, AND VILANTEROL TO TREAT AIRFLOW OBSTRUCTION IN CHRONIC OBSTRUCTIVE PULMONULLRY DISEASE (COPD) AND TO REDUCE COPD EXACERBATIONS IN PTS WITH HISTORY OF EXACERBATIONS
0.05MG/INH ARNUITY ELLIPTA GLAXOSMITHKLINE N205625 May 17, 2018 RX POWDER INHALATION May 17, 2021 NEW STRENGTH
0.1MG/INH ARNUITY ELLIPTA GLAXOSMITHKLINE N205625 Aug. 20, 2014 RX POWDER INHALATION May 17, 2021 NEW PATIENT POPULATION
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 18, 2017 RX POWDER INHALATION Sept. 9, 2023 MAINTENULLNCE TREATMENT OF ASTHMA IN PATIENTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH TRELEGY ELLIPTA GLAXOSMITHKLINE N209482 Sept. 9, 2020 RX POWDER INHALATION Sept. 9, 2023 NEW STRENGTH

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glucocorticoid receptor Nuclear hormone receptor AGONIST IC50 10.12 CHEMBL CHEMBL
Glucocorticoid receptor Transcription factor IC50 8.30 CHEMBL

External reference:

IDSource
D06315 KEGG_DRUG
4026165 VUID
N0000179800 NUI
90566-53-3 SECONDARY_CAS_RN
4020529 VANDF
4026165 VANDF
C0720466 UMLSCUI
C0082607 UMLSCUI
CHEBI:74899 CHEBI
CHEBI:5134 CHEBI
GW6 PDB_CHEM_ID
CHEMBL1676 ChEMBL_ID
DB08906 DRUGBANK_ID
CHEMBL1473 ChEMBL_ID
9854489 PUBCHEM_CID
D000068298 MESH_DESCRIPTOR_UI
C523187 MESH_SUPPLEMENTAL_RECORD_UI
10892 IUPHAR_LIGAND_ID
8521 INN_ID
5636 INN_ID
JS86977WNV UNII
CUT2W21N7U UNII
5311101 PUBCHEM_CID
6699 IUPHAR_LIGAND_ID
DB13867 DRUGBANK_ID
41126 RXNORM
109674 MMSL
23848 MMSL
51966 MMSL
d01296 MMSL
004952 NDDF
012173 NDDF
108632003 SNOMEDCT_US
397192001 SNOMEDCT_US
426409006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
FLONULLSE SENSIMISTALLERGY RELIEF HUMAN OTC DRUG LABEL 1 0135-0615 SPRAY, METERED 27.50 ug NULLSAL NDA 16 sections
FLONULLSE SENSIMISTALLERGY RELIEF HUMAN OTC DRUG LABEL 1 0135-0616 SPRAY, METERED 27.50 ug NULLSAL NDA 16 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0859 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Arnuity Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0874 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Arnuity Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0876 POWDER 200 ug RESPIRATORY (INHALATION) NDA 27 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 0173-0882 POWDER 200 ug RESPIRATORY (INHALATION) NDA 27 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0887 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections
Arnuity Ellipta HUMAN PRESCRIPTION DRUG LABEL 1 0173-0888 POWDER 50 ug RESPIRATORY (INHALATION) NDA 27 sections
Trelegy Ellipta HUMAN PRESCRIPTION DRUG LABEL 3 0173-0893 POWDER 200 ug RESPIRATORY (INHALATION) NDA 27 sections
Veramyst HUMAN PRESCRIPTION DRUG LABEL 1 54868-6168 SPRAY, METERED 27.50 ug NULLSAL NDA 27 sections
Breo Ellipta HUMAN PRESCRIPTION DRUG LABEL 2 70518-2028 POWDER 100 ug RESPIRATORY (INHALATION) NDA 27 sections